Brexpiprazole dihydrochloride

Modify Date: 2024-01-03 11:58:28

Brexpiprazole dihydrochloride Structure
Brexpiprazole dihydrochloride structure
Common Name Brexpiprazole dihydrochloride
CAS Number 913612-38-1 Molecular Weight N/A
Density N/A Boiling Point N/A
Molecular Formula N/A Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Brexpiprazole dihydrochloride


Brexpiprazole (OPC-34712) hydrochloride, an atypical orally active antipsychotic drug, 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].

 Names

Name Brexpiprazole dihydrochloride

 Brexpiprazole dihydrochloride Biological Activity

Description Brexpiprazole (OPC-34712) hydrochloride, an atypical orally active antipsychotic drug, 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].
Related Catalog
Target

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)

In Vitro Brexpiprazole (0-1.0 μM, 4 days) potentiates NGF-induced neurite outgrowth in a dose-dependent manner in PC12 cells[1].
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.
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.

[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.

 Chemical & Physical Properties

No Any Chemical & Physical Properties