Home Neuronal Signaling 5-HT Receptor

5-HT Receptor Agonists

Cat.No. Product Name Information Product Use Citations Product Validations
S1975 Aripiprazole Aripiprazole (OPC-14597) is a novel atypical antipsychotic drug that is reported to be a high-affinity 5-HT receptor partial agonist.
Mol Psychiatry, 2025, 10.1038/s41380-025-03374-6
Biomol Ther (Seoul), 2025, 33(1):170-181
J Dev Biol, 2025, 13(3)22
Verified customer review of Aripiprazole
S4244 Serotonin (5-HT) HCl Serotonin (5-HT) HCl is a monoamine neurotransmitter and Endogenous 5-HT receptor agonist.
EMBO Mol Med, 2025, 10.1038/s44321-025-00293-5
Anim Biosci, 2025, 38(8):1633-1643
Mod Pathol, 2022, 10.1038/s41379-022-01110-x
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, 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)
Verified customer review of Prucalopride
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)
Verified customer review of Prucalopride Succinate
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
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
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 pKi 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
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
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
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
S1488 Naratriptan HCl Naratriptan HCl is a triptan agent that is used for the treatment of migraine headaches.
S1385 Mosapride Citrate Mosapride Citrate (TAK-370, AS-4370, Gasmotin) is a gastroprokinetic agent that acts as a selective 5HT4 agonist.
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.
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.
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.
E6060New 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.
S5253 Cisapride (R 51619) Cisapride (R 51619, Kaudalit, Kinestase, Prepulsid, Presid, Pridesia, Propulsid) is a nonselective 5-HT4 receptor agonist with gastroprokinetic effects.
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.
E6067New 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.
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.
S6351New 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.
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.
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.
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).
E4870 Naratriptan Naratriptan is an agonist of 5-hydroxytryptamine1B/D (5-HT1B/D) receptors, which reduces the frequency of cluster headache.
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.
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
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.
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
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.
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.