1427049-19-1
Chemical Structure
Brexpiprazole-d8-1
Synonym(s): OPC-34712-d8-1
- CAS No.: 1427049-19-1
- Formula:C25H19D8N3O2S
- Molecular Weight:441.62
IUPAC Name: 7-(4-(4-(benzo[b]thiophen-4-yl)piperazin-1-yl)butoxy-1,1,2,2,3,3,4,4-d8)quinolin-2(1H)-one
InChIKey: ZKIAIYBUSXZPLP-IGZDHSKUSA-N
SMILES: O=C1C=CC2=CC=C(C=C2N1)OC([2H])([2H])C([2H])([2H])C([2H])([2H])C([2H])([2H])N3CCN(CC3)C4=C5C(SC=C5)=CC=C4
Biological Activity: Brexpiprazole-d8-1 (OPC-34712-d8-1) is the deuterium labeled Brexpiprazole (HY-15780)[1]. Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM)[2][3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
Brexpiprazole-d8-1 | 96.48% | Brexpiprazole-d8-1 (OPC-34712-d8-1) is the deuterium labeled Brexpiprazole (HY-15780). Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM). | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
Brexpiprazole (Standard) | 99.59% | Brexpiprazole (Standard) is the analytical standard of Brexpiprazole. This product is intended for research and analytical applications. Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM). | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
Brexpiprazole-d8 | 99.0% | Brexpiprazole-d8 (OPC-34712-d8) is the deuterium labeled Brexpiprazole (HY-15780). Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM). | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
Brexpiprazole-d8 (hydrochloride) | Brexpiprazole-d8 (hydrochloride) is the deuterium labeled Brexpiprazole hydrochloride. | |||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
Brexpiprazole | 99.80% | Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM). | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
- [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. [Content Brief]
- [2]. Ishima T, et al. Potentiation of neurite outgrowth by brexpiprazole, a novel serotonin-dopamine activity modulator: a role for serotonin 5-HT1A and 5-HT2A receptors. Eur Neuropsychopharmacol. 2015 Apr;25(4):505-11. [Content Brief]
- [3]. Yoshimi N, et al. Improvement of dizocilpine-induced social recognition deficits in mice by brexpiprazole, a novel serotonin-dopamine activity modulator. Eur Neuropsychopharmacol. 2015 Mar;25(3):356-64. [Content Brief]
