5-ht1a receptor

Didesmethyl cariprazine, a metabolite of Cariprazine, is the major cyclic active part. Didesmethyl cariprazine has a long half-life of 1-3 weeks. Cariprazine is a potent D3 preference D3/D2 receptor partial agonist of dopamine for the treatment of schizophrenia, bipolar mania, and depression, with a high affinity for d3 and d2 receptors and a moderate affinity for 5-HT 1A receptors.

AP521 is an agonist of the human 5-HT1A receptor (IC50: 94 nM).

AS19 is a potent, selective 5-HT7 receptor agonist (IC50: 0.83 nM; Ki: 0.6 nM) with demonstrated selectivity for 5-HT7 over 5-HT1A, 5-HT1B, 5-HT1D, and 5-HT5A receptors (Kis: 89.7 nM, 490 nM, 6.6 nM, and 98.5 nM, respectively).

Bifeprunox is a potent partial agonist of dopamine D2-like and 5-HT1A receptor (pEC50: 6.37 for hippocampus 5-HT1A; pKis: 7.19 and 8.83 for cortex 5-HT1A and striatum D2). It is an antipsychotic for the research of schizophrenia.

Cariprazine-D6 is a deuterium-labeled Cariprazine. Cariprazine (T4577) is an antipsychotic agent (D3 receptors, Ki: 0.085 nM; D2 receptors, Ki: 0.49 nM).

Dehydroaripiprazole (DM-14857) is the active metabolite of aripiprazole. Aripiprazole is an antipsychotic drug, which is metabolized by CYP3A4 and CYP2D6 and mainly forms dehydroaripiprazole. Dehydroaripiprazole has antipsychotic activity equivalent to aripiprazole.

Lesopitron dihydrochloride with IC50 of 125 nM in rat hippocampal membranes, is a full and selective 5-HT1A receptor agonist.

Pimethixene (Calmixen) 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 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively).

Pimethixene maleate (Pimetixene maleate) is a potent 5-HT2B receptor antagonist with sedative and antitussive activity.Pimethixene maleate inhibits 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2, and can be used in studies of dry and irritant cough in children. irritant cough in children.

SEP-363856 is an agent of orally active and CNS active psychotropic with a unique, non-D2/5-HT2A mechanism of action, exerts its antipsychotic-like effects, has the potential to treatment of schizophrenia.

SEP-363856 hydrochloride (SEP-856 hydrochloride) is an orally active, CNS-active psychotropic agent with a unique non-D2/5-HT2A mechanism of action, demonstrating antipsychotic-like effects and potential for schizophrenia treatment.

Brilaroxazine (RP5063) is a potent multimodal dopamine/5-HT modulator. Brilaroxazine is a partial agonist of dopamine D2, D3, and D4 receptors, 5-HT1A (Ki =1.5 nM) and 5-HT2A (Ki = 2.5 nM), and has antagonist activity 5-HT2B, and 5-HT7 receptors with Kis of 0.19 nM and 2.7 nM, respectively. Brilaroxazine can be used for research about cognitive impairments in neuropsychiatric and neurological diseases.

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 (Ki: 0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (2.6 nM).

GR 113808 is a selective 5-HT4 receptor antagonist that inhibits 5-HT1B, 5-HT2A, 5-HT2C, and 5-HT3 receptors, and attenuates dopamine release.

p-MPPI hydrochloride is a selective 5-HT1A receptor antagonist with antidepressant and anxiolytic-like effects.

Flesinoxan, a hypotensive agent, is an effective, high-affinity, and selective 5-hydroxytryptamine1A receptor agonist (EC50: 24 nM).

Buspirone (Buspirone free base) is an azaspiro compound which has a role as an anxiolytic drug, a sedative, a serotonergic agonist and an EC 3.4.21.26 (prolyl oligopeptidase) inhibitor.

Buspirone hydrochloride (Buspar) is a 5HT(1A) receptor agonist, used to treat generalized anxiety disorder (GAD).

BMY 7378 dihydrochloride (BMY7378 HCl) , α1D-adrenergic receptor antagonist, is a weak partial agonist/antagonist of 5-HT1A receptor.

RS102895 hydrochloride is a potent antagonist of CCR2(IC50 of 360 nM).

Adoprazine (SLV313) is a potential atypical antipsychotic bearing potent D2 receptor antagonist and 5-HT1A receptor agonist properties.

Fiduxosin is a selective and potent α1-adrenoceptor antagonist with inhibitory effects on α1a-adrenoceptor, α1b-adrenoceptor and α1d-adrenoceptor, with Ki values of 0.160 nM, 24.9 nM and 0.920 nM, respectively. Fiduxosin can be used for the treatment of benign prostatic hyperplasia.

Pradigastat (LCQ-908) is an orally active, potent and selective diacylglycerol acyltransferase 1 (DGAT1) inhibitor for the treatment of constipation, which may be used in the study of obesity and diabetes.

Naluzotan(PRX 00023) is a novel and potent 5-HT1A agonist with IC50 and Ki values of approximately 20 nM and 5.1 nM, respectively.Naluzotan is a potent hERG K+ channel blocker with an IC50 value of 3800 nM.Naluzotan exhibits anxiolytic activity and can be used to study depression.