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5-HT Receptors

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Catalog No. Product Name Application Product Information


5-HT1A/B/D receptor antagonist
GSK163090 is a potent, selective, and orally active 5-HT1A/B/D receptor antagonist with pKi of 9.4/8.5/9.7, and 6.3/6.7 for 5-HT1A/B/D, and dopamine D2/D3, respectively.

SB271046 HCl

5-HT Receptor Antagonist
SB271046 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.


5HT3 receptor antagonist
Lerisetron is a serotonin type 3 (5-HT3) receptor antagonist with antiemetic activity.


5-HT3 antagonist
LY278584 is a potent and selective antagonist of 5-HT3 receptors. LY278584 is a useful ligand for studying the localization of 5-HT3 receptors in rat brain


5-HT3 receptor antagonist
Ricasetron is a drug which acts as a selective antagonist at the serotonin 5-HT3 receptor.

Ketanserin tartrate

5HT2A antagonist
Ketanserin tartrate is a salt of Ketanserin. Ketanserin is reported to have a high affinity for multiple G protein-coupled receptors, such as serotonin receptors.


5-HT4 receptor antagonist
Piboserod is a selective 5-HT(4) receptor antagonist.
A15282 SALE

WAY-100635 maleate salt

5HT1A antagonist
WAY-100635 maleate is a potent and selective 5-hydroxytryptamine1A antagonist with an IC50 of 0.95 - 0.12 nM for 5-HT.

LY 344864

5HT1F agonist
LY344864 is a selective receptor agonist with an affinity of 6 nM (Ki) at the recently cloned 5-HT1F receptor.


5-HT3 antagonist
Granisetron is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.

SB 258585 HCl

5-HT6 serotonin receptor antagonist
SB 258585 hydrochloride has been found to be a selective and potent SR-6 antagonist. This compound displays more than a 160-fold selectivity over other serotonin receptor subtypes.
A14434 SALE

Pimavanserin (ACP-103)

5-HT2A receptor agonist
Pimavanserin is a potent and selective 5-HT2A receptor inverse agonist with mean pIC50 of with 8.7 in the cell-based functional assay.

WAY 181187

5-HT6 agonist
WAY 181187 is a high affinity and selective 5-HT6 agonist with Ki value of 2.2 nM.


5-HT6 receptor antagonist
LuAE58054 is a potent and selective 5-HT6 receptor antagonist under development by Lundbeck as an augmentation therapy for the treatment of cognitive deficits associated with Alzheimer's disease and schizophrenia.

S 32212 HCl

5-HT2C agonist
S 32212 hydrochloride is an inverse agonist of 5-HT2C receptors (pKi = 8.18 at human 5-HT2C INI receptors).

PU 02

5-HT3 Receptor Modulator
PU 02 is a negative allosteric modulator of 5-HT3 receptors.

Lu AE58054 (Idalopirdine)

5-HT6R antagonist
Lu AE58054 is a potent and selective 5-HT6 receptor antagonist.


D2/5-HT2 receptor antagonist
Blonanserin is a D2/5-HT2 receptor antagonist; atypical antipsychotic.

Edivoxetine HCl

norepinephrine reuptake inhibitor
Edivoxetine HCl is a drug which acts as a selective norepinephrine reuptake inhibitor


5-HT2B receptor antagonist
PRX-08066, a Novel 5-Hydroxytryptamine Receptor 2B Antagonist, reduced monocrotaline-induced pulmonary arterial hypertension and right ventricular hypertrophy in rats.
A13860 SALE


Flibanserin is a new drug being investigated for the prevention of HSDD in woman.


5-HT1F receptor agonist
Lasmiditan is is a high-affinity, highly selective 5-HT1F receptor agonist (Ki=2.1 nM), compared with Ki of 1043 nM and 1357 nM at the 5-HT(1B) and 5-HT(1D) receptors, respectively.

Tropisetron HCL

5-HT3 receptor antagonist
Tropisetron is a selective 5-HT3 receptor antagonist and ??7-nicotinic receptor agonist with an IC50 of 70.1 ?? 0.9 nM for 5-HT3 receptor.
A13293 SALE


5-HT Receptor antagonist
Tandospirone is a partial agonist at 5HT1A receptors. It significantly reduces haloperidol-induced bradykinesia in a dose-dependent manner.

Bifeprunox Mesylate

Bifeprunox Mesylate is an antipsychotic compound through activation of the serotonin 5-hydroxytryptamine (5-HT)1A receptor.
A14092 SALE


5-HT6 receptor antagonist
SB-742457 is a selective 5-HT6 receptor antagonist with cognition, memory, and learning-enhancing effects.
A14102 SALE

SB 399885 HCl

5-HT6 antagonist
SB 399885 hydrochloride is a potent, brain penetrant, and orally active SR-6 antagonist. It displays > 200-fold selectivity for SR-6 over other serotonin receptors (pKi values are 9.11, 8.81 and 9.02 for human recombinant, native rat and native human SR-6 receptors, respectively).

Cyclobenzaprine HCl

5-HT2 receptor antagonist
Cyclobenzaprine HCl is a muscle relaxant by blocking pain sensations.

Levomilnacipran HCl

serotonin/NE reuptake inhibitor
Levomilnacipran HCl is a selective serotonin and norepinephrine reuptake inhibitor.


serotonin uptake inhibitor
Norfluoxetine is an active metabolite of the antidepressant fluoxetine that inhibits serotonin uptake with a pKi value of 7.35.1 The S-enantiomer of norfluoxetine has 20-times higher serotonin reuptake blocking potency than the R-enantiomer (pKis = 7.86 versus 6.51, respectively).

NAN-190 hydrobromide

5-HT1A receptor antagonist
NAN-190 is a drug and research chemical widely used in scientific studies. It was previously believed to act as a selective 5-HT1A receptor antagonist, but a subsequent discovery showed that it also potently blocks the α2-adrenergic receptor.

Buspirone HCl

5HT(1A) receptor agonist
Buspirone is a serotonergic (5HT(1A) receptor agonist) anxiolytic drug with some D(2) dopaminergic effect, used for anxiety disorders.


5-HT1E/5-HT1F receptor agonist
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.


5-HT1A receptor agonist/serotonin reuptake inhibitor
YL0919, a novel antidepressant candidate with dual activity as a 5-HT1A receptor agonist and a selective serotonin reuptake inhibitor,the IC50 values of YL-0919 inhibiting the uptake of 5-HT into rat cerebral cortical synaptosomes and human recombinant cells were 1.78??0.34 nM and 1.93??0.18 nM respectively.

Cyproheptadine hydrochloride

serotonin/histamine2 antagonist
Cyproheptadine hydrochloride sesquihydrate is an antihistamine and is an antagonist of serotonin and histamine2.

Azasetron HCl

5-HT3 receptor antagonist
Azasetron HCl 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.


Serotonin2A Receptor Inverse Agonist
Pimavanserin is a potent and selective serotonin 5-HT2A inverse agonist with pIC50 of 8.73, used to treat psychosis associated with Parkinson??s disease.
A15923 SALE


5HT(1A) receptor agonist
Eptapirone is a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential.

Pardoprunox HCl (SLV-308)

Pardoprunox is an antiparkinsonian drug currently under development by Solvay for the treatment of Parkinson's disease.


Tianeptine is a selective facilitator of 5-HT uptake in vitro and in vivo.


Quetiapine is an atypical antipsychotic used in the treatment of schizophrenia, bipolar I mania, bipolar II depression, bipolar I depression.

Asenapine HCl

adrenergic receptor/5-HT receptor inhibitor
Asenapine hydrochloride inhibits adrenergic receptor (α1, α2A, α2B, α2C) with Ki of 0.25-1.2 nM and also inhibits 5-HT receptor (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) with Ki of 0.03-4.0 nM.

Alosetron Hydrochloride

5HT3-receptor antagonist
Alosetron is s Serotonin 5HT3-receptor antagonist that is used in treatment of irritable bowel syndrome.
A15286 SALE


5-HT/dopamine receptor antagonist
Ziprasidone is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity.

Desvenlafaxine succinate hydrate

serotonin (5-HT)/norepinephrine (NE) reuptake inhibitor
Desvenlafaxine succinate hydrate is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI).
A15048 SALE

Clozapine N-oxide

5-HT1C receptor antagonist
Clozapine N-oxide is a major metabolite of Clozapine noted to decrease SR-2A (5-HT2 serotonin receptor) density in vitro.

Atomoxetine HCl

norepinephrine (NE) transporter inhibitor
Atomoxetine hydrochloride is a competitive and specific inhibitor of SLC6A2 while demonstrating weak ST and DAT inhibition as studied in synaptosomes of rat hypothalamus.

Amitriptyline HCl

Amitriptyline inhibits serotonin receptor, norepinephrine receptor, 5-HT4, 5-HT2 and sigma 1 receptor with IC50 of 3.45 nM, 13.3 nM, 7.31 nM, 235 nM and 287 nM, respectively.
A10607 SALE

Mosapride citrate

5-HT4-receptor agonist
Mosapride citrate acts as 5-HT4 receptor agonist and 5-HT3 receptor antagonist.


Serotonin reuptake inhibitor
Vilazodone acts as a serotonin reuptake inhibitor (IC50 = 0.5 nM) and 5-HT1A receptor partial agonist (IC50 = 0.2 nM; IA = ~60-70%).

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