For research use only.
Catalog No.S4639 Synonyms: OPC-34712
CAS No. 913611-97-9
Brexpiprazole (OPC-34712) is a novel D2 dopamine and serotonin 1A partial agonist, called serotonin-dopamine activity modulator (SDAM), and a potent antagonist of serotonin 2A receptors, noradrenergic alpha 1B and 2C receptors with Ki values of 0.3, 0.12, 0.47, 0.17 and 0.59 nM for D2L, 5-HT1A, 5-HT2A, α1B receptors and α2C receptors respectivey.
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|Description||Brexpiprazole (OPC-34712) is a novel D2 dopamine and serotonin 1A partial agonist, called serotonin-dopamine activity modulator (SDAM), and a potent antagonist of serotonin 2A receptors, noradrenergic alpha 1B and 2C receptors with Ki values of 0.3, 0.12, 0.47, 0.17 and 0.59 nM for D2L, 5-HT1A, 5-HT2A, α1B receptors and α2C receptors respectivey.|
Brexpiprazole is a potent partial agonist at human 5-hydroxytryptamine (5-HT) 5-HT1A (Ki=0.12 nM) and dopamine D2L (Ki=0.3 nM) receptors, and an antagonist at 5-HT2A receptors (Ki=0.47 nM). It also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2Creceptors (Ki=0.59 nM). Furthermore, this drug displays moderate affinity for human D3, 5-HT2B and 5-HT7 receptors, as well as α1A, and α1D adrenergic receptors. Brexpiprazole potentiated NGF-induced neurite outgrowth in PC12 cells. It could significantly potentiate the effects of fluoxetine (or paroxetine) on neurite outgrowth.
|In vivo||Brexpiprazole is able to ameliorate PCP- 191 induced cognitive deficits in mice, via 5-HT1A receptors.|
|In vitro||DMSO||24 mg/mL (55.35 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03734354||Completed||Drug: Brexpiprazole||Health||Otsuka Beijing Research Institute||April 7 2019||Phase 1|
|NCT02875080||Completed||Drug: OPC-34712||Healthy Adult Male||Otsuka Pharmaceutical Co. Ltd.||September 27 2016||Phase 1|
|NCT00905307||Completed||Drug: OPC-34712|Drug: Placebo|Drug: Aripiprazole||Schizophrenia||Otsuka Pharmaceutical Development & Commercialization Inc.||July 2009||Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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