5-HT Receptor

Choose Selective 5-HT Receptor Inhibitors

5-HT Receptor Signaling Pathway Map

5-HT Receptor Signaling Pathways

5-HT Receptor Products

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  • New 5-HT Receptor Products
Catalog No. Product Name Information Product Use Citations Product Validations
S1333 Fluoxetine (Lilly 110140) HCl Fluoxetine HCl (Lilly110140) is a selective serotonin-reuptake inhibitor (SSRI) at the neuronal membrane, used in the treatment of depression.
FASEB J, 2021, 35(5):e21581
Sci Rep, 2021, 11(1):1250
Endocrine, 2021, 10.1007/s12020-021-02818-7
S1483 Iloperidone Iloperidone (HP873) is a dopamine (D2)/serotonin (5-HT2) receptor antagonist, used for the treatment of schizophrenia.
Anticancer Res, 2021, 41(2):687-697
Sci Rep, 2018, 8(1):15753
S1642 Methyldopa Methyldopa (Aldomet) is a DOPA decarboxylase competitive inhibitor with an ED50 of 21.8 mg/kg.
S1869 Dapoxetine HCl Dapoxetine HCl (LY-210448) is a short-acting novel selective serotonin reuptake inhibitor, used for the treatment of premature ejaculation.
S2084 Duloxetine HCl Duloxetine HCl (LY-248686) is a serotonin-norepinephrine reuptake inhibitor with Ki of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD).
Drug Metab Dispos, 2015, 44(3):378-88
J Pharmacol Exp Ther, 2014, 349(3):402-7
Am J Physiol Renal Physiol, 2013, 305(12):F1663-8
S2464 Sevoflurane Sevoflurane (Fluoromethyl) is a noncompetitive inhibitor of 5-HT3 receptor. Sevoflurane acts as a low-soluble inhalation anesthetics.
ACS Chem Neurosci, 2021, 10.1021/acschemneuro.1c00131
S2582 Trazodone HCl Trazodone HCl (AF-1161, KB-831) is an antidepressant belonging to the class of serotonin receptor antagonists and reuptake inhibitors for treatment of anxiety disorders.
S3024 Lamotrigine Lamotrigine (BW-430C) is a novel anticonvulsant drug for inhibition of 5-HT with IC50 of 240 μM and 474 μM in human platelets and rat brain synaptosomes, and also is a sodium channel blocker.
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 34(6):1911-1918
Hum Cell, 2021, 10.1007/s13577-021-00579-z
S3175 Atomoxetine HCl Atomoxetine (LY 139603) is a selective norepinephrine (NE) transporter inhibitor with Ki of 5 nM, with 15- and 290-fold lower affinity for human 5-HT and DA transporters.
S3183 Amitriptyline HCl Amitriptyline HCl is an inhibitor of both serotonin transporter (SERT) and norepinephrine transporter (NET) with Ki of 3.45 nM and 13.3 nM, respectively. Amitriptyline HCl also inhibits histamine receptor H1, histamine receptor H4, 5-HT2 and sigma 1 receptor with Ki of 0.5 nM, 7.31 nM, 235 nM and 287 nM, respectively. Amitriptyline is a tricyclic antidepressant (TCA).
Environ Toxicol Chem, 2021, 10.1002/etc.5018
PLoS Pathog, 2020, 16;16(3):e1008341
Sci Rep, 2018, 8(1):15753
S3817 Harmine hydrochloride Harmine (Telepathine), a fluorescent harmala alkaloid belonging to the beta-carboline family of compounds, is a highly cell-permeant and competitive inhibitor of ATP binding to the kinase pocket of DYRK1A, with about 60-fold higher IC50 value for DYRK2. Harmine also inhibits monoamine oxidases (MAOs) and cdc-like kinases (CLKs). Harmine inhibits 5-HT2A serotonin receptor with Ki of 397 nM.
S3913New Pimethixene maleate Pimethixene (Pimetixene) maleate, an antihistamine, anntimigraine agent and antiserotonergic compound, is a highly potent antagonist of a broad range of monoamine receptors, including a variety of serotonin receptors. Pimethixene maleate inhibits 5-HT2A, 5-HT2B, 5-HT2C, 5-HT1A, 5-HT1B, 5-HT6, 5-HT7, Adrenergic α-1A, Dopamine D1 Receptor, Dopamine D2 Receptor, Dopamine D4.4 Receptor, Histamine H1 Receptor, Muscarinic M1 and Muscarinic M2 with pKi of 10.22, 10.44, 8.42, 7.63, < 5, 7.30, 7.28, 7.61, 6.37, 8.19, 7.54, 10.14, 8.61 and 9.38, respectively.
S4053 Sertraline HCl Sertraline HCl (CP-51974-1) is a 5-HT antagonist with Ki of 13 nM.
Antimicrob Agents Chemother, 2021, AAC.01146-20
Sci Rep, 2021, 11(1):1250
J Glob Antimicrob Resist, 2021, 27:167-171
S4064 Escitalopram Oxalate Escitalopram Oxalate is a selective serotonin (5-HT) reuptake inhibitor (SSRI) with Ki of 0.89 nM.
S4377 Imipramine HCl Imipramine (Melipramine) is a tricyclic antidepressant (TCA) of the dibenzazepine group, mainly used in the treatment of major depression and enuresis (inability to control urination).
Antioxidants (Basel), 2021, 10(6)956
S4749 Citalopram HBr Citalopram HBr (Nitalapram HBr, Prepram HBr, Bonitrile HBr, Lu 10-171 HBr), an antidepressant, is an orally administered selective serotonin reuptake inhibitor (SSRI) with IC50 of 1.8 nM.
Aging (Albany NY), 2021, 13(11):14729-14744
Sci Rep, 2021, 11(1):1250
Viruses, 2021, 13(8)1533
S5071 Duloxetine Duloxetine (LY-248686) is a potent inhibitor of serotonin (5-hydroxytryptamine, 5-HT) and noradrenaline (NE) uptake in vitro and in vivo and is 3- to 5-times more effective at inhibiting 5-HT uptake.
S5485 Desipramine Hydrochloride Desipramine hydrochloride (Desmethylimipramine, Norimipramine, EX-4355, G-35020, JB-8181, NSC-114901) is a dibenzazepine-derivative tricyclic antidepressant that acts as a selective norepinephrine reuptake inhibitor. It also shows weak serotonin reuptake inhibitory, α1-blocking, antihistamine, and anticholinergic effects.
S5563 Thioridazine hydrochloride Thioridazine (Aldazine, Mellaril) is a potent antianxiety and antipsychotic agent.
Cell Syst, 2019, 8(2):97-108
S8183 Pimavanserin Pimavanserin (ACP-103) is a potent and selective serotonin 5-HT2A inverse agonist with pIC50 of 8.73, used to treat psychosis associated with Parkinson’s disease.
Br J Pharmacol, 2021, 10.1111/bph.15756
Mol Ther Oncolytics, 2020, 19:19-32
ACS Chem Neurosci, 2020, 11(2):173-183
S9039 Albiflorin Albiflorin, a natural product isolated from Paeoniae Radix, is a novel 5-HT and NE reuptake inhibitor with high selectivity.
S9239 Isocorynoxeine Isocorynoxeine (7-Isocorynoxeine), a major alkaloid found in Uncaria rhynchophylla, exhibits wide beneficial effects on the cardiovascular and cardiocerebral vascular systems. Isocorynoxeine suppress 5-HT2A receptor-mediated current response with IC50 of 72.4 μM.
S9258 (+)-Isocorynoline Isocorynoxeine, a major bioactive tetracyclic oxindole alkaloids found in Uncaria rhynchophylla, exhibits a dose-dependent inhibition of 5-HT2A receptor-mediated current response with an IC50 of 72.4 μM and shows various beneficial effects, including lowering blood pressure, vasodilatation, and protection against ischemia-induced neuronal damage.
S9510 Protriptyline hydrochloride Protriptyline Hydrochloride is the hydrochloride salt form of protriptyline. Protriptyline is a tricyclic secondary amine with antidepressant property which acts by inhibition of serotonin and norepinephrine reuptake.
S4740 Sodium ferulate Sodium ferulate (SF, Ferulic acid sodium salt), the sodium salt of ferulic acid, is a drug used in traditional Chinese medicine for treatment of cardiovascular and cerebrovascular diseases and to prevent thrombosis.
S0313 Volinanserin Volinanserin (Volinanserin Hydrochloride Salt, MDL100907, M 100907, MDL-100,907) is a highly selective and potent 5-HT2 receptor antagonist with Ki of 0.36 nM. Volinanserin shows antipsychotic activity.
S0779 Pirenperone Pirenperone (R-47456, R-50656), a quinazoline derivative, is a selective antagonist of SR-2A (5-HT2 serotonin receptor) when employed in low doses. Pirenperone behaves like a typical neuroleptic when used in higher doses (greater than 0.1 mg/kg).
S1243 Agomelatine (S20098) Agomelatine (S20098) is classified as a norepinephrine-dopamine disinhibitor (NDDI) due to its antagonism of the 5-HT2C receptor.
Sci Rep, 2018, 8(1):15753
Neuropsychiatry (London), 2018, None
Arch Oral Biol, 2017, 82:11-18
S1245 Latrepirdine 2HCl Latrepirdine is an orally active,and neuroactive antagonist of multiple drug targets, including histamine receptors, GluR, and 5-HT receptors, used as an antihistamine drug.
S1283 Asenapine maleate Asenapine maleate (Org 5222) is a high-affinity antagonist of serotonin, norepinephrine, dopamine and histamine receptors, used for the treatment of schizophrenia and acute mania associated with bipolar disorder.
Biochem Biophys Res Commun, 2021, 553:172-179
Anticancer Res, 2021, 41(2):687-697
Sci Rep, 2018, 8(1):15753
S1345 Granisetron HCl Granisetron is a serotonin 5-HT3 receptor antagonist,used to treat chemotherapy-induced nausea and vomiting.
S1390 Ondansetron HCl Ondansetron HCl (GR 38032F) is a serotonin 5-HT3 receptor antagonist, used to prevent nausea and vomiting caused by cancer chemotherapy, and radiation therapy.
Immunity, 2019, 50(5):1163-1171
Int J Urol, 2016, 23(11):946-951
S1394 Pizotifen Malate Pizotifen Malate (BC-105) is a benzocycloheptane based agent used for recurrent migraine headaches.
S1444 Ziprasidone HCl Ziprasidone HCl (CP-88059) is a novel and potent dopamine and serotonin (5-HT) receptor antagonist, used in the treatment of schizophrenia and bipolar disorder.
Anticancer Res, 2021, 41(2):687-697
Molecules, 2020, 25(18)E4206
Nature, 2018, 560(7718):372-376
S1615 Risperidone Risperidone (R-64766) is a mutil-targeted antagonist for dopamine, serotonin, adrenergic and histamine receptors, used to treat schizophrenia and bipolar disorder.
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00196-X
Anticancer Res, 2021, 41(2):687-697
BMC Evol Biol, 2018, 18(1):89
S1898 Tropisetron HCl Tropisetron HCl (ICS 205-930) is a potent and selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist, used to treat nausea and vomiting following chemotherapy.
S1996 Ondansetron Ondansetron (GR 38032F, GR-C507/75) is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic.
Int J Urol, 2016, 23(11):946-951
S2016 Mirtazapine Mirtazapine (Org3770) is an adrenergic and seroton receptor antagonist, used to treat depression.
S2106 Azasetron HCl Azasetron HCl (Y-25130) is a selective 5-HT3 receptor antagonist with IC50 of 0.33 nM used in the management of nausea and vomiting induced by cancer chemotherapy.
S2112 Blonanserin Blonanserin (AD 5423) is a relatively selective serotonin (5-HT)2A and dopamine D2 antagonist, used the treatment of schizophrenia.
Sci Rep, 2018, 8(1):15753
S2232 Ketanserin Ketanserin (R41468) is a specific 5-HT2A serotonin receptor antagonist with Ki of 2.5 nM for rat and human 5-HT2A, used as an antihypertensive drug.
Lab Invest, 2021, 1-14
Int Immunopharmacol, 2019, 10.1016/j.intimp.2019.106036
Sci Rep, 2018, 8(1):15753
S2346 Puerarin Puerarin (Kakonein), an isoflavones found in the root of Radix puerariae, is a 5-HT2C receptor and benzodiazepine site antagonist.
Biochim Biophys Acta Mol Cell Res, 2022, S0167-4889(21)00262-7
Front Pharmacol, 2021, 12:632825
Int J Mol Sci, 2020, 21(14):5025
S2459 Clozapine Clozapine (HF 1854, LX 100-129) is an atypical antipsychotic drug by acting as a 5-HT antagonist, used in the treatment of schizophrenia.
Anticancer Res, 2021, 41(2):687-697
Ann Neurol, 2020, 10.1002/ana.25935
BMC Evol Biol, 2018, 18(1):89
S2493 Olanzapine Olanzapine (LY170053) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist.
Nat Protoc, 2021, 10.1038/s41596-021-00624-z
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00196-X
Pharmacol Res, 2021, 170:105714
S2644 Lerisetron Lerisetron (F 0930, F 0930RS) is a 5-HT3 receptor antagonist with IC50 of 0.81μM.
S2649 SB 200646 SB 200646 (SB 200646A) is a potent, selective and oral-active antagonist of 5-HT2B/2C over 5-HT2A receptor with 50 fold selectivity. The pKi for rat 5-HT2C receptor, rat 5-HT2B receptor and rat 5-HT2A receptor are 6.9, 7.5 and 5.2, respectively. SB 200646 has electrophysiological and anxiolytic properties in vivo.
S2663 WAY-100635 Maleate WAY-100635 Maleate is a potent and selective 5-HT receptor antagonist with IC50 of 0.95 nM.
Sci Rep, 2021, 11(1):9300
J Pain, 2019, 20(1):16.e1-16.e16
Neurochem Res, 2018, 43(7):1371-1382
S2669 LY310762 HCl LY310762 is a 5-HT1D receptor antagonist with Ki of 249 nM, having a weaker affinity for 5-HT1B receptor.
S2677 BRL-15572 Dihydrochloride BRL-15572 is a 5-HT1D receptor antagonist with pKi of 7.9, also shows a considerable affinity at 5-HT1A and 5-HT2B receptors, exhibiting 60-fold selectivity over 5-HT1B receptor.
Brain Behav Immun, 2018, 74:49-67
Anesth Analg, 2018, 10.1213/ANE.0000000000003757
Int Immunopharmacol, 2018, 56:168-178
S2698 RS-127445 RS-127445 (MT500) is a selective 5-HT2B receptor antagonist with pKi of 9.5 and pIC50 of 10.4, exhibits >1000-fold selectivity against other 5-HT receptors.
Lab Invest, 2021, 1-14
Int Immunopharmacol, 2019, 10.1016/j.intimp.2019.106036
Front Pharmacol, 2018, 9:587
S2849 SB269970 HCl SB269970 HCl is a hydrochloride salt form of SB-269970, which is a 5-HT7 receptor antagonist with pKi of 8.3, exhibits >50-fold selectivity against other receptors.
Cancers (Basel), 2021, 13(21)5305
J Neurotrauma, 2018, 10.1089/neu.2018.5652
Sci Rep, 2015, 5:8060
S2856 SB 271046 hydrochloride SB 271046 hydrochloride is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 8.9, exhibits 200-fold greater selectivity over other 5-HT receptor subtypes.
Sci Rep, 2018, 8(1):15753
S2865 VUF 10166 VUF10166 is a novel, potent and competitive antagonist for 5-HT3A receptor with Ki of 0.04 nM, its affinity at 5-HT3AB receptor is significantly lower.
S2894 SB742457 SB742457 (GSK 742457) is a highly selective 5-HT6 receptor antagonist with pKi of 9.63, exhibits >100-fold selectivity over other receptors. Phase 2.
Sci Rep, 2018, 8(1):15753
Sci Rep, 2017, 7(1):4983
S3050 Palonosetron HCl Palonosetron HCl (RS 25259, RS 25259 197) is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting.
S3054 Alverine Citrate Alverine citrate (NSC 35459) is a drug used for functional gastrointestinal disorders. Alverine citrate is a 5-HT1A receptor antagonist, with an IC50 of 101 nM.
Am J Physiol Lung Cell Mol Physiol, 2018, 315(2):L133-L148
S3706 Sarpogrelate hydrochloride Sarpogrelate (MCI-9042) is a selective 5-HT2A antagonist with pKi values of 8.52, 7.43 and 6.57 for 5-HT2A, 5-HT2C and 5-HT2B receptors respectively.
S3723 Ramosetron Hydrochloride Ramosetron Hydrochloride (YM-060) is the hydrochloride salt of ramosetron, a selective serotonin (5-HT) receptor antagonist with potential antiemetic activity.
Theranostics, 2020, 10(16):7351-7368
S3821 Nuciferine Nuciferine (Sanjoinine E, (-)-Nuciferine, VLT 049) is a major active aporphine alkaloid from the leaves of N. nucifera Gaertn and possesses anti-hyperlipidemia, anti-hypotensive, anti-arrhythmic, and insulin secretagogue activities. Nuciferine is an antagonist at 5-HT2A (IC50=478 nM), 5-HT2C (IC50=131 nM), and 5-HT2B (IC50=1 μM), an inverse agonist at 5-HT7 (IC50=150 nM), a partial agonist at D2 (EC50=64 nM), D5 (EC50=2.6 μM) and 5-HT6 (EC50=700 nM), an agonist at 5-HT1A (EC50=3.2 μM) and D4 (EC50=2 μM) receptor.
Br J Pharmacol, 2021, 178(5):1182-1199
Tohoku J Exp Med, 2021, 254(1):17-23
S4086 Loxapine Succinate Loxapine Succinate is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent.
Anticancer Res, 2021, 41(2):687-697
S4249 Flopropione Flopropione is a spasmolytic or antispasmodic agent, and acts as a 5-HT1A receptor antagonist.
Front Microbiol, 2020, 10:2936
S4283 Cyclobenzaprine HCl Cyclobenzaprine HCl is a muscle relaxant by blocking pain sensations, used for the treatment of muscle spasms; A 5-HT2 receptor antagonist.
S4358New Pimozide Pimozide (Orap, R6238) is an antagonist of Dopamine Receptors with Ki of 0.83 nM, 3.0 nM and 6600 nM for dopamine D3, D2 and D1 receptors, respectively. Pimozide also exhibits binding affinity at α2-adrenoceptor and 5-HT1A with Ki of 360 nM and 310 nM, respectively. Pimozide is an antipsychotic drug with anti-tumor activity and suppresses STAT3 and STAT5 activity.
Biol Pharm Bull, 2021, 10.1248/bpb.b21-00531
S4635 Cyproheptadine hydrochloride sesquihydrate Cyproheptadine hydrochloride (Periactin, Peritol) is non-selective 5HT2 antagonist with IC50 of 0.6 nM. Also a SETD7/9 inhibitor.
Anticancer Res, 2019, 39(7):3767-3775
S4694 Alosetron Hydrochloride Alosetron Hydrochloride (GR 68755C, GR 68755X, Lotronex) is the hydrochloride salt form of alosetron, a potent and selective 5-HT3 receptor antagonist.
Cell, 2017, 170(1):185-198
S4748 Ondansetron Hydrochloride Dihydrate Ondansetron is a highly specific and selective serotonin 5-HT3 receptor antagonist (Ki=6.16 nM), with low affinity for dopamine receptors.
S4889 Perospirone hydrochloride Perospirone (SM-9018) is an atypical or second-generation antipsychotic of the azapirone family that antagonizes serotonin 5HT2A receptors and dopamine D2 receptors. It also displays affinity towards 5HT1A receptors as a partial agonist.
S5052 Granisetron Granisetron (Sancuso, Kevatril, Granisetronum, Sustol) is a serotonin receptor (5HT-3 selective) antagonist that is used as an antiemetic and antinauseant for cancer chemotherapy.
S5060 Metadoxine Metadoxine (Metadoxil, Metasin, pyridoxine-pyrrolidone carboxylat), also known as pyridoxine-pyrrolidone carboxylate, is a drug used to treat chronic and acute alcohol intoxication. Metadoxine is a novel 5-HT2B receptor antagonist with a possible therapeutic role in treating ADHD.
S5185New Perospirone Perospirone (SM-9018 free base) is an orally active antagonist of 5-hydroxytryptamine2 (5-HT2) receptor, dopamine2 (D2) receptor and 5-HT1A receptor with Ki of 0.6 nM, 1.4 nM and 2.9 nM, respectively.
S5197New Loxapine Loxapine (Adasuve), a typical neuroleptic, is a drug with D2/D3 receptor antagonist activity and a higher affinity for D3 than D2. Loxapine displays an extremely strong binding affinity for dopamine D4 and serotonin 5-HT2 receptors.
S5326 Dolasetron Dolasetron is a highly specific and selective serotonin 5-HT3 receptor antagonist. It has minimal activity at other known serotonin receptors, and has low affinity for dopamine receptors.
S5398 Nefazodone hydrochloride Nefazodone hydrochloride (BMY-13754-1) is the hydrochloride salt form of nefazodone, which is an atypical antidepressant showing antagonistic activity on serotonin reuptake.
S5428 Promazine hydrochloride Promazine (Romtiazin, Sinophenin) is an antagonist at types 1, 2, and 4 dopamine receptors, 5-HT receptor types 2A and 2C, muscarinic receptors 1 through 5, alpha(1)-receptors, and histamine H1-receptors with antipsychotic effects.
S5472 Nafronyl oxalate salt Nafronyl oxalate salt is the oxalate salt form of nafronyl, which is a selective antagonist of 5-HT2 receptors and a vasodilator used in the management of peripheral and cerebral vascular disorders.
S5538 Tropisetron Tropisetron (ICS 205-930) is a 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor.
S5714 lurasidone Lurasidone (SM-13496) is a second-generation antipsychotic agent that exhibits full antagonism at dopamine D2 and serotonin 5-HT2A receptors with binding affinities Ki = 1 nM and Ki = 0.5 nM, respectively. It also has high affinity for serotonin 5-HT7 receptors (Ki = 0.5 nM), partial agonist activity at 5-HT1A receptors (Ki = 6.4 nM) and lacks affinity for histamine H1 and muscarinic M1 receptors.
S5740 Palonosetron Palonosetron (RS25259, RS 25259 197) is a 5-HT3 antagonist with Ki value of 0.17 nM. It is used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV).
S5749 Chlorpromazine Chlorpromazine (CPZ) is a low-potency typical antipsychotic agent that is used to treat psychotic disorders such as schizophrenia. Chlorpromazine (CPZ) inhibits 5-HT(2A) receptor and dopamine D2 in vitro. Chlorpromazine (CPZ) also inhibits sodium channel and blocks HERG potassium channels with IC50 of 21.6 μM.
Theranostics, 2021, 11(5):2364-2380
Front Oncol, 2021, 11:665832
Int J Nanomedicine, 2021, 16:2487-2499
S5770New Pizotifen Pizotifen (Pizotyline, BC-105) is a potent antagonist of 5-Hydroxytryptamine (5-HT, Serotonin) 5-HT2 receptor with a high affinity for 5-HT1C binding site.
S5857 Trazodone Trazodone (AF-1161) is a 5-HT 2A/2C receptor antagonist that is used as an antidepressant for treating major depressive disorder and anxiety disorders.
S5947 Amitriptyline Amitriptyline (MK-230, N-750, Ro41575) is a tricyclic antidepressant (TCA) with analgesic properties, widely used to treat depression and neuropathic pain. Amitriptyline is an inhibitor of both serotonin transporter (SERT) and norepinephrine transporter (NET) with Ki of 3.45 nM and 13.3 nM, respectively. Amitriptyline also inhibits histamine receptor H1, histamine receptor H4, 5-HT2 and sigma 1 receptor with Ki of 0.5 nM, 7.31 nM, 235 nM and 287 nM, respectively. This product is a waxy solid.
Cancers (Basel), 2019, 11(12)
S5949New Metoclopramide hydrochloride hydrate Metoclopramide hydrochloride (Clorpa, Gimoti, Maxolon, Reglan) hydrate is primarily a Dopamine receptor antagonist, with 5HT3 receptor antagonist and 5HT4 receptor agonist activity, and used as an antiemetic and gastroprokinetic.
Pharmazie, 2021, 76(4):172-174
S5965New Urapidil Urapidil is an antihypertensive drug acting as an α1 adrenoreceptor antagonist and a 5-HT1A agonist.
S7538 RS-102895 Hydrochloride RS-102895 hydrochloride (HCl) is a potent antagonist of Chemokine (C-C motif) receptor 2 (CCR2) with IC50 of 360 nM, and shows no effect on CCR1. RS-102895 hydrochloride also inhibits human α1a and α1d receptors, rat brain cortex 5-HT1a receptor in cells with IC50s of 130 nM, 320 nM, 470 nM, respectively.
S8010 PRX-08066 Maleic acid PRX-08066 Maleic acid is a selective 5-HT2B receptor antagonist with IC50 of 3.4 nM, prevents the severity of pulmonary arterial hypertension in the MCT rat model. Phase 2.
Clin Exp Metastasis, 2018, 35(3):123-134
S9174 Xanthotoxol Xanthotoxol (8-Hydroxypsoralen, 8-Hydroxypsoralene, 8-Hydroxyfuranocoumarin, Psoralen), a biologically active linear furocoumarin found in a large number of plants, shows strong pharmacological activities as anti-inflammatory, antioxidant, 5-HT antagonistic, and neuroprotective effects.
S0104 Pardoprunox (SLV-308) hydrochloride Pardoprunox hydrochloride (DU-126891, SME-308) is a potent but partial dopamine D2 receptor agonist with pEC50 of 8.0, and a partial agonist in the induction of [35S]GTPγS binding with pEC50 of 9.2 and a serotonin 5-HT1A receptor agonist, with pEC50 of 6.3, respectively.
S0476 SCH-23390 hydrochloride SCH-23390 hydrochloride (R-(+)-SCH-23390, SCH-23390) is a highly potent and selective dopamine D1-like receptor antagonist with Ki of 0.2 nM and 0.3 nM for the D1 and D5 dopamine receptor subtypes, respectively. SCH-23390 hydrochloride is a potent and high efficacy agonist at h5-HT2C receptors with Ki of 9.3 nM. SCH-23390 hydrochloride directly inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with IC50 of 268 nM.
S0496 PF-04995274 PF-04995274 (PF-4995274) is a potent, high-affinity, orally active and partial agonist of serotonin 4 receptor (5-HT4R) with EC50 of 0.47 nM, 0.36 nM, 0.37 nM and 0.26 nM for human 5-HT4A/4B/4D/4E, respectively. As for rat 5-HT4S/4L/4E, the EC50 is 0.59 nM, 0.65 nM and 0.62 nM, respectively. PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease.
S1385 Mosapride Citrate Mosapride Citrate (AS-4370) is a gastroprokinetic agent that acts as a selective 5HT4 agonist.
S1432 Sumatriptan Succinate Sumatriptan Succinate (GR 43175) is a triptan sulfa drug containing a sulfonamide group for the treatment of migraine headaches.
J Toxicol Sci, 2017, 42(6):755-761
S1436 Tianeptine sodium Tianeptine sodium is a selective serotonin reuptake enhancer (SSRE), used for treating major depressive episodes.
Transl Psychiatry, 2014, 4:e411
S1488 Naratriptan HCl Naratriptan HCl is a triptan agent that is used for the treatment of migraine headaches.
S1607 Rizatriptan Benzoate Rizatriptan Benzoate (MK-462) is an agonist at serotonin 5-HT1B and 5-HT1D receptors, used to treat acute migraine attacks.
S1649 Zolmitriptan Zolmitriptan is a novel and highly selective 5-HT(1B/1D) receptor agonist, used in the treatment of acute migraines.
Int J Pharm, 2019, 560:294-305
S1975 Aripiprazole Aripiprazole (OPC-14597) is a novel atypical antipsychotic drug that is reported to be a high-affinity 5-HT receptor partial agonist.
Elife, 2021, 10e72463
Antimicrob Agents Chemother, 2021, AAC.01146-20
Biochem Biophys Res Commun, 2021, 578:70-76
S2025 Urapidil HCl Urapidil HCl is a hydrochloride salt form of urapidil which is α1-adrenoceptor antagonist and 5-HT1A receptor agonist with pIC50 of 6.13 and 6.4 respectively.
S2096 Almotriptan Malate Almotriptan Malate (LAS 31416) is a selective 5-hydroxytryptamine1B/1D (5-HT1B/1D) receptor agonist, used for the treatment of Migraine attacks in adults.
Oncotarget, 2017, 9(3):3507-3518
Oncotarget, 2016, 7(9):9975-92
S2578 1-Phenylbiguanide 1-Phenylbiguanide (Phenylbiguanide, PBG, N-Phenylbiguanide) is a 5-hydroxytryptamine3 (5-HT3) receptor agonist with EC50 of 3.0 μM.
S2852 BRL-54443 BRL 54443 is a 5-HT1E and 5-HT1F receptor agonist with pKi of 8.7 and 9.25, respectively, with a weak binding affinity for 5-HT1A, 5-HT1B, 5-HT1D receptors.
Theranostics, 2021, 11(14):6950-6965
S2875 Prucalopride Prucalopride (R-93877) is a selective, high affinity 5-HT receptor agonist for 5-HT4A and 5-HT4B receptor with Ki of 2.5 nM and 8 nM, respectively, exhibits >290-fold selectivity against other 5-HT receptor subtypes.
Front Pharmacol, 2019, 10:1491
Gut, 2019, 68(8):1406-1416
Nutrients, 2017, 9(12)
S3180 Eletriptan HBr Eletriptan (UK-116044) is a selective 5-HT1B and 5-HT1D receptor agonist with Ki of 0.92 nM and 3.14 nM, respectively.
S3510New NLX-101 NLX-101 (F-15599) is a highly selective 5-HT1A receptor biased agonist that mediates antidepressant-like activity in rats via prefrontal cortex 5-HT 1A receptors.
S4244 Serotonin HCl Serotonin HCl (5-HT) is a monoamine neurotransmitter and Endogenous 5-HT receptor agonist.
Theranostics, 2021, 11(14):6950-6965
Sci Rep, 2021, 11(1):1250
Eur J Pharmacol, 2021, 908:174355
S4247 Prucalopride Succinate Prucalopride is a selective, high affinity 5-HT4 receptor agonist. The Ki values of prucalopride for human 5-HT(4a) and 5-HT(4b) receptor are 2.5 nM and 8 nM, respectively.
Front Pharmacol, 2019, 10:1491
Front Pharmacol, 2018, 9:171
Neurogastroenterol Motil, 2018, 30(2)
S4256 Buspirone HCl Buspirone is a serotonergic (5HT(1A) receptor agonist) anxiolytic drug with some D(2) dopaminergic effect, used for anxiety disorders.
Food Chem Toxicol, 2020, 30;141:111394
S4259 Vilazodone HCl Vilazodone HCl is a selective serotonin reuptake inhibitor (SSRI) and a partial agonist of 5-HT1A receptors, used for the treatment of major depressive disorder.
J Pain, 2019, 20(1):16.e1-16.e16
Acta Pol Pharm, 2017, 74(3):765-775
S4639 Brexpiprazole Brexpiprazole (OPC-34712) is a novel D2 dopamine and serotonin 1A partial agonist, called serotonin-dopamine activity modulator (SDAM), and a potent antagonist of serotonin 2A receptors, noradrenergic alpha 1B and 2C receptors with Ki values of 0.3, 0.12, 0.47, 0.17 and 0.59 nM for D2L, 5-HT1A, 5-HT2A, α1B receptors and α2C receptors respectivey.
S4751 Cisapride hydrate Cisapride (Propulsid, Alimix, Propulsin, Enteropride, Kinestase) acts directly as a selective serotonin 5-HT4 receptor agonist with IC50 of 0.483 μM. And It also acts indirectly as a parasympathomimetic.
Elife, 2021, 10e68714
S4839 Mosapride Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist.
S5064New Lasmiditan Lasmiditan (Reyvow) is a highly selective 5-hydroxytryptamine (serotonin) receptor 1F (5-HT1F) agonist that can be used as a promising acute anti-migraine therapy.
S5153 Tetrahydroberberine Tetrahydroberberine (Canadine) is an isoquinoline alkaloid with micromolar affinity for dopamine D2 (antagonist, pKi = 6.08) and 5-HT1A (agonist, pKi = 5.38) receptors but moderate to no affinity for other relevant serotonin receptors.
S5253 Cisapride (R 51619) Cisapride (R 51619, Kaudalit, Kinestase, Prepulsid, Presid, Pridesia, Propulsid) is a nonselective 5-HT4 receptor agonist with gastroprokinetic effects.
S5401 Tegaserod Maleate Tegaserod Maleate is a hydrogen maleate salt form of tegaserod, which is a 5-HT4 receptor partial agonist and binds with high affinity to 5-HT4 receptors. It has limited affinity for 5-HT1 receptors and no appreciable affinity for other 5-HT receptors, muscarinic, adrenergic, dopaminergic or opiate receptors.
Front Oncol, 2021, 11:683241
S5741 Quetiapine Quetiapine is an atypical antipsychotic used for the treatment of schizophrenia, bipolar disorder, and major depressive disorder.Quetiapine is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine have moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.23, 5.74, 7.54, 5.55.
S5848 Frovatriptan Succinate Frovatriptan Succinate is the succinate salt form of frovatriptan, a synthetic triptan with serotonin (5-HT) receptor agonist activity especially for the 5-HT1B/1D receptors.
S6324 5-Methoxytryptamine 5-Methoxytryptamine (Mexamine, Methoxytryptamine) is a tryptamine derivative that acts as a full agonist at the 5-HT1, 5-HT2, 5-HT4, 5-HT6, and 5-HT7 receptors.
S6489 Lasmiditan succinate Lasmiditan succinate (COL-144, LY573144) is a novel, centrally acting, highly selective 5-HT(1F) receptor agonist (Ki=2.21 nM) without vasoconstrictor activity.
S8447 8-OH-DPAT (8-Hydroxy-DPAT) 8-OH-DPAT (8-Hydroxy-DPAT) is a kind of classic 5-HT1A agonist with the pIC50 of 8.19. It has a selectivity of almost-1000 fold for a subtype of the 5-HT1 binding site; Its biological half-life is 1.5 hous.
S3716 Flibanserin Flibanserin (BIMT-17, BIMT-17-BS) is a nonhormonal, centrally acting molecule that acts as an agonist at postsynaptic 5-HT1A receptors and as an antagonist at 5-HT2A receptors.
Nat Commun, 2021, 12(1):5919
S5506 Vortioxetine Vortioxetine, a novel antidepressant for the treatment of major depressive disorder, is a 5-HT3, 5-HT7 and 5-HT1D receptor antagonist, 5-HT1B receptor partial agonist, 5-HT1A receptor agonist and serotonin (5-HT) transporter (SERT) inhibitor.
S5843 Cinitapride Hydrogen Tartrate Cinitapride Hydrogen Tartrate is a gastroprokinetic agent that acts as an agonist of the 5-HT1 and 5-HT4 receptors and as an antagonist of the 5-HT2 receptors
S5858 Vilazodone Vilazodone (EMD-68843, SB-659746A) is a novel antidepressant having a selective serotonin (5-HT) reuptake inhibitory and 5-HT1A receptor partial agonist activity. The affinity of vilazodone is much higher in the 5-HT reuptake site (Ki=0.1 nM) than in norepinephrine (Ki=56 nM) and dopamine (Ki=37 nM) sites.
J Pain, 2019, 20(1):16.e1-16.e16
S8021 Vortioxetine (Lu AA21004) HBr Vortioxetine (Lu AA21004), a multimodal serotonergic agent, is an antagonist of human (h) serotonin (5-HT)3A receptor and h5-HT7 receptor with Ki of 3.7 nM and 19 nM, respectively. Vortioxetine (Lu AA21004) is also a h5-HT1B receptor partial agonist with Ki of 33 nM and h5-HT1A receptor agonist with Ki of 15 nM, and a human 5-HT transporter (SERT) inhibitor with Ki of 1.6 nM.
S0222 Lvguidingan Lvguidingan (Anticonvulsant 7903, 3,4-dichlorophenyl propenylisobutylamide) is an anticonvulsant/antiepileptic agent. Lvguidingan (Anticonvulsant 7903) is found to be able to increase the concentration of 5-HT and 5-HIAA in mice brain.
S3196 Azacyclonol Azacyclonol (MER 17, MDL 4829), also known as γ-pipradol, is a drug used to diminish hallucinations in psychotic individuals.
Oncol Rep, 2020, 44(6):2503-2516
S1333 Fluoxetine (Lilly 110140) HCl Fluoxetine HCl (Lilly110140) is a selective serotonin-reuptake inhibitor (SSRI) at the neuronal membrane, used in the treatment of depression.
FASEB J, 2021, 35(5):e21581
Sci Rep, 2021, 11(1):1250
Endocrine, 2021, 10.1007/s12020-021-02818-7
S1483 Iloperidone Iloperidone (HP873) is a dopamine (D2)/serotonin (5-HT2) receptor antagonist, used for the treatment of schizophrenia.
Anticancer Res, 2021, 41(2):687-697
Sci Rep, 2018, 8(1):15753
S1642 Methyldopa Methyldopa (Aldomet) is a DOPA decarboxylase competitive inhibitor with an ED50 of 21.8 mg/kg.
S1869 Dapoxetine HCl Dapoxetine HCl (LY-210448) is a short-acting novel selective serotonin reuptake inhibitor, used for the treatment of premature ejaculation.
S2084 Duloxetine HCl Duloxetine HCl (LY-248686) is a serotonin-norepinephrine reuptake inhibitor with Ki of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD).
Drug Metab Dispos, 2015, 44(3):378-88
J Pharmacol Exp Ther, 2014, 349(3):402-7
Am J Physiol Renal Physiol, 2013, 305(12):F1663-8
S2464 Sevoflurane Sevoflurane (Fluoromethyl) is a noncompetitive inhibitor of 5-HT3 receptor. Sevoflurane acts as a low-soluble inhalation anesthetics.
ACS Chem Neurosci, 2021, 10.1021/acschemneuro.1c00131
S2582 Trazodone HCl Trazodone HCl (AF-1161, KB-831) is an antidepressant belonging to the class of serotonin receptor antagonists and reuptake inhibitors for treatment of anxiety disorders.
S3024 Lamotrigine Lamotrigine (BW-430C) is a novel anticonvulsant drug for inhibition of 5-HT with IC50 of 240 μM and 474 μM in human platelets and rat brain synaptosomes, and also is a sodium channel blocker.
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 34(6):1911-1918
Hum Cell, 2021, 10.1007/s13577-021-00579-z
S3175 Atomoxetine HCl Atomoxetine (LY 139603) is a selective norepinephrine (NE) transporter inhibitor with Ki of 5 nM, with 15- and 290-fold lower affinity for human 5-HT and DA transporters.
S3183 Amitriptyline HCl Amitriptyline HCl is an inhibitor of both serotonin transporter (SERT) and norepinephrine transporter (NET) with Ki of 3.45 nM and 13.3 nM, respectively. Amitriptyline HCl also inhibits histamine receptor H1, histamine receptor H4, 5-HT2 and sigma 1 receptor with Ki of 0.5 nM, 7.31 nM, 235 nM and 287 nM, respectively. Amitriptyline is a tricyclic antidepressant (TCA).
Environ Toxicol Chem, 2021, 10.1002/etc.5018
PLoS Pathog, 2020, 16;16(3):e1008341
Sci Rep, 2018, 8(1):15753
S3817 Harmine hydrochloride Harmine (Telepathine), a fluorescent harmala alkaloid belonging to the beta-carboline family of compounds, is a highly cell-permeant and competitive inhibitor of ATP binding to the kinase pocket of DYRK1A, with about 60-fold higher IC50 value for DYRK2. Harmine also inhibits monoamine oxidases (MAOs) and cdc-like kinases (CLKs). Harmine inhibits 5-HT2A serotonin receptor with Ki of 397 nM.
S3913New Pimethixene maleate Pimethixene (Pimetixene) maleate, an antihistamine, anntimigraine agent and antiserotonergic compound, is a highly potent antagonist of a broad range of monoamine receptors, including a variety of serotonin receptors. Pimethixene maleate inhibits 5-HT2A, 5-HT2B, 5-HT2C, 5-HT1A, 5-HT1B, 5-HT6, 5-HT7, Adrenergic α-1A, Dopamine D1 Receptor, Dopamine D2 Receptor, Dopamine D4.4 Receptor, Histamine H1 Receptor, Muscarinic M1 and Muscarinic M2 with pKi of 10.22, 10.44, 8.42, 7.63, < 5, 7.30, 7.28, 7.61, 6.37, 8.19, 7.54, 10.14, 8.61 and 9.38, respectively.
S4053 Sertraline HCl Sertraline HCl (CP-51974-1) is a 5-HT antagonist with Ki of 13 nM.
Antimicrob Agents Chemother, 2021, AAC.01146-20
Sci Rep, 2021, 11(1):1250
J Glob Antimicrob Resist, 2021, 27:167-171
S4064 Escitalopram Oxalate Escitalopram Oxalate is a selective serotonin (5-HT) reuptake inhibitor (SSRI) with Ki of 0.89 nM.
S4377 Imipramine HCl Imipramine (Melipramine) is a tricyclic antidepressant (TCA) of the dibenzazepine group, mainly used in the treatment of major depression and enuresis (inability to control urination).
Antioxidants (Basel), 2021, 10(6)956
S4749 Citalopram HBr Citalopram HBr (Nitalapram HBr, Prepram HBr, Bonitrile HBr, Lu 10-171 HBr), an antidepressant, is an orally administered selective serotonin reuptake inhibitor (SSRI) with IC50 of 1.8 nM.
Aging (Albany NY), 2021, 13(11):14729-14744
Sci Rep, 2021, 11(1):1250
Viruses, 2021, 13(8)1533
S5071 Duloxetine Duloxetine (LY-248686) is a potent inhibitor of serotonin (5-hydroxytryptamine, 5-HT) and noradrenaline (NE) uptake in vitro and in vivo and is 3- to 5-times more effective at inhibiting 5-HT uptake.
S5485 Desipramine Hydrochloride Desipramine hydrochloride (Desmethylimipramine, Norimipramine, EX-4355, G-35020, JB-8181, NSC-114901) is a dibenzazepine-derivative tricyclic antidepressant that acts as a selective norepinephrine reuptake inhibitor. It also shows weak serotonin reuptake inhibitory, α1-blocking, antihistamine, and anticholinergic effects.
S5563 Thioridazine hydrochloride Thioridazine (Aldazine, Mellaril) is a potent antianxiety and antipsychotic agent.
Cell Syst, 2019, 8(2):97-108
S8183 Pimavanserin Pimavanserin (ACP-103) is a potent and selective serotonin 5-HT2A inverse agonist with pIC50 of 8.73, used to treat psychosis associated with Parkinson’s disease.
Br J Pharmacol, 2021, 10.1111/bph.15756
Mol Ther Oncolytics, 2020, 19:19-32
ACS Chem Neurosci, 2020, 11(2):173-183
S9039 Albiflorin Albiflorin, a natural product isolated from Paeoniae Radix, is a novel 5-HT and NE reuptake inhibitor with high selectivity.
S9239 Isocorynoxeine Isocorynoxeine (7-Isocorynoxeine), a major alkaloid found in Uncaria rhynchophylla, exhibits wide beneficial effects on the cardiovascular and cardiocerebral vascular systems. Isocorynoxeine suppress 5-HT2A receptor-mediated current response with IC50 of 72.4 μM.
S9258 (+)-Isocorynoline Isocorynoxeine, a major bioactive tetracyclic oxindole alkaloids found in Uncaria rhynchophylla, exhibits a dose-dependent inhibition of 5-HT2A receptor-mediated current response with an IC50 of 72.4 μM and shows various beneficial effects, including lowering blood pressure, vasodilatation, and protection against ischemia-induced neuronal damage.
S9510 Protriptyline hydrochloride Protriptyline Hydrochloride is the hydrochloride salt form of protriptyline. Protriptyline is a tricyclic secondary amine with antidepressant property which acts by inhibition of serotonin and norepinephrine reuptake.
S4740 Sodium ferulate Sodium ferulate (SF, Ferulic acid sodium salt), the sodium salt of ferulic acid, is a drug used in traditional Chinese medicine for treatment of cardiovascular and cerebrovascular diseases and to prevent thrombosis.
S0313 Volinanserin Volinanserin (Volinanserin Hydrochloride Salt, MDL100907, M 100907, MDL-100,907) is a highly selective and potent 5-HT2 receptor antagonist with Ki of 0.36 nM. Volinanserin shows antipsychotic activity.
S0779 Pirenperone Pirenperone (R-47456, R-50656), a quinazoline derivative, is a selective antagonist of SR-2A (5-HT2 serotonin receptor) when employed in low doses. Pirenperone behaves like a typical neuroleptic when used in higher doses (greater than 0.1 mg/kg).
S1243 Agomelatine (S20098) Agomelatine (S20098) is classified as a norepinephrine-dopamine disinhibitor (NDDI) due to its antagonism of the 5-HT2C receptor.
Sci Rep, 2018, 8(1):15753
Neuropsychiatry (London), 2018, None
Arch Oral Biol, 2017, 82:11-18
S1245 Latrepirdine 2HCl Latrepirdine is an orally active,and neuroactive antagonist of multiple drug targets, including histamine receptors, GluR, and 5-HT receptors, used as an antihistamine drug.
S1283 Asenapine maleate Asenapine maleate (Org 5222) is a high-affinity antagonist of serotonin, norepinephrine, dopamine and histamine receptors, used for the treatment of schizophrenia and acute mania associated with bipolar disorder.
Biochem Biophys Res Commun, 2021, 553:172-179
Anticancer Res, 2021, 41(2):687-697
Sci Rep, 2018, 8(1):15753
S1345 Granisetron HCl Granisetron is a serotonin 5-HT3 receptor antagonist,used to treat chemotherapy-induced nausea and vomiting.
S1390 Ondansetron HCl Ondansetron HCl (GR 38032F) is a serotonin 5-HT3 receptor antagonist, used to prevent nausea and vomiting caused by cancer chemotherapy, and radiation therapy.
Immunity, 2019, 50(5):1163-1171
Int J Urol, 2016, 23(11):946-951
S1394 Pizotifen Malate Pizotifen Malate (BC-105) is a benzocycloheptane based agent used for recurrent migraine headaches.
S1444 Ziprasidone HCl Ziprasidone HCl (CP-88059) is a novel and potent dopamine and serotonin (5-HT) receptor antagonist, used in the treatment of schizophrenia and bipolar disorder.
Anticancer Res, 2021, 41(2):687-697
Molecules, 2020, 25(18)E4206
Nature, 2018, 560(7718):372-376
S1615 Risperidone Risperidone (R-64766) is a mutil-targeted antagonist for dopamine, serotonin, adrenergic and histamine receptors, used to treat schizophrenia and bipolar disorder.
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00196-X
Anticancer Res, 2021, 41(2):687-697
BMC Evol Biol, 2018, 18(1):89
S1898 Tropisetron HCl Tropisetron HCl (ICS 205-930) is a potent and selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist, used to treat nausea and vomiting following chemotherapy.
S1996 Ondansetron Ondansetron (GR 38032F, GR-C507/75) is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic.
Int J Urol, 2016, 23(11):946-951
S2016 Mirtazapine Mirtazapine (Org3770) is an adrenergic and seroton receptor antagonist, used to treat depression.
S2106 Azasetron HCl Azasetron HCl (Y-25130) is a selective 5-HT3 receptor antagonist with IC50 of 0.33 nM used in the management of nausea and vomiting induced by cancer chemotherapy.
S2112 Blonanserin Blonanserin (AD 5423) is a relatively selective serotonin (5-HT)2A and dopamine D2 antagonist, used the treatment of schizophrenia.
Sci Rep, 2018, 8(1):15753
S2232 Ketanserin Ketanserin (R41468) is a specific 5-HT2A serotonin receptor antagonist with Ki of 2.5 nM for rat and human 5-HT2A, used as an antihypertensive drug.
Lab Invest, 2021, 1-14
Int Immunopharmacol, 2019, 10.1016/j.intimp.2019.106036
Sci Rep, 2018, 8(1):15753
S2346 Puerarin Puerarin (Kakonein), an isoflavones found in the root of Radix puerariae, is a 5-HT2C receptor and benzodiazepine site antagonist.
Biochim Biophys Acta Mol Cell Res, 2022, S0167-4889(21)00262-7
Front Pharmacol, 2021, 12:632825
Int J Mol Sci, 2020, 21(14):5025
S2459 Clozapine Clozapine (HF 1854, LX 100-129) is an atypical antipsychotic drug by acting as a 5-HT antagonist, used in the treatment of schizophrenia.
Anticancer Res, 2021, 41(2):687-697
Ann Neurol, 2020, 10.1002/ana.25935
BMC Evol Biol, 2018, 18(1):89
S2493 Olanzapine Olanzapine (LY170053) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist.
Nat Protoc, 2021, 10.1038/s41596-021-00624-z
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00196-X
Pharmacol Res, 2021, 170:105714
S2644 Lerisetron Lerisetron (F 0930, F 0930RS) is a 5-HT3 receptor antagonist with IC50 of 0.81μM.
S2649 SB 200646 SB 200646 (SB 200646A) is a potent, selective and oral-active antagonist of 5-HT2B/2C over 5-HT2A receptor with 50 fold selectivity. The pKi for rat 5-HT2C receptor, rat 5-HT2B receptor and rat 5-HT2A receptor are 6.9, 7.5 and 5.2, respectively. SB 200646 has electrophysiological and anxiolytic properties in vivo.
S2663 WAY-100635 Maleate WAY-100635 Maleate is a potent and selective 5-HT receptor antagonist with IC50 of 0.95 nM.
Sci Rep, 2021, 11(1):9300
J Pain, 2019, 20(1):16.e1-16.e16
Neurochem Res, 2018, 43(7):1371-1382
S2669 LY310762 HCl LY310762 is a 5-HT1D receptor antagonist with Ki of 249 nM, having a weaker affinity for 5-HT1B receptor.
S2677 BRL-15572 Dihydrochloride BRL-15572 is a 5-HT1D receptor antagonist with pKi of 7.9, also shows a considerable affinity at 5-HT1A and 5-HT2B receptors, exhibiting 60-fold selectivity over 5-HT1B receptor.
Brain Behav Immun, 2018, 74:49-67
Anesth Analg, 2018, 10.1213/ANE.0000000000003757
Int Immunopharmacol, 2018, 56:168-178
S2698 RS-127445 RS-127445 (MT500) is a selective 5-HT2B receptor antagonist with pKi of 9.5 and pIC50 of 10.4, exhibits >1000-fold selectivity against other 5-HT receptors.
Lab Invest, 2021, 1-14
Int Immunopharmacol, 2019, 10.1016/j.intimp.2019.106036
Front Pharmacol, 2018, 9:587
S2849 SB269970 HCl SB269970 HCl is a hydrochloride salt form of SB-269970, which is a 5-HT7 receptor antagonist with pKi of 8.3, exhibits >50-fold selectivity against other receptors.
Cancers (Basel), 2021, 13(21)5305
J Neurotrauma, 2018, 10.1089/neu.2018.5652
Sci Rep, 2015, 5:8060
S2856 SB 271046 hydrochloride SB 271046 hydrochloride is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 8.9, exhibits 200-fold greater selectivity over other 5-HT receptor subtypes.
Sci Rep, 2018, 8(1):15753
S2865 VUF 10166 VUF10166 is a novel, potent and competitive antagonist for 5-HT3A receptor with Ki of 0.04 nM, its affinity at 5-HT3AB receptor is significantly lower.
S2894 SB742457 SB742457 (GSK 742457) is a highly selective 5-HT6 receptor antagonist with pKi of 9.63, exhibits >100-fold selectivity over other receptors. Phase 2.
Sci Rep, 2018, 8(1):15753
Sci Rep, 2017, 7(1):4983
S3050 Palonosetron HCl Palonosetron HCl (RS 25259, RS 25259 197) is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting.
S3054 Alverine Citrate Alverine citrate (NSC 35459) is a drug used for functional gastrointestinal disorders. Alverine citrate is a 5-HT1A receptor antagonist, with an IC50 of 101 nM.
Am J Physiol Lung Cell Mol Physiol, 2018, 315(2):L133-L148
S3706 Sarpogrelate hydrochloride Sarpogrelate (MCI-9042) is a selective 5-HT2A antagonist with pKi values of 8.52, 7.43 and 6.57 for 5-HT2A, 5-HT2C and 5-HT2B receptors respectively.
S3723 Ramosetron Hydrochloride Ramosetron Hydrochloride (YM-060) is the hydrochloride salt of ramosetron, a selective serotonin (5-HT) receptor antagonist with potential antiemetic activity.
Theranostics, 2020, 10(16):7351-7368
S3821 Nuciferine Nuciferine (Sanjoinine E, (-)-Nuciferine, VLT 049) is a major active aporphine alkaloid from the leaves of N. nucifera Gaertn and possesses anti-hyperlipidemia, anti-hypotensive, anti-arrhythmic, and insulin secretagogue activities. Nuciferine is an antagonist at 5-HT2A (IC50=478 nM), 5-HT2C (IC50=131 nM), and 5-HT2B (IC50=1 μM), an inverse agonist at 5-HT7 (IC50=150 nM), a partial agonist at D2 (EC50=64 nM), D5 (EC50=2.6 μM) and 5-HT6 (EC50=700 nM), an agonist at 5-HT1A (EC50=3.2 μM) and D4 (EC50=2 μM) receptor.
Br J Pharmacol, 2021, 178(5):1182-1199
Tohoku J Exp Med, 2021, 254(1):17-23
S4086 Loxapine Succinate Loxapine Succinate is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent.
Anticancer Res, 2021, 41(2):687-697
S4249 Flopropione Flopropione is a spasmolytic or antispasmodic agent, and acts as a 5-HT1A receptor antagonist.
Front Microbiol, 2020, 10:2936
S4283 Cyclobenzaprine HCl Cyclobenzaprine HCl is a muscle relaxant by blocking pain sensations, used for the treatment of muscle spasms; A 5-HT2 receptor antagonist.
S4358New Pimozide Pimozide (Orap, R6238) is an antagonist of Dopamine Receptors with Ki of 0.83 nM, 3.0 nM and 6600 nM for dopamine D3, D2 and D1 receptors, respectively. Pimozide also exhibits binding affinity at α2-adrenoceptor and 5-HT1A with Ki of 360 nM and 310 nM, respectively. Pimozide is an antipsychotic drug with anti-tumor activity and suppresses STAT3 and STAT5 activity.
Biol Pharm Bull, 2021, 10.1248/bpb.b21-00531
S4635 Cyproheptadine hydrochloride sesquihydrate Cyproheptadine hydrochloride (Periactin, Peritol) is non-selective 5HT2 antagonist with IC50 of 0.6 nM. Also a SETD7/9 inhibitor.
Anticancer Res, 2019, 39(7):3767-3775
S4694 Alosetron Hydrochloride Alosetron Hydrochloride (GR 68755C, GR 68755X, Lotronex) is the hydrochloride salt form of alosetron, a potent and selective 5-HT3 receptor antagonist.
Cell, 2017, 170(1):185-198
S4748 Ondansetron Hydrochloride Dihydrate Ondansetron is a highly specific and selective serotonin 5-HT3 receptor antagonist (Ki=6.16 nM), with low affinity for dopamine receptors.
S4889 Perospirone hydrochloride Perospirone (SM-9018) is an atypical or second-generation antipsychotic of the azapirone family that antagonizes serotonin 5HT2A receptors and dopamine D2 receptors. It also displays affinity towards 5HT1A receptors as a partial agonist.
S5052 Granisetron Granisetron (Sancuso, Kevatril, Granisetronum, Sustol) is a serotonin receptor (5HT-3 selective) antagonist that is used as an antiemetic and antinauseant for cancer chemotherapy.
S5060 Metadoxine Metadoxine (Metadoxil, Metasin, pyridoxine-pyrrolidone carboxylat), also known as pyridoxine-pyrrolidone carboxylate, is a drug used to treat chronic and acute alcohol intoxication. Metadoxine is a novel 5-HT2B receptor antagonist with a possible therapeutic role in treating ADHD.
S5185New Perospirone Perospirone (SM-9018 free base) is an orally active antagonist of 5-hydroxytryptamine2 (5-HT2) receptor, dopamine2 (D2) receptor and 5-HT1A receptor with Ki of 0.6 nM, 1.4 nM and 2.9 nM, respectively.
S5197New Loxapine Loxapine (Adasuve), a typical neuroleptic, is a drug with D2/D3 receptor antagonist activity and a higher affinity for D3 than D2. Loxapine displays an extremely strong binding affinity for dopamine D4 and serotonin 5-HT2 receptors.
S5326 Dolasetron Dolasetron is a highly specific and selective serotonin 5-HT3 receptor antagonist. It has minimal activity at other known serotonin receptors, and has low affinity for dopamine receptors.
S5398 Nefazodone hydrochloride Nefazodone hydrochloride (BMY-13754-1) is the hydrochloride salt form of nefazodone, which is an atypical antidepressant showing antagonistic activity on serotonin reuptake.
S5428 Promazine hydrochloride Promazine (Romtiazin, Sinophenin) is an antagonist at types 1, 2, and 4 dopamine receptors, 5-HT receptor types 2A and 2C, muscarinic receptors 1 through 5, alpha(1)-receptors, and histamine H1-receptors with antipsychotic effects.
S5472 Nafronyl oxalate salt Nafronyl oxalate salt is the oxalate salt form of nafronyl, which is a selective antagonist of 5-HT2 receptors and a vasodilator used in the management of peripheral and cerebral vascular disorders.
S5538 Tropisetron Tropisetron (ICS 205-930) is a 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor.
S5714 lurasidone Lurasidone (SM-13496) is a second-generation antipsychotic agent that exhibits full antagonism at dopamine D2 and serotonin 5-HT2A receptors with binding affinities Ki = 1 nM and Ki = 0.5 nM, respectively. It also has high affinity for serotonin 5-HT7 receptors (Ki = 0.5 nM), partial agonist activity at 5-HT1A receptors (Ki = 6.4 nM) and lacks affinity for histamine H1 and muscarinic M1 receptors.
S5740 Palonosetron Palonosetron (RS25259, RS 25259 197) is a 5-HT3 antagonist with Ki value of 0.17 nM. It is used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV).
S5749 Chlorpromazine Chlorpromazine (CPZ) is a low-potency typical antipsychotic agent that is used to treat psychotic disorders such as schizophrenia. Chlorpromazine (CPZ) inhibits 5-HT(2A) receptor and dopamine D2 in vitro. Chlorpromazine (CPZ) also inhibits sodium channel and blocks HERG potassium channels with IC50 of 21.6 μM.
Theranostics, 2021, 11(5):2364-2380
Front Oncol, 2021, 11:665832
Int J Nanomedicine, 2021, 16:2487-2499
S5770New Pizotifen Pizotifen (Pizotyline, BC-105) is a potent antagonist of 5-Hydroxytryptamine (5-HT, Serotonin) 5-HT2 receptor with a high affinity for 5-HT1C binding site.
S5857 Trazodone Trazodone (AF-1161) is a 5-HT 2A/2C receptor antagonist that is used as an antidepressant for treating major depressive disorder and anxiety disorders.
S5947 Amitriptyline Amitriptyline (MK-230, N-750, Ro41575) is a tricyclic antidepressant (TCA) with analgesic properties, widely used to treat depression and neuropathic pain. Amitriptyline is an inhibitor of both serotonin transporter (SERT) and norepinephrine transporter (NET) with Ki of 3.45 nM and 13.3 nM, respectively. Amitriptyline also inhibits histamine receptor H1, histamine receptor H4, 5-HT2 and sigma 1 receptor with Ki of 0.5 nM, 7.31 nM, 235 nM and 287 nM, respectively. This product is a waxy solid.
Cancers (Basel), 2019, 11(12)
S5949New Metoclopramide hydrochloride hydrate Metoclopramide hydrochloride (Clorpa, Gimoti, Maxolon, Reglan) hydrate is primarily a Dopamine receptor antagonist, with 5HT3 receptor antagonist and 5HT4 receptor agonist activity, and used as an antiemetic and gastroprokinetic.
Pharmazie, 2021, 76(4):172-174
S5965New Urapidil Urapidil is an antihypertensive drug acting as an α1 adrenoreceptor antagonist and a 5-HT1A agonist.
S7538 RS-102895 Hydrochloride RS-102895 hydrochloride (HCl) is a potent antagonist of Chemokine (C-C motif) receptor 2 (CCR2) with IC50 of 360 nM, and shows no effect on CCR1. RS-102895 hydrochloride also inhibits human α1a and α1d receptors, rat brain cortex 5-HT1a receptor in cells with IC50s of 130 nM, 320 nM, 470 nM, respectively.
S8010 PRX-08066 Maleic acid PRX-08066 Maleic acid is a selective 5-HT2B receptor antagonist with IC50 of 3.4 nM, prevents the severity of pulmonary arterial hypertension in the MCT rat model. Phase 2.
Clin Exp Metastasis, 2018, 35(3):123-134
S9174 Xanthotoxol Xanthotoxol (8-Hydroxypsoralen, 8-Hydroxypsoralene, 8-Hydroxyfuranocoumarin, Psoralen), a biologically active linear furocoumarin found in a large number of plants, shows strong pharmacological activities as anti-inflammatory, antioxidant, 5-HT antagonistic, and neuroprotective effects.
S0104 Pardoprunox (SLV-308) hydrochloride Pardoprunox hydrochloride (DU-126891, SME-308) is a potent but partial dopamine D2 receptor agonist with pEC50 of 8.0, and a partial agonist in the induction of [35S]GTPγS binding with pEC50 of 9.2 and a serotonin 5-HT1A receptor agonist, with pEC50 of 6.3, respectively.
S0476 SCH-23390 hydrochloride SCH-23390 hydrochloride (R-(+)-SCH-23390, SCH-23390) is a highly potent and selective dopamine D1-like receptor antagonist with Ki of 0.2 nM and 0.3 nM for the D1 and D5 dopamine receptor subtypes, respectively. SCH-23390 hydrochloride is a potent and high efficacy agonist at h5-HT2C receptors with Ki of 9.3 nM. SCH-23390 hydrochloride directly inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with IC50 of 268 nM.
S0496 PF-04995274 PF-04995274 (PF-4995274) is a potent, high-affinity, orally active and partial agonist of serotonin 4 receptor (5-HT4R) with EC50 of 0.47 nM, 0.36 nM, 0.37 nM and 0.26 nM for human 5-HT4A/4B/4D/4E, respectively. As for rat 5-HT4S/4L/4E, the EC50 is 0.59 nM, 0.65 nM and 0.62 nM, respectively. PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease.
S1385 Mosapride Citrate Mosapride Citrate (AS-4370) is a gastroprokinetic agent that acts as a selective 5HT4 agonist.
S1432 Sumatriptan Succinate Sumatriptan Succinate (GR 43175) is a triptan sulfa drug containing a sulfonamide group for the treatment of migraine headaches.
J Toxicol Sci, 2017, 42(6):755-761
S1436 Tianeptine sodium Tianeptine sodium is a selective serotonin reuptake enhancer (SSRE), used for treating major depressive episodes.
Transl Psychiatry, 2014, 4:e411
S1488 Naratriptan HCl Naratriptan HCl is a triptan agent that is used for the treatment of migraine headaches.
S1607 Rizatriptan Benzoate Rizatriptan Benzoate (MK-462) is an agonist at serotonin 5-HT1B and 5-HT1D receptors, used to treat acute migraine attacks.
S1649 Zolmitriptan Zolmitriptan is a novel and highly selective 5-HT(1B/1D) receptor agonist, used in the treatment of acute migraines.
Int J Pharm, 2019, 560:294-305
S1975 Aripiprazole Aripiprazole (OPC-14597) is a novel atypical antipsychotic drug that is reported to be a high-affinity 5-HT receptor partial agonist.
Elife, 2021, 10e72463
Antimicrob Agents Chemother, 2021, AAC.01146-20
Biochem Biophys Res Commun, 2021, 578:70-76
S2025 Urapidil HCl Urapidil HCl is a hydrochloride salt form of urapidil which is α1-adrenoceptor antagonist and 5-HT1A receptor agonist with pIC50 of 6.13 and 6.4 respectively.
S2096 Almotriptan Malate Almotriptan Malate (LAS 31416) is a selective 5-hydroxytryptamine1B/1D (5-HT1B/1D) receptor agonist, used for the treatment of Migraine attacks in adults.
Oncotarget, 2017, 9(3):3507-3518
Oncotarget, 2016, 7(9):9975-92
S2578 1-Phenylbiguanide 1-Phenylbiguanide (Phenylbiguanide, PBG, N-Phenylbiguanide) is a 5-hydroxytryptamine3 (5-HT3) receptor agonist with EC50 of 3.0 μM.
S2852 BRL-54443 BRL 54443 is a 5-HT1E and 5-HT1F receptor agonist with pKi of 8.7 and 9.25, respectively, with a weak binding affinity for 5-HT1A, 5-HT1B, 5-HT1D receptors.
Theranostics, 2021, 11(14):6950-6965
S2875 Prucalopride Prucalopride (R-93877) is a selective, high affinity 5-HT receptor agonist for 5-HT4A and 5-HT4B receptor with Ki of 2.5 nM and 8 nM, respectively, exhibits >290-fold selectivity against other 5-HT receptor subtypes.
Front Pharmacol, 2019, 10:1491
Gut, 2019, 68(8):1406-1416
Nutrients, 2017, 9(12)
S3180 Eletriptan HBr Eletriptan (UK-116044) is a selective 5-HT1B and 5-HT1D receptor agonist with Ki of 0.92 nM and 3.14 nM, respectively.
S3510New NLX-101 NLX-101 (F-15599) is a highly selective 5-HT1A receptor biased agonist that mediates antidepressant-like activity in rats via prefrontal cortex 5-HT 1A receptors.
S4244 Serotonin HCl Serotonin HCl (5-HT) is a monoamine neurotransmitter and Endogenous 5-HT receptor agonist.
Theranostics, 2021, 11(14):6950-6965
Sci Rep, 2021, 11(1):1250
Eur J Pharmacol, 2021, 908:174355
S4247 Prucalopride Succinate Prucalopride is a selective, high affinity 5-HT4 receptor agonist. The Ki values of prucalopride for human 5-HT(4a) and 5-HT(4b) receptor are 2.5 nM and 8 nM, respectively.
Front Pharmacol, 2019, 10:1491
Front Pharmacol, 2018, 9:171
Neurogastroenterol Motil, 2018, 30(2)
S4256 Buspirone HCl Buspirone is a serotonergic (5HT(1A) receptor agonist) anxiolytic drug with some D(2) dopaminergic effect, used for anxiety disorders.
Food Chem Toxicol, 2020, 30;141:111394
S4259 Vilazodone HCl Vilazodone HCl is a selective serotonin reuptake inhibitor (SSRI) and a partial agonist of 5-HT1A receptors, used for the treatment of major depressive disorder.
J Pain, 2019, 20(1):16.e1-16.e16
Acta Pol Pharm, 2017, 74(3):765-775
S4639 Brexpiprazole Brexpiprazole (OPC-34712) is a novel D2 dopamine and serotonin 1A partial agonist, called serotonin-dopamine activity modulator (SDAM), and a potent antagonist of serotonin 2A receptors, noradrenergic alpha 1B and 2C receptors with Ki values of 0.3, 0.12, 0.47, 0.17 and 0.59 nM for D2L, 5-HT1A, 5-HT2A, α1B receptors and α2C receptors respectivey.
S4751 Cisapride hydrate Cisapride (Propulsid, Alimix, Propulsin, Enteropride, Kinestase) acts directly as a selective serotonin 5-HT4 receptor agonist with IC50 of 0.483 μM. And It also acts indirectly as a parasympathomimetic.
Elife, 2021, 10e68714
S4839 Mosapride Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist.
S5064New Lasmiditan Lasmiditan (Reyvow) is a highly selective 5-hydroxytryptamine (serotonin) receptor 1F (5-HT1F) agonist that can be used as a promising acute anti-migraine therapy.
S5153 Tetrahydroberberine Tetrahydroberberine (Canadine) is an isoquinoline alkaloid with micromolar affinity for dopamine D2 (antagonist, pKi = 6.08) and 5-HT1A (agonist, pKi = 5.38) receptors but moderate to no affinity for other relevant serotonin receptors.
S5253 Cisapride (R 51619) Cisapride (R 51619, Kaudalit, Kinestase, Prepulsid, Presid, Pridesia, Propulsid) is a nonselective 5-HT4 receptor agonist with gastroprokinetic effects.
S5401 Tegaserod Maleate Tegaserod Maleate is a hydrogen maleate salt form of tegaserod, which is a 5-HT4 receptor partial agonist and binds with high affinity to 5-HT4 receptors. It has limited affinity for 5-HT1 receptors and no appreciable affinity for other 5-HT receptors, muscarinic, adrenergic, dopaminergic or opiate receptors.
Front Oncol, 2021, 11:683241
S5741 Quetiapine Quetiapine is an atypical antipsychotic used for the treatment of schizophrenia, bipolar disorder, and major depressive disorder.Quetiapine is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine have moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.23, 5.74, 7.54, 5.55.
S5848 Frovatriptan Succinate Frovatriptan Succinate is the succinate salt form of frovatriptan, a synthetic triptan with serotonin (5-HT) receptor agonist activity especially for the 5-HT1B/1D receptors.
S6324 5-Methoxytryptamine 5-Methoxytryptamine (Mexamine, Methoxytryptamine) is a tryptamine derivative that acts as a full agonist at the 5-HT1, 5-HT2, 5-HT4, 5-HT6, and 5-HT7 receptors.
S6489 Lasmiditan succinate Lasmiditan succinate (COL-144, LY573144) is a novel, centrally acting, highly selective 5-HT(1F) receptor agonist (Ki=2.21 nM) without vasoconstrictor activity.
S8447 8-OH-DPAT (8-Hydroxy-DPAT) 8-OH-DPAT (8-Hydroxy-DPAT) is a kind of classic 5-HT1A agonist with the pIC50 of 8.19. It has a selectivity of almost-1000 fold for a subtype of the 5-HT1 binding site; Its biological half-life is 1.5 hous.
S3716 Flibanserin Flibanserin (BIMT-17, BIMT-17-BS) is a nonhormonal, centrally acting molecule that acts as an agonist at postsynaptic 5-HT1A receptors and as an antagonist at 5-HT2A receptors.
Nat Commun, 2021, 12(1):5919
S5506 Vortioxetine Vortioxetine, a novel antidepressant for the treatment of major depressive disorder, is a 5-HT3, 5-HT7 and 5-HT1D receptor antagonist, 5-HT1B receptor partial agonist, 5-HT1A receptor agonist and serotonin (5-HT) transporter (SERT) inhibitor.
S5843 Cinitapride Hydrogen Tartrate Cinitapride Hydrogen Tartrate is a gastroprokinetic agent that acts as an agonist of the 5-HT1 and 5-HT4 receptors and as an antagonist of the 5-HT2 receptors
S5858 Vilazodone Vilazodone (EMD-68843, SB-659746A) is a novel antidepressant having a selective serotonin (5-HT) reuptake inhibitory and 5-HT1A receptor partial agonist activity. The affinity of vilazodone is much higher in the 5-HT reuptake site (Ki=0.1 nM) than in norepinephrine (Ki=56 nM) and dopamine (Ki=37 nM) sites.
J Pain, 2019, 20(1):16.e1-16.e16
S8021 Vortioxetine (Lu AA21004) HBr Vortioxetine (Lu AA21004), a multimodal serotonergic agent, is an antagonist of human (h) serotonin (5-HT)3A receptor and h5-HT7 receptor with Ki of 3.7 nM and 19 nM, respectively. Vortioxetine (Lu AA21004) is also a h5-HT1B receptor partial agonist with Ki of 33 nM and h5-HT1A receptor agonist with Ki of 15 nM, and a human 5-HT transporter (SERT) inhibitor with Ki of 1.6 nM.
S3913New Pimethixene maleate Pimethixene (Pimetixene) maleate, an antihistamine, anntimigraine agent and antiserotonergic compound, is a highly potent antagonist of a broad range of monoamine receptors, including a variety of serotonin receptors. Pimethixene maleate inhibits 5-HT2A, 5-HT2B, 5-HT2C, 5-HT1A, 5-HT1B, 5-HT6, 5-HT7, Adrenergic α-1A, Dopamine D1 Receptor, Dopamine D2 Receptor, Dopamine D4.4 Receptor, Histamine H1 Receptor, Muscarinic M1 and Muscarinic M2 with pKi of 10.22, 10.44, 8.42, 7.63, < 5, 7.30, 7.28, 7.61, 6.37, 8.19, 7.54, 10.14, 8.61 and 9.38, respectively.
S4358New Pimozide Pimozide (Orap, R6238) is an antagonist of Dopamine Receptors with Ki of 0.83 nM, 3.0 nM and 6600 nM for dopamine D3, D2 and D1 receptors, respectively. Pimozide also exhibits binding affinity at α2-adrenoceptor and 5-HT1A with Ki of 360 nM and 310 nM, respectively. Pimozide is an antipsychotic drug with anti-tumor activity and suppresses STAT3 and STAT5 activity.
Biol Pharm Bull, 2021, 10.1248/bpb.b21-00531
S5185New Perospirone Perospirone (SM-9018 free base) is an orally active antagonist of 5-hydroxytryptamine2 (5-HT2) receptor, dopamine2 (D2) receptor and 5-HT1A receptor with Ki of 0.6 nM, 1.4 nM and 2.9 nM, respectively.
S5197New Loxapine Loxapine (Adasuve), a typical neuroleptic, is a drug with D2/D3 receptor antagonist activity and a higher affinity for D3 than D2. Loxapine displays an extremely strong binding affinity for dopamine D4 and serotonin 5-HT2 receptors.
S5770New Pizotifen Pizotifen (Pizotyline, BC-105) is a potent antagonist of 5-Hydroxytryptamine (5-HT, Serotonin) 5-HT2 receptor with a high affinity for 5-HT1C binding site.
S5949New Metoclopramide hydrochloride hydrate Metoclopramide hydrochloride (Clorpa, Gimoti, Maxolon, Reglan) hydrate is primarily a Dopamine receptor antagonist, with 5HT3 receptor antagonist and 5HT4 receptor agonist activity, and used as an antiemetic and gastroprokinetic.
Pharmazie, 2021, 76(4):172-174
S5965New Urapidil Urapidil is an antihypertensive drug acting as an α1 adrenoreceptor antagonist and a 5-HT1A agonist.
S3510New NLX-101 NLX-101 (F-15599) is a highly selective 5-HT1A receptor biased agonist that mediates antidepressant-like activity in rats via prefrontal cortex 5-HT 1A receptors.
S5064New Lasmiditan Lasmiditan (Reyvow) is a highly selective 5-hydroxytryptamine (serotonin) receptor 1F (5-HT1F) agonist that can be used as a promising acute anti-migraine therapy.
Tags: 5-HT receptor drugs | Serotonin receptor drugs | 5-HT receptor agonist and antagonist drugs | Serotonin receptor antagonist drugs | Serotonin receptor agonist drugs | 5-HT3 receptor antagonist drugs | 5-HT receptor agonist and antagonist clinical trial | 5-HT receptor agonist and antagonist ic50 | 5-HT receptor agonist and antagonist review