GPCR / G Protein

 
 
7-TM Receptors Products 7-TM Receptors New Products Compare Solubility


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Catalog No. Product Name Application Product Information
A14026

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.
A15838

GSK163090

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.
A14163

WAY 181187

5-HT6 agonist
WAY 181187 is a high affinity and selective 5-HT6 agonist with Ki value of 2.2 nM.
A13664

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.
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.
A15438

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.
A15501

Lerisetron

5HT3 receptor antagonist
Lerisetron is a serotonin type 3 (5-HT3) receptor antagonist with antiemetic activity.
A15500

LY278584

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
A15096

Granisetron

5-HT3 antagonist
Granisetron is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.
A15148

LY 344864

5HT1F agonist
LY344864 is a selective receptor agonist with an affinity of 6 nM (Ki) at the recently cloned 5-HT1F receptor.
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.
A15542

Piboserod

5-HT4 receptor antagonist
Piboserod is a selective 5-HT(4) receptor antagonist.
A15499

Ricasetron

5-HT3 receptor antagonist
Ricasetron is a drug which acts as a selective antagonist at the serotonin 5-HT3 receptor.
A14091

Bifeprunox Mesylate

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

SB-742457

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).
A14255

Cyclobenzaprine HCl

5-HT2 receptor antagonist
Cyclobenzaprine HCl is a muscle relaxant by blocking pain sensations.
A14391

Levomilnacipran HCl

serotonin/NE reuptake inhibitor
Levomilnacipran HCl is a selective serotonin and norepinephrine reuptake inhibitor.
A14356

LuAE58054

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.
A14375

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.
A14198

Lasmiditan

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.
A13293 SALE

Tandospirone

5-HT Receptor antagonist
Tandospirone is a partial agonist at 5HT1A receptors. It significantly reduces haloperidol-induced bradykinesia in a dose-dependent manner.
A13267

PRX-08066

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.
A11824

Blonanserin

D2/5-HT2 receptor antagonist
Blonanserin is a D2/5-HT2 receptor antagonist; atypical antipsychotic.
A12598 SALE

lorcaserin hydrochloride (APD-356)

serotonin 2C receptor agonist
lorcaserin hydrochloride (APD-356) is a serotonin 2C receptor agonist indicated as an adjunct to a reduced-calorie diet and increased physical activity for chronic weight management in adults
A13092

NAD 299 hydrochloride (Robalzotan)

5-HT1A receptor antagonist
NAD 299 hydrochloride (Robalzotan) is a selective, high affinity 5-HT1A receptor antagonist (Ki = 0.6 nM in vitro).
A13833

RU 24969 hemisuccinate

5-HT1A/1B and 5-HT2C agonist
RU 24969 hemisuccinate is a potent 5-HT1A/1B and moderate 5-HT2C agonist that may also release 5-HT.
A13767

Tropanserin

5-HT3 receptor antagonist
Tropanserin acts as a potent and selective 5-HT3 receptor antagonist.
A13766

SDZ 205-557 HCl

5-HT4 Receptor Antagonist
SDZ 205-557 is a potent, selective 5-HT4 serotonin receptor antagonist.
A13762 SALE

N-Desmethylclozapine

5-HT2C serotonin receptor antagonist
N-Desmethylclozapine is a potent and selective 5-HT2C serotonin receptor antagonist
A13757

PU 02

5-HT3 Receptor Modulator
PU 02 is a negative allosteric modulator of 5-HT3 receptors.
A12521

Lu AE58054 (Idalopirdine)

5-HT6R antagonist
Lu AE58054 is a potent and selective 5-HT6 receptor antagonist.
A13860 SALE

Flibanserin

-
Flibanserin is a new drug being investigated for the prevention of HSDD in woman.
A13865

Edivoxetine HCl

norepinephrine reuptake inhibitor
Edivoxetine HCl is a drug which acts as a selective norepinephrine reuptake inhibitor
A13501

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).
A11538

Pardoprunox HCl (SLV-308)

-
Pardoprunox is an antiparkinsonian drug currently under development by Solvay for the treatment of Parkinson's disease.
A15923 SALE

Eptapirone

5HT(1A) receptor agonist
Eptapirone is a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential.
A15884

Pimavanserin

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.
A16169

Cyproheptadine hydrochloride

serotonin/histamine2 antagonist
Cyproheptadine hydrochloride sesquihydrate is an antihistamine and is an antagonist of serotonin and histamine2.
A16337

YL-0919

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.
A15592

BRL-54443

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.
A15687

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.
A16404

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.
A11598

Tianeptine

-
Tianeptine is a selective facilitator of 5-HT uptake in vitro and in vivo.
A15491

Desvenlafaxine succinate hydrate

serotonin (5-HT)/norepinephrine (NE) reuptake inhibitor
Desvenlafaxine succinate hydrate is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI).
A13458

Norfluoxetine

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).
A13417

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.
A13424

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.
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.
A15216

Quetiapine

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

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