5-HT Receptor Inhibitors

Cat.No.	Product Name	Information	Product Use Citations
S2232	Ketanserin	Ketanserin (R41468, Ketanserinum) is a specific 5-HT2A serotonin receptor antagonist with K_i 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
S2875	Prucalopride	Prucalopride (R-93877) is a selective, high affinity 5-HT receptor agonist for 5-HT4A and 5-HT4B receptor with K_i of 2.5 nM and 8 nM, respectively, and exhibits >290-fold selectivity against other 5-HT receptor subtypes.	Gut, 2019, 68(8):1406-1416 Front Pharmacol, 2019, 10:1491 Nutrients, 2017, 9(12)
S2849	SB269970 HCl	SB269970 HCl is a hydrochloride salt form of SB-269970, which is a 5-HT7 receptor antagonist with pK_i 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
S2677	BRL-15572 Dihydrochloride	BRL-15572 is a 5-HT1D receptor antagonist with pK_i 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 pK_i 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
S4247	Prucalopride Succinate	Prucalopride(R-108512) 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)
S4259	Vilazodone HCl	Vilazodone HCl(EMD68843,SB659746A) is a selective serotonin reuptake inhibitor (SSRI) and a partial agonist of 5-HT1A receptors, used for the treatment of major depressive disorder.	Cell Rep Med, 2024, 5(10):101777 Eur J Pharmacol, 2024, 985:177058 J Pain, 2019, 20(1):16.e1-16.e16
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
S8183	Pimavanserin tartrate	Pimavanserin tartrate(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.	Nat Neurosci, 2025, 28(11):2285-2295 Br J Pharmacol, 2021, 10.1111/bph.15756 Mol Ther Oncolytics, 2020, 19:19-32
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 bioRxiv, 2021, 10.1101/2021.11.14.468520 Sci Rep, 2018, 8(1):15753
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
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
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.	J Immunother Cancer, 2024, 12(11)e009805 Oncotarget, 2017, 9(3):3507-3518 Oncotarget, 2016, 7(9):9975-92
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
S3196	Azacyclonol	Azacyclonol (MER 17, MDL 4829), also known as γ-pipradol, is a drug used to diminish hallucinations in psychotic individuals.	Bioengineered, 2021, 12(1):7446-7458 Oncol Rep, 2020, 44(6):2503-2516
S5401	Tegaserod Maleate	Tegaserod Maleate(HTF-919) 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.	Cancers (Basel), 2022, 14(15)3592 Front Oncol, 2021, 11:683241
S2852	BRL-54443	BRL 54443 is a 5-HT1E and 5-HT1F receptor agonist with pK_i of 8.7 and 9.25, respectively, with a weak binding affinity for 5-HT1A, 5-HT1B, 5-HT1D receptors.	bioRxiv, 2024, 10.1101/2024.01.28.577572 Theranostics, 2021, 11(14):6950-6965
S8447	8-OH-DPAT (8-Hydroxy-DPAT)	8-OH-DPAT (8-Hydroxy-DPAT) is a classic 5-HT1A agonist with a pIC50 of 8.19. This compound has a selectivity of almost-1000 fold for a subtype of the 5-HT1 binding site, and its biological half-life is 1.5 hours.	Nat Neurosci, 2025, 28(11):2285-2295 Gastroenterology, 2024, 167(5):993-1007
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.	J Immunother Cancer, 2024, 12(11)e009805 Elife, 2021, 10e68714
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
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.	Arch Biochem Biophys, 2024, 754:109958 Nat Commun, 2021, 12(1):5919
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
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
S1607	Rizatriptan Benzoate	Rizatriptan Benzoate (MK-462) is an agonist at serotonin 5-HT1B and 5-HT1D receptors, used to treat acute migraine attacks.	Viruses, 2024, 16(10)1559
S1649	Zolmitriptan	Zolmitriptan (BW-311C90) 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
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
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
S2856	SB 271046 hydrochloride	SB 271046 hydrochloride is a potent, selective and orally active 5-HT6 receptor antagonist with pK_i of 8.9, exhibits 200-fold greater selectivity over other 5-HT receptor subtypes.	Sci Rep, 2018, 8(1):15753
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
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.	J Immunother Cancer, 2024, 12(11)e009805
E4953	Citalopram	Citalopram is a selective serotonin reuptake inhibitor (SSRI) that selectively inhibits the 5-HT transporter, blocks the reuptake of 5-HT in the presynaptic membrane, prolongs and increases the effects of 5-HT, and enhances serotonin neurotransmission by potently and selectively inhibiting serotonin reuptake (SSRI).	Alzheimers Dement, 2025, 21(3):e70081
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
S4256	Buspirone HCl	Buspirone(Buspirone hydrochloride) 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
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
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.	J Lipid Res, 2022, 63(8):100249
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.	J Immunother Cancer, 2024, 12(11)e009805
S2578	1-Phenylbiguanide	1-Phenylbiguanide (Phenylbiguanide, PBG, N-Phenylbiguanide) is a 5-hydroxytryptamine3 (5-HT3) receptor agonist with EC50 of 3.0 μM.	Cell Res, 2025, 10.1038/s41422-025-01085-9
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
S3175	Atomoxetine HCl	Atomoxetine (LY 139603) is a selective norepinephrine (NE) transporter inhibitor with K_i of 5 nM, with 15- and 290-fold lower affinity for human 5-HT and DA transporters.	Cell Commun Signal, 2024, 22(1):532
S5563	Thioridazine hydrochloride	Thioridazine (Aldazine, Mellaril) is a potent antianxiety and antipsychotic agent.	Cell Syst, 2019, 8(2):97-108
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
S1869	Dapoxetine HCl	Dapoxetine HCl (LY-210448) is a short-acting novel selective serotonin reuptake inhibitor, used for the treatment of premature ejaculation.
S1488	Naratriptan HCl	Naratriptan HCl is a triptan agent that is used for the treatment of migraine headaches.
S2691	BMY 7378 Dihydrochloride	BMY 7378 is a multi-targeted inhibitor of α2C-adrenoceptor and α1D-adrenoceptor with pK_i of 6.54 and 8.2, respectively, and acts as a mixed agonist and antagonist for 5-HT1A receptor with pK_i of 8.3.
S1385	Mosapride Citrate	Mosapride Citrate (TAK-370, AS-4370, Gasmotin) is a gastroprokinetic agent that acts as a selective 5HT4 agonist.
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.
S3180	Eletriptan HBr	Eletriptan (UK-116044) is a selective 5-HT1B and 5-HT1D receptor agonist with K_i of 0.92 nM and 3.14 nM, respectively.
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.
S5741	Quetiapine	Quetiapine(ICI204636) is an atypical antipsychotic used for the treatment of schizophrenia, bipolar disorder, and major depressive disorder. This compound is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. It is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. This chemical has 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.
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. This compound is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease.
E6066^New	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.
S5848	Frovatriptan Succinate	Frovatriptan Succinate(SB 209509 Succinate,VML 251 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.
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.
E6060^New	BUSPIRONE	BUSPIRONE (Ansial) is a potent agonist of serotonin 5-HT1A receptor as well as an antagonist of dopamine D2 autoreceptor. It exhibits anxiolytic and antidepressant activity, alleviates anxiety, depression, and colitis, suppresses neuroinflammation, modulates gut microbiota, and can be used in research for treating anxiety and depression.
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.
S5253	Cisapride (R 51619)	Cisapride (R 51619, Kaudalit, Kinestase, Prepulsid, Presid, Pridesia, Propulsid) is a nonselective 5-HT4 receptor agonist with gastroprokinetic effects.
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.
S0282	YL 0919	YL0919, a novel structure compound, exerts dual effect on the serotonergic system, as both 5-hydroxytryptamine receptor 1A (5-HT1A) agonist and 5-HT uptake blocker, showing remarkable antidepressant effects in animal models.
S9239	Isocorynoxeine	Isocorynoxeine (7-Isocorynoxeine), a major alkaloid found in Uncaria rhynchophylla, exhibits wide beneficial effects on the cardiovascular and cardiocerebral vascular systems. This compound suppresses 5-HT2A receptor-mediated current response with IC50 of 72.4 μM.
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.
E6067^New	Frovatriptan succinate hydrate	Frovatriptan succinate hydrate ((R)-Frovatriptan succinate hydrate, SB 209509 succinate) is a potent, selective and orally active agonist of 5-HT1B with pEC50 value of 8.2 and 5-HT1D receptor. It displays >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and a >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor.
S2865	VUF 10166	VUF10166 is a novel, potent and competitive antagonist for 5-HT3A receptor with K_i of 0.04 nM, its affinity at 5-HT3AB receptor is significantly lower.
E4835	Sumatriptan	Sumatriptan (GR43175) is a selective agonist of 5-HT1D receptor, which is effectively used in the acute treatment of migraine. It causes a vasopressor response in the systemic and pulmonary arterial circulations and coronary artery vasoconstriction.
S6351^New	Serotonin	Serotonin is a monoamine neurotransmitter in the Central Nervous System (CNS) and an endogenous 5-HT receptor agonist. This compound is also a catechol O-methyltransferase (COMT) inhibitor.
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.
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.
S0318	Ansofaxine hydrochloride	Ansofaxine hydrochloride (LY03005, LPM570065), a triple reuptake inhibitor, inhibits serotonin, dopamine and norepinephrine reuptake with IC50 values of 723, 491 and 763 nM, respectively.
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.
S3510	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.
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.
E4851	Tandospirone citrate	Tandospirone citrate, is a potent, selective and a partial agonist of the 5-HT1A receptor. It exhibited good permeability in the intestine, with passive diffusion being the main mode of drug absorption, it also has anxiolytic effects and can be used in generalized anxiety disorder treatments.
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.
E4976	Tegaserod	Tegaserod is an orally active agonist of serotonin receptor 4 (5-HT4R) and also acts as an antagonist of 5-HT2B receptor with pKi values of 7.5, 8.4, and 7.0 for human recombinant 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. This compound has anti-tumor activity and is used in the research of irritable bowel syndrome (IBS).
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.
E4812	Fluoxetine	Fluoxetine (LY-110140 free base) is a selective 5-hydroxytryptamine (5-HT) reuptake inhibitor. This compound is used widely in the treatment of depression, anxiety-related symptoms and also displays anticonvulsant activity.
E4870	Naratriptan	Naratriptan is an agonist of 5-hydroxytryptamine_1B/D (5-HT_1B/D) receptors, which reduces the frequency of cluster headache.
E4866	Paroxetine	Paroxetine is a potent and selective serotonin reuptake inhibitor (SSRI) used to treat depression and anxiety disorders. It inhibits pyroptosis and reduces osteoclast formation by blocking the NF-κB signalling pathway.
S3913	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.
S0113	Eptapirone	Eptapirone (F11440) is a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential.The affinity (pKi) of this compound for 5-HT1A binding sites is 8.33.
S4839	Mosapride	Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist.
S9039	Albiflorin	Albiflorin, a natural product isolated from Paeoniae Radix, is a novel 5-HT and NE reuptake inhibitor with high selectivity.
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.
S5987^New	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.
E7725	Doxepin	Doxepin (MF 10) is a potent inhibitor of serotonin reuptake and noradrenaline reuptake with a Ki of 68 nM and 29.5 nM, respectively. It acts as a receptor antagonist for histamine H1, acetylcholine muscarinic, and α1 adrenoceptor with a Ki of 0.24 nM, 83 nM, and 24 nM, respectively and significantly inhibits CYP450.
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.
E4839	Ziprasidone	Ziprasidone(CP-88059,Geodon,Zeldox) is an orally active agonist of 5-HT(1A) receptor. It has high affinity for dopamine D2, D3, 5-hydroxytryptamine 5HT2A, 5HT2C, 5HT1A, 5HT1D, α-adrenergic receptors
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.
E2356	Tandospirone	Tandospirone (SM-3997), a potent and selective 5-HT1A receptor partial agonist, with a Ki of 27 nM, has anxiolytic and antidepressant activities.
S6465	Tafamidis	Tafamidis is a kinetic stabilizer of transthyretin (TTR) that prevents amyloidogenesis by wild-type and mutant TTRs.
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
E6699^New	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-HT_2B/2C over 5-HT_2A receptor antagonist with pKi values of 7.5, 6.9 and 5.2 for 5-HT_2B, 5-HT_2C and 5-HT_2A, 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.
E4907	Clomipramine	Clomipramine(Hydiphen, Anafranil base) blocks the production of norepinephrine in the central nervous system and 5-HT reuptake, thereby exerting sedative and anticholinergic effects, with IC50 of 1.5 nM. This compound is also a non-selective monoamine reuptake inhibitor that can affect the transmission of multiple neurotransmitters.
S0222	Lvguidingan	Lvguidingan (Anticonvulsant 7903, 3,4-dichlorophenyl propenylisobutylamide) is an anticonvulsant/antiepileptic agent. This compound is found to be able to increase the concentration of 5-HT and 5-HIAA in mice brain.
E4862	Pimethixene	Pimethixene(Calmixen, Pimetixene) is a highly potent and non-selective antagonist of the 5-HT_2B 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.
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.
S2669	LY310762 HCl	LY310762 is a 5-HT1D receptor antagonist with K_i 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
S3024	Lamotrigine	Lamotrigine (BW-430C,LTG) 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 this compound also is a sodium channel blocker.	iScience, 2024, 27(10):110862 Front Pharmacol, 2024, 15:1489888 Nat Commun, 2022, 13(1):2785
S4053	Sertraline HCl	Sertraline HCl (CP-51974-1) is a 5-HT antagonist with K_i of 13 nM.	EMBO Mol Med, 2025, 17(4):625-644 Cell Rep, 2024, 43(10):114818 Antimicrob Agents Chemother, 2021, AAC.01146-20
S2084	Duloxetine HCl	Duloxetine HCl (LY-248686) is a serotonin-norepinephrine reuptake inhibitor with K_i of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD).	Cancers (Basel), 2022, 14(19)4883 Drug Metab Dispos, 2015, 44(3):378-88 J Pharmacol Exp Ther, 2014, 349(3):402-7
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
S4064	Escitalopram Oxalate	Escitalopram Oxalate is a selective serotonin (5-HT) reuptake inhibitor (SSRI) with K_i of 0.89 nM.	Proc Natl Acad Sci U S A, 2025, 122(10):e2420499122 Cell Rep, 2024, 43(10):114818 J Matern Fetal Neonatal Med, 2023, 36(1):2183468
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. This compound 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. It 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
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
S4377	Imipramine HCl	Imipramine (Melipramine,G 22355) is a tricyclic antidepressant (TCA) of the dibenzazepine group, mainly used in the treatment of major depression and enuresis (inability to control urination).	Cancer Drug Resist, 2022, 5(3):612-624 Antioxidants (Basel), 2021, 10(6)956 Biomedicines, 2021, 9(9)1230
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. This compound is a potent and high efficacy agonist at h5-HT2C receptors with Ki of 9.3 nM. It directly inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with IC50 of 268 nM.	Behav Brain Funct, 2025, 21(1):22 Theranostics, 2023, 13(10):3149-3164 JCI Insight, 2023, 8(16)e170434
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), PPARγ and cdc-like kinases (CLKs). Harmine inhibits 5-HT2A serotonin receptor with Ki of 397 nM.	Cell Death Discov, 2025, 11(1):282 Cancers (Basel), 2022, 14(2)326
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)
S5949	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.	Anticancer Drugs, 2022, 10.1097/CAD.0000000000001344 Pharmazie, 2021, 76(4):172-174
S1642	Methyldopa	Methyldopa (Aldomet) is a DOPA decarboxylase competitive inhibitor with an ED50 of 21.8 mg/kg.	J Immunother Cancer, 2024, 12(11)e009805
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 D_2L, and 9.31 for D_2S receptors. It also acts as an antagonist forserotonin receptors, with pKi of 9.24, 8.59, 7.73, and 6.87 for5-HT2B,5-HT_1A, 5-HT_2A, and 5-HT_2C 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.
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.
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.
E4856	Rotigotine Hydrochloride	Rotigotine Hydrochloride (N-0923 Hydrochloride) is a potent Agonist of dopamine receptor, with Ki values of 0.71 nM for dopamine D3 receptor, 4-15 nM for D2, D5, D4 receptors, and 83 nM for dopamine D1 receptor. It also acts as a partial agonist of the 5-HT1A receptor, and as an antagonist of the α2B-adrenergic receptor.
S5965	Urapidil	Urapidil is an antihypertensive drug acting as an α1 adrenoreceptor antagonist and a 5-HT1A agonist.
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.
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.
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.
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.
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.
E7427	Dehydroaripiprazole	Dehydroaripiprazole (OPC-14857, DM-14857) is the active metabolite of aripiprazole, primarily metabolized by CYP3A4 and CYP2D6. It inhibits glutamate release from rat prefrontocortical nerve terminals by activating dopamine D2 and 5-HT1A receptors, reducing nerve terminal excitability and VDCC activation through a PKA-mediated signaling cascade, potentially contributing to its neuroprotective effects in excitotoxic injury.