Home Neuronal Signaling 5-HT Receptor

5-HT Receptor Antagonists

Cat.No. Product Name Information Product Use Citations Product Validations
S2493 Olanzapine Olanzapine (LY170053,Zyprexa, Zalasta, Zolafren, Olzapin, Oferta, Zypadhera) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist.
Brain Behav Immun, 2025, 130:106111
Mol Psychiatry, 2025, 10.1038/s41380-025-03374-6
FASEB J, 2025, 39(3):e70355
Verified customer review of Olanzapine
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.
Clin Exp Metastasis, 2025, 42(2):12
J Immunother Cancer, 2024, 12(11)e009805
Alzheimers Dement, 2023, 10.1002/alz.13090
Verified customer review of Clozapine
S2663 WAY-100635 Maleate WAY-100635 Maleate is a potent and selective 5-HT receptor antagonist with IC50 of 0.95 nM.
Nat Neurosci, 2025, 28(11):2285-2295
Gastroenterology, 2024, 167(5):993-1007
Med Sci Sports Exerc, 2022, 54(4):566-581
Verified customer review of WAY-100635 Maleate
S2346 Puerarin Puerarin (Kakonein), an isoflavones found in the root of Radix puerariae, is a 5-HT2C receptor and benzodiazepine site antagonist.
Acta Biochim Biophys Sin (Shanghai), 2024, 56(2):270-279
Int J Mol Sci, 2023, 24(9)8328
Ecotoxicol Environ Saf, 2022, 247:114239
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.
J Adv Res, 2024, S2090-1232(24)00079-1
Cell Commun Signal, 2024, 22(1):266
Mol Cancer, 2023, 22(1):136
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.
UNIVERSITY OF PÉCS, 2023,
Anticancer Res, 2021, 41(2):687-697
Molecules, 2020, 25(18)E4206
Verified customer review of Ziprasidone HCl
S2232 Ketanserin Ketanserin (R41468, Ketanserinum) 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.
J Immunother Cancer, 2025, 13(6)e011088
Lab Invest, 2021, 1-14
Int Immunopharmacol, 2019, 10.1016/j.intimp.2019.106036
Verified customer review of Ketanserin
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.
J Adv Res, 2024, S2090-1232(24)00079-1
Med Sci Sports Exerc, 2022, 54(4):566-581
Cancers (Basel), 2021, 13(21)5305
Verified customer review of SB269970 HCl
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
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.
J Dev Biol, 2025, 13(3)22
Biomolecules, 2023, 10.3390/biom13091321
Biomolecules, 2023, 13(9)1321
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.
J Neuroinflammation, 2022, 19(1):23
Lab Invest, 2021, 1-14
Int Immunopharmacol, 2019, 10.1016/j.intimp.2019.106036
S1243 Agomelatine (S20098) Agomelatine (Valdoxan, Melitor, Thymanax, S20098) is classified as a norepinephrine-dopamine disinhibitor (NDDI) due to its antagonism of the 5-HT2C receptor.
Cells, 2022, 11(21)3467
Sci Rep, 2018, 8(1):15753
Neuropsychiatry (London), 2018, None
S1615 Risperidone Risperidone (R-64766) is a mutil-targeted antagonist for dopamine, serotonin, adrenergic and histamine receptors, used to treat schizophrenia and bipolar disorder.
Biochem Biophys Res Commun, 2025, 786:152756
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00196-X
Anticancer Res, 2021, 41(2):687-697
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. This compound 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.
Int J Neuropsychopharmacol, 2025, pyaf019
Antioxidants (Basel), 2024, 13(6)714
Br J Pharmacol, 2021, 178(5):1182-1199
S1390 Ondansetron HCl Ondansetron HCl is a serotonin 5-HT3 receptor antagonist, used to prevent nausea and vomiting caused by cancer chemotherapy, and radiation therapy.
Cell Host Microbe, 2025, 33(3):408-419.e8
Immunity, 2019, 50(5):1163-1171
Int J Urol, 2016, 23(11):946-951
Verified customer review of Ondansetron HCl
S4249 Flopropione Flopropione is a spasmolytic or antispasmodic agent, and acts as a 5-HT1A receptor antagonist.
SSRN, 2023, 17 Pages
Cells, 2022, 11(16)2585
Front Microbiol, 2020, 10:2936
S2112 Blonanserin Blonanserin (AD 5423) is a relatively selective serotonin (5-HT)2A and dopamine D2 antagonist, used the treatment of schizophrenia.
Curr Issues Mol Biol, 2025, 47(6)391
Sci Rep, 2018, 8(1):15753
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
Verified customer review of SB742457
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.
Eur J Pharmacol, 2024, 979:176835
Cell, 2017, 170(1):185-198
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.
Chin Med, 2024, 19(1):87
Neural Regen Res, 2023, 18(9):2019-2028
S1345 Granisetron HCl Granisetron is a serotonin 5-HT3 receptor antagonist,used to treat chemotherapy-induced nausea and vomiting.
Redox Biol, 2023, 67:102889
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
Verified customer review of PRX-08066 Maleic acid
S4086 Loxapine Succinate Loxapine Succinate(NSC 759578) is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent.
Anticancer Res, 2021, 41(2):687-697
S1996 Ondansetron Ondansetron (GR 38032F, GR-C507/75,SN 307) is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic.
Int J Urol, 2016, 23(11):946-951
Verified customer review of Ondansetron
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
Verified customer review of SB 271046 hydrochloride
S0723 BRL 15572 BRL-15572 is a preferential antagonist at native human 5-HT1D receptors, can be a useful tool for the differentiation between human 5-HT1B and 5-HT1D receptors in functional studies.
J Neuroinflammation, 2022, 19(1):205
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.
EMBO Mol Med, 2025, 10.1038/s44321-025-00293-5
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.
J Med Virol, 2023, 95(6):e28856
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
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
S5770 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.
Front Pharmacol, 2025, 16:1539032
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.
Anim Biosci, 2025, 38(8):1633-1643
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
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.
Neural Regen Res, 2023, 18(9):2047-2055
S2016 Mirtazapine Mirtazapine (Org3770,6-Azamianserin) is an adrenergic and seroton receptor antagonist, used to treat depression.
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.
S1394 Pizotifen Malate Pizotifen Malate (Sandomigran, pizotyline,BC-105) is a benzocycloheptane based agent used for recurrent migraine headaches.
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.
E6066New cyproheptadine Cyproheptadine is a potent and orally active antagonist of 5-HT2A receptor with antiserotonergic and antidepressant effects. It also exhibits antiplatelet activities and has the potential to treat thromboembolic and depressive disorders.
S5326 Dolasetron Dolasetron(MDL-73147EF) 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.
E4952 Nefazodone Nefazodone is a selective antagonist of 5-HT2Areceptors and moderately inhibits serotonin and norepinephrine reuptake, enhancing 5-HT synaptic transmission. It is also a potent inhibitor of CYP3A4 with reduced anticholinergic, alpha-adrenolytic, and sedative effects, along with notable immunoprotective properties.
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.
S0939 γ-Mangostin γ-Mangostin (Gamma-Mangostin) is a novel competitive 5-hydroxytryptamine 2A (5-HT2A) receptors antagonist, which can reduce the perfusion pressure response of rat coronary artery to 5-HT2A with an IC50 of 0.32 µM and inhibit [3H] spiperone binding to cultured rat aortic myocytes with an IC50 of 3.5 nM. Gamma-Mangostin is also an inhibitor of Transthyretin (TTR) fibrillization.
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.
E4903 Dalasetron Mesylate Hydrate Dolasetron Mesylate hydrate(MDL-73147EF hydrate) is an antagonist of serotonin 5-HT3 receptor. It is used in the treatment of patients with nausea and vomiting following chemotherapy.
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. This compound shows antipsychotic activity.
E4477 Lumateperone Lumateperone (ITI-007) is an antagonist of 5-HT2A receptor with Ki of 0.54 nM. It has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia.
S5185 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.
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. This compound behaves like a typical neuroleptic when used in higher doses (greater than 0.1 mg/kg).
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.
E4840 Ziprasidone hydrochloride monohydrate Ziprasidone hydrochloride monohydrate is an antipsychotic drug, a combined antagonist of 5-HT (serotonin) and dopamine receptor. It exhibits binding affinities for D2, 5-HT2A, 5-HT1A with Ki values 4.8 nM, 0.42 nM, 3.4 nM respectively.
E0070 4F 4PP oxalate 4F 4PP oxalate is an antagonist of the serotonin (5-HT) receptor subtype 5-HT2A (Ki = 5.3 nM), which is selective for 5-HT2A receptors over 5-HT1C receptors (Ki = 620 nM). 
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. This compound has electrophysiological and anxiolytic properties in vivo.
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.
S5987New Ritanserin (R 55667) Ritanserin (R 55667) is a highly potent, selective, orally active, and long-acting antagonist of 5-HT2 receptor with an IC50 of 0.9 nM. It exhibits minimal activity at H1, D2, and adrenergic receptors and enhances midbrain dopamine neuron activity by blocking 5-HT2-mediated inhibition.
E7733 SB 242084 dihydrochloride SB 242084 dihydrochloride is a selective, high affinity, potent and brain penetrant antagonist of 5-HT2C receptor with pKi of 9.0. It exhibits anxiolytic-like activity and may have potential for treating anxiety, depression, and negative symptoms of schizophrenia.
E4930 Asenapine Asenapine(Org 5222, HSDB8061) is a multi-target receptor antagonist. It acts as an antagonist of serotonin receptors with pKi values of 8.4-10.5, adrenoceptors with pKi values of 8.9-9.5, dopamine receptors with pKi values of 8.9-9.4 and histamine receptors with pKi values of 8.2-9.0.
E6699New Opiranserin hydrochloride Opiranserin hydrochloride (VVZ-149 hydrochloride) is a non-opioid and non-NSAID analgesic that acts as a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC50 of 0.86 μM and 1.3 μM, respectively.
S0893 SB-200646A SB-200646A is the first selective 5-HT2B/2C over 5-HT2A receptor antagonist with pKi values of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. 
E4874 Lumateperone Tosylate Lumateperone tosylate(ITI-007) is an antagonist of 5-HT2A receptor. It also acts as a partial agonist of presynaptic D2 receptors, as an antagonist of postsynaptic D2 receptors, and as a modulator of dopamine D1 receptor. Lumateperone tosylate demonstrates anticancer activity.
S2644 Lerisetron Lerisetron (F 0930, F 0930RS) is a 5-HT3 receptor antagonist with IC50 of 0.81μM.
E8039 Roluperidone Roluperidone (CYR-101; MIN-101) is a cyclic amide derivative with antagonistic activity against serotonergic 5-HT2A, sigma-2, and α1A-adrenergic receptors. It exhibits Ki of 7.53 nM for 5-HT2A and 8.19 nM for sigma-2 receptors, with potential for the treatment of schizophrenia.
E4862 Pimethixene Pimethixene(Calmixen, Pimetixene) is a highly potent and non-selective antagonist of the 5-HT2B receptor, with a pKi of 10.44. It also functions as an antihistamine and anticholinergic agent, and is a highly potent multi-target antagonist with antagonistic effects on multiple receptors.
S4283 Cyclobenzaprine HCl Cyclobenzaprine HCl(Cyclobenzaprine hydrochloride) is a muscle relaxant by blocking pain sensations, used for the treatment of muscle spasms; A 5-HT2 receptor antagonist.
S2669 LY310762 HCl LY310762 is a 5-HT1D receptor antagonist with Ki of 249 nM, having a weaker affinity for 5-HT1B receptor.
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.
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).
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. This compound is a novel 5-HT2B receptor antagonist with a possible therapeutic role in treating ADHD.
S5749 Chlorpromazine Chlorpromazine (CPZ) is a low-potency typical antipsychotic agent that is used to treat psychotic disorders such as schizophrenia. This compound inhibits 5-HT(2A) receptor and dopamine D2 in vitro. It also inhibits sodium channel and blocks HERG potassium channels with IC50 of 21.6 μM.
EMBO J, 2025, 10.1038/s44318-025-00537-7
Mol Psychiatry, 2025, 10.1038/s41380-025-03374-6
J Thromb Haemost, 2025, 23(9):2926-2943
S4358 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. This compound also exhibits binding affinity at 5-HT1A and α1-adrenoceptor with Ki of 310 nM and 39 nM, respectively. It is an antipsychotic drug with anti-tumor activity and suppresses STAT3 and STAT5 activity.
Mol Metab, 2025, 91:102069
Oncogenesis, 2025, 14(1):31
Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101286
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. This compound 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.
Alzheimers Dement, 2023, 10.1002/alz.13090
Chem Biol Drug Des, 2022, 100(5):699-721
bioRxiv, 2021, 10.1101/2021.11.14.468520
S5947 Amitriptyline Amitriptyline (MK-230, N-750, Ro41575) is a tricyclic antidepressant (TCA) with analgesic properties, widely used to treat depression and neuropathic pain. This compound is an inhibitor of both serotonin transporter (SERT) and norepinephrine transporter (NET) with Ki of 3.45 nM and 13.3 nM, respectively. It 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.
Cancer Cell, 2025, 43(4):776-796.e14
Cancers (Basel), 2019, 11(12)
E4910 Cariprazine Cariprazine(RGH-188, MP-214) acts primarily as a partial agonist at dopamine receptors, with pKi values of 10.07 for D3, 9.16 for D2L, and 9.31 for D2S receptors. It also acts as an antagonist forserotonin receptors, with pKi of 9.24, 8.59, 7.73, and 6.87 for5-HT2B,5-HT1A, 5-HT2A, and 5-HT2C receptors, respectively.
J Dev Biol, 2025, 13(3)22
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.
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.
S5707 Aripiprazole lauroxil Aripiprazole lauroxil(Aristada) is an extended-release prodrug of aripiprazole designed for intramuscular injection. It acts as a dopamine-serotonin system stabilizer, with a potent partial agonist for dopamine D2 and serotonin 5-HT1A receptors while an antagonist for serotonin 5-HT2A receptors.
S6087 Indophagolin Indophagolin, a potent indoline-containing autophagy inhibitor with IC50 of 140 nM, antagonizes the purinergic receptor P2X4 as well as P2X1 and P2X3 with IC50s of 2.71, 2.40 and 3.49 μM, respectively, also has a strong antagonistic effect on serotonin receptor 5-HT6 with IC50 of 1.0 μM.
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.