| Identification | Back Directory | [Name]
Brexpiprazole dihydrochloride | [CAS]
913612-38-1 | [Synonyms]
Brexpiprazole HCl
OPC 34712 dihydrochloride
Brexpiprazole dihydrochloride
antipsychotic,OPC34712,OPC-34712,Serotonin Receptor,5-hydroxytryptamine Receptor,Brexpiprazole,recognition deficits,Dopamine Receptor,Beta Receptor,neurite outgrowth,Adrenergic Receptor,Brexpiprazole HCl,PC12,5-HT Receptor,Inhibitor,OPC 34712,orally active,inhibit | [Molecular Formula]
C25H28ClN3O2S | [MDL Number]
MFCD29059914 | [MOL File]
913612-38-1.mol | [Molecular Weight]
470.03 |
| Hazard Information | Back Directory | [Uses]
Brexpiprazole (OPC-34712) hydrochloride, 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 hydrochloride is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole hydrochloride also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM)[1][2]. | [in vivo]
Brexpiprazole (0-0.1 mg/kg; p.o.; once) improves social recognition deficits in mice[2]. | Animal Model: | Male C57BL/6NCrSlc mice, Dizocilpine (0.1 mg/kg) (HY-15084B) induced social recognition deficits[2] | | Dosage: | 0.01, 0.03 and 0.1 mg/kg | | Administration: | Oral administration, once | | Result: | Significantly ameliorated Dizocilpine-induced social recognition deficits, without sedation or a reduction of exploratory behavior. |
| [IC 50]
5-HT1A Receptor: 0.12 nM (Ki); 5-HT2A Receptor: 0.47 nM (Ki); D2L Receptor: 0.3 nM (Ki); human noradrenergic α1B: 0.17 nM (Ki); human noradrenergic α2C: 0.59 nM (Ki) | [References]
[1] 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. DOI:10.1016/j.euroneuro.2015.01.014
[2] 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. DOI:10.1016/j.euroneuro.2014.12.014 |
|
| Company Name: |
BOC Sciences
|
| Tel: |
16314854226 |
| Website: |
www.bocsci.com |
|