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GPCR/G Protein 5-HT Receptor

5-HT Receptor

5-hydroxytryptamine receptors or 5-HT receptors, or serotonin receptors, are a group of G protein-coupled receptor and ligand-gated ion channels found in the central and peripheral nervous systems. They mediate both excitatory and inhibitory neurotransmission. The serotonin receptors are activated by the neurotransmitter serotonin, which acts as their natural ligand.
Cat No. product name
T12262L NPS ALX Compound 4a dihydrochloride NPS ALX Compound 4a dihydrochloride is a potent and selective antagonist of 5-HT6 receptor (IC50 of 7.2 nM)
T12262 NPS ALX Compound 4a NPS ALX Compound 4a is a potent and selective antagonist of 5-HT6 receptor (IC50 of 7.2 nM)
T12489L Pimethixene maleate Pimethixene maleate is a highly potent5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors antagonist(wi...
T12489 Pimethixene Pimethixene is a highly potent 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors antagonist(pKis of 7...
T12480 Pipamperone Pipamperone is a high-affinity 5-HT2A receptor and D4 receptor antagonist (pKi of 8.2 and 8.0,respectively) .
T12565 PRX933 hydrochloride PRX933 hydrochloride is an agonist of 5-HT2c receptor.
T10075 2-Methyl-5-HT 2-Methyl-5-HT (2-Methyl-5-hydroxytryptamine) is a potent and selective 5-HT3 receptor agonist with anti-depressive-like effects.
T10075L2 2-Methyl-5-HT hydrochloride 2-Methyl-5-HT hydrochloride (2-Methyl-5-hydroxytryptamine) is a potent and selective 5-HT3 receptor agonist with anti-depressive-like effects.
T10114 3-Hydroxy agomelatine 3-Hydroxy agomelatine is an Agomelatine metabolite and a 5-HT2C receptor antagonist (IC50: 3.2 μM; Ki: 1.8 μM).
T10113 3-Hydroxy agomelatine D3 3-Hydroxy agomelatine D3 is a deuterium labeled 3-Hydroxy agomelatine. 3-Hydroxy agomelatine is an Agomelatine metabolite and a 5-HT2C receptor antagonist (IC50...
T10168 5-HT1A modulator 1 5-HT1A modulator 1 displays very high affinities for the 5HT1A, adrenergic α1, and dopamine D2 receptor (IC50s: 2 nM, 10 nM and 40 nM).
T10498 5-HT2A antagonist 1 5-HT2A antagonist 1 is a 5-HT2A antagonist extracted from patent US5728835A and JP 1007727. It may be useful in the treatment of gastrointestinal disorders circ...
T10162 5-HT3 antagonist 3 5-HT3 antagonist 3 (Compound 15b) is a high-affinity 5-HT3 receptor antagonist. It binds to 5-HT3 receptors in rat brain cortical membranes (Ki: 0.25 nM).
T10006 5-HT3-In-1 5-HT3-In-1 (compound example 8) is extracted from patent EP0748807A1 with 5-HT3 inhibition activity.
T10169 5-HT4 antagonist 1 5-HT4 antagonist 1 is a 5-HT4 receptor antagonist (pKi: 9.6).
T10053 5HT6-ligand-1 5HT6-ligand-1 is a potent 5-HT6 receptor ligand (Ki: 1.43 nM).
T10170 5-HT7 agonist 1 5-HT7 agonist 1 is a selective 5-HT7 receptor agonist (IC50: 222.93 nM), which can be used for the 5-HT7 receptor-related disease, such as CNS disorders.
T10192 7-Desmethyl-3-hydroxyagomelatine 7-Desmethyl-3-hydroxyagomelatine is a metabolite of Agomelatine and has less activity than Agomelatine. Agomelatine is a melatonergic (MT1 and MT2) agonist and ...
T10989 Dehydroaripiprazole Dehydroaripiprazole (OPC-14857) is the active metabolite of aripiprazole. Aripiprazole is an antipsychotic drug, which is metabolized by CYP3A4 and CYP2D6 and m...
T10996 Deramciclane Deramciclane has high affinity for 5-HT2A and 5-HT2C receptors. It acts as an antagonist in both receptor subtypes and has inverse agonist properties for 5-HT2C...
T11075 Donitriptan Donitriptan is an effective agonist for the 5-HT1B/1D receptor, with pKis of 9.4 and 9.3, respectively.
T10075L 2-Methyl-5-HT maleate 2-Methyl-5-HT maleate (2-Methyl-5-hydroxytryptamine maleate) is a potent and selective 5-HT3 receptor agonist, which is shown to display anti-depressive-like ef...
T8445 PU-02 PU-02 is a potent and selective antagonist of 5-HT3 receptor.
T8438 4i 4i is a 5-HT3 receptor antagonist,It modulates the serotonergic system.
T14190 Alniditan Alniditan is a receptors agonist of 5-HT1B/1D in HEK 293 cells (IC50: 1.7 and 1.3 nM). For 5-HT1B/1D receptors, the pKi values are 8.96 and 9.40, respectively...
T14526 Bemesetron Bemesetron (MDL 72222) is an antagonist of 5-HT3 receptor (IC50: nM). It has Neuroprotective effect[2].
T12631 (R)-Mirtazapine D3 (R)-Mirtazapine D3 is a deuterium labeled (R)-Mirtazapine.(R)-Mirtazapine is a antagonist of 5-HT3 receptor.
T12632 (R)-Mirtazapine (R)-Mirtazapine is a R(−)-enantiomer of Mirtazapine with antinociceptive properties in an animal model of acute thermal nociception. (R)-Mirtazapine is a anta...
T12638 (R)-Praziquantel D11 (R)-Praziquantel D11 is the deuterium labeled (R)-Praziquantel. (R)-Praziquantel is the active enantiomer of Praziquantel, is a partial the human 5-HT2B recepto...
T12716 RG-12915 RG-12915 is a selective antagonist of 5-HT3(IC50 value of 0.16 nM).
T10267 Agomelatine (L(+)-Tartaric acid) Agomelatine (S-20098) L(+)-Tartaric acid is a specific agonist of MT1 and MT2 receptors (Kis: 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and...
T10294 AM9405 AM9405 is a novel peripherally active cannabinoid type 1 (CB1) and serotonin type 3 receptor agonist. It inhibits twitch contraction of the ileum and the colon ...
T10344 AP521 AP521 is an agonist of the human 5-HT1A receptor (IC50: 94 nM).
T10371 Arotinolol Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker. Arotinolol also shows potency for inhibiting the binding of the ra...
T10380 AS19 AS19 is a potent, selective 5-HT7 receptor agonist (IC50: 0.83 nM; Ki: 0.6 nM). AS19 is selective for 5-HT7 over 5-HT1A, 5-HT1B, 5-HT1D, and 5-HT5A receptors (K...
T14782 Brilaroxazine Brilaroxazine (RP5603) is a partial agonist of dopamine (DA) D2, D3, and D4 receptors, 5-HT1A (Ki: 1.5 nM) and 5-HT2A (Ki: 2.5 nM), and has antagonist activity ...
T14853 Cabergoline Cabergoline is an ergot derived-dopamine D2-like receptor agonist (Ki: 0.7, 1.5, and 1.2 for D2, D3, and 5-HT2B receptors).
T14968 Cinanserin hydrochloride Cinanserin hydrochloride is a selective and highly affinity 5-HT2 receptor antagonist (Ki: 41 nM). It has a much higher binding affinity for the 5-HT2 than for ...
T10837L Clocapramine Clocapramine is a D2 and 5-HT2A receptors antagonist.
T15026 Cyamemazine Cyamemazine, contains the phenothiazine chromophore, is a neuroleptic agent used as an anxiolytic. Cyamemazine is a potent 5-HT3 (Ki: 12 nM), 5-HT2A (Ki: 1.5 nM...
T15034 Roluperidone Roluperidone is a novel cyclic amide derivative. It has high equipotent affinities for 5-HT2A and sigma-2 receptors (Ki: 7.53 nM and 8.19 nM for 5-HT2A and sigm...
T15100 Desmethyl cariprazine Desmethyl cariprazine is a Cariprazine active metabolite. Cariprazine, an antipsychotic drug candidate, shows a high affinity for the D3 (Ki: 0.085 nM) and D2 (...
T15117 Didesmethyl cariprazine Cariprazine is an antipsychotic drug candidate. It shows high affinity for the D3 and D2 receptors, and moderate affinity for the 5-HT1A receptor. Didesmethyl c...
T15270 Fananserin Fananserin is an orally bioavailable and selective antagonist of the 5-HT2 receptor (Ki: 0.37 nM for the rat 5-HT2A receptor). It also is an antagonist of dopam...
T15414 GR 113808
T12806 (S)-Mirtazapine D3 (S)-Mirtazapine D3 is a deuterium labeled (S)-Mirtazapine. (S)-Mirtazapine is a stereoselective antagonist of 5-HT2 receptor. (S)-Mirtazapine is metabolized by ...
T12841 SB-224289 hydrochloride SB-224289 hydrochloride is a selective antagonist of 5-HT1B receptor, with anxiolytic effect.
T12859L SB 243213 dihydrochloride SB 243213 dihydrochloride is an orally active, selective and high-affinity antagonist of 5-hydroxytryptamine (5-HT)2C receptor(pKi of 9.37 and a pKb of 9.8 for ...
T12859 SB 243213 hydrochloride SB 243213 hydrochloride is an orally active, selective and high-affinity antagonist of 5-hydroxytryptamine (5-HT)2C receptor(pKi of 9.37 and a pKb of 9.8).It ha...
T12842 SB-269970 SB-269970 is a antagonist of 5-HT7 receptor(pKi of 8.3).
NPS ALX Compound 4a dihydrochloride
T12262LCAS 1781934-44-8
NPS ALX Compound 4a dihydrochloride is a potent and selective antagonist of 5-HT6 receptor (IC50 of 7.2 nM)
NPS ALX Compound 4a
T12262CAS 299433-10-6
NPS ALX Compound 4a is a potent and selective antagonist of 5-HT6 receptor (IC50 of 7.2 nM)
Pimethixene maleate
T12489LCAS 13187-06-9
Pimethixene maleate is a highly potent5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors antagonist(wi...
Pimethixene
T12489CAS 314-03-4
Pimethixene is a highly potent 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors antagonist(pKis of 7...
Pipamperone
T12480CAS 1893-33-0
Pipamperone is a high-affinity 5-HT2A receptor and D4 receptor antagonist (pKi of 8.2 and 8.0,respectively) .
PRX933 hydrochloride
T12565CAS 639029-42-8
PRX933 hydrochloride is an agonist of 5-HT2c receptor.
2-Methyl-5-HT
T10075CAS 78263-90-8
2-Methyl-5-HT (2-Methyl-5-hydroxytryptamine) is a potent and selective 5-HT3 receptor agonist with anti-depressive-like effects.
2-Methyl-5-HT hydrochloride
T10075L2CAS 845861-49-6
2-Methyl-5-HT hydrochloride (2-Methyl-5-hydroxytryptamine) is a potent and selective 5-HT3 receptor agonist with anti-depressive-like effects.
3-Hydroxy agomelatine
T10114CAS 166526-99-4
3-Hydroxy agomelatine is an Agomelatine metabolite and a 5-HT2C receptor antagonist (IC50: 3.2 μM; Ki: 1.8 μM).
3-Hydroxy agomelatine D3
T10113CAS 1079774-23-4
3-Hydroxy agomelatine D3 is a deuterium labeled 3-Hydroxy agomelatine. 3-Hydroxy agomelatine is an Agomelatine metabolite and a 5-HT2C receptor antagonist (IC50...
5-HT1A modulator 1
T10168CAS 142477-34-7
5-HT1A modulator 1 displays very high affinities for the 5HT1A, adrenergic α1, and dopamine D2 receptor (IC50s: 2 nM, 10 nM and 40 nM).
5-HT2A antagonist 1
T10498CAS 204643-75-4
5-HT2A antagonist 1 is a 5-HT2A antagonist extracted from patent US5728835A and JP 1007727. It may be useful in the treatment of gastrointestinal disorders circ...
5-HT3 antagonist 3
T10162CAS 120635-47-4
5-HT3 antagonist 3 (Compound 15b) is a high-affinity 5-HT3 receptor antagonist. It binds to 5-HT3 receptors in rat brain cortical membranes (Ki: 0.25 nM).
5-HT3-In-1
T10006CAS 186348-68-5
5-HT3-In-1 (compound example 8) is extracted from patent EP0748807A1 with 5-HT3 inhibition activity.
5-HT4 antagonist 1
T10169CAS 261766-73-8
5-HT4 antagonist 1 is a 5-HT4 receptor antagonist (pKi: 9.6).
5HT6-ligand-1
T10053CAS 1038988-11-2
5HT6-ligand-1 is a potent 5-HT6 receptor ligand (Ki: 1.43 nM).
5-HT7 agonist 1
T10170CAS 334974-31-1
5-HT7 agonist 1 is a selective 5-HT7 receptor agonist (IC50: 222.93 nM), which can be used for the 5-HT7 receptor-related disease, such as CNS disorders.
7-Desmethyl-3-hydroxyagomelatine
T10192CAS 166527-00-0
7-Desmethyl-3-hydroxyagomelatine is a metabolite of Agomelatine and has less activity than Agomelatine. Agomelatine is a melatonergic (MT1 and MT2) agonist and ...
Dehydroaripiprazole
T10989CAS 129722-25-4
Dehydroaripiprazole (OPC-14857) is the active metabolite of aripiprazole. Aripiprazole is an antipsychotic drug, which is metabolized by CYP3A4 and CYP2D6 and m...
Deramciclane
T10996CAS 120444-71-5
Deramciclane has high affinity for 5-HT2A and 5-HT2C receptors. It acts as an antagonist in both receptor subtypes and has inverse agonist properties for 5-HT2C...
Donitriptan
T11075CAS 170912-52-4
Donitriptan is an effective agonist for the 5-HT1B/1D receptor, with pKis of 9.4 and 9.3, respectively.
2-Methyl-5-HT maleate
T10075LCAS 78263-91-9
2-Methyl-5-HT maleate (2-Methyl-5-hydroxytryptamine maleate) is a potent and selective 5-HT3 receptor agonist, which is shown to display anti-depressive-like ef...
PU-02
T8445CAS 313984-77-9
PU-02 is a potent and selective antagonist of 5-HT3 receptor.
4i
T8438CAS 930478-88-9
4i is a 5-HT3 receptor antagonist,It modulates the serotonergic system.
Alniditan
T14190CAS 152317-89-0
Alniditan is a receptors agonist of 5-HT1B/1D in HEK 293 cells (IC50: 1.7 and 1.3 nM). For 5-HT1B/1D receptors, the pKi values are 8.96 and 9.40, respectively...
Bemesetron
T14526CAS 40796-97-2
Bemesetron (MDL 72222) is an antagonist of 5-HT3 receptor (IC50: nM). It has Neuroprotective effect[2].
(R)-Mirtazapine D3
T12631CAS
(R)-Mirtazapine D3 is a deuterium labeled (R)-Mirtazapine.(R)-Mirtazapine is a antagonist of 5-HT3 receptor.
(R)-Mirtazapine
T12632CAS 61364-37-2
(R)-Mirtazapine is a R(−)-enantiomer of Mirtazapine with antinociceptive properties in an animal model of acute thermal nociception. (R)-Mirtazapine is a anta...
(R)-Praziquantel D11
T12638CAS 1399880-38-6
(R)-Praziquantel D11 is the deuterium labeled (R)-Praziquantel. (R)-Praziquantel is the active enantiomer of Praziquantel, is a partial the human 5-HT2B recepto...
RG-12915
T12716CAS 136174-04-4
RG-12915 is a selective antagonist of 5-HT3(IC50 value of 0.16 nM).
Agomelatine (L(+)-Tartaric acid)
T10267CAS 824393-18-2
Agomelatine (S-20098) L(+)-Tartaric acid is a specific agonist of MT1 and MT2 receptors (Kis: 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and...
AM9405
T10294CAS
AM9405 is a novel peripherally active cannabinoid type 1 (CB1) and serotonin type 3 receptor agonist. It inhibits twitch contraction of the ileum and the colon ...
AP521
T10344CAS 151227-08-6
AP521 is an agonist of the human 5-HT1A receptor (IC50: 94 nM).
Arotinolol
T10371CAS 68377-92-4
Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker. Arotinolol also shows potency for inhibiting the binding of the ra...
AS19
T10380CAS 1000578-26-6
AS19 is a potent, selective 5-HT7 receptor agonist (IC50: 0.83 nM; Ki: 0.6 nM). AS19 is selective for 5-HT7 over 5-HT1A, 5-HT1B, 5-HT1D, and 5-HT5A receptors (K...
Brilaroxazine
T14782CAS 1239729-06-6
Brilaroxazine (RP5603) is a partial agonist of dopamine (DA) D2, D3, and D4 receptors, 5-HT1A (Ki: 1.5 nM) and 5-HT2A (Ki: 2.5 nM), and has antagonist activity ...
Cabergoline
T14853CAS 81409-90-7
Cabergoline is an ergot derived-dopamine D2-like receptor agonist (Ki: 0.7, 1.5, and 1.2 for D2, D3, and 5-HT2B receptors).
Cinanserin hydrochloride
T14968CAS 54-84-2
Cinanserin hydrochloride is a selective and highly affinity 5-HT2 receptor antagonist (Ki: 41 nM). It has a much higher binding affinity for the 5-HT2 than for ...
Clocapramine
T10837LCAS 47739-98-0
Clocapramine is a D2 and 5-HT2A receptors antagonist.
Cyamemazine
T15026CAS 3546-03-0
Cyamemazine, contains the phenothiazine chromophore, is a neuroleptic agent used as an anxiolytic. Cyamemazine is a potent 5-HT3 (Ki: 12 nM), 5-HT2A (Ki: 1.5 nM...
Roluperidone
T15034CAS 359625-79-9
Roluperidone is a novel cyclic amide derivative. It has high equipotent affinities for 5-HT2A and sigma-2 receptors (Ki: 7.53 nM and 8.19 nM for 5-HT2A and sigm...
Desmethyl cariprazine
T15100CAS 839712-15-1
Desmethyl cariprazine is a Cariprazine active metabolite. Cariprazine, an antipsychotic drug candidate, shows a high affinity for the D3 (Ki: 0.085 nM) and D2 (...
Didesmethyl cariprazine
T15117CAS 839712-25-3
Cariprazine is an antipsychotic drug candidate. It shows high affinity for the D3 and D2 receptors, and moderate affinity for the 5-HT1A receptor. Didesmethyl c...
Fananserin
T15270CAS 127625-29-0
Fananserin is an orally bioavailable and selective antagonist of the 5-HT2 receptor (Ki: 0.37 nM for the rat 5-HT2A receptor). It also is an antagonist of dopam...
GR 113808
T15414CAS 144625-51-4
(S)-Mirtazapine D3
T12806CAS
(S)-Mirtazapine D3 is a deuterium labeled (S)-Mirtazapine. (S)-Mirtazapine is a stereoselective antagonist of 5-HT2 receptor. (S)-Mirtazapine is metabolized by ...
SB-224289 hydrochloride
T12841CAS 180084-26-8
SB-224289 hydrochloride is a selective antagonist of 5-HT1B receptor, with anxiolytic effect.
SB 243213 dihydrochloride
T12859LCAS 1780372-25-9
SB 243213 dihydrochloride is an orally active, selective and high-affinity antagonist of 5-hydroxytryptamine (5-HT)2C receptor(pKi of 9.37 and a pKb of 9.8 for ...
SB 243213 hydrochloride
T12859CAS 200940-23-4
SB 243213 hydrochloride is an orally active, selective and high-affinity antagonist of 5-hydroxytryptamine (5-HT)2C receptor(pKi of 9.37 and a pKb of 9.8).It ha...
SB-269970
T12842CAS 201038-74-6
SB-269970 is a antagonist of 5-HT7 receptor(pKi of 8.3).