Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Brexpiprazole (OPC-34712) is a partial agonist of human 5-hydroxytryptamine (5-HT) 5-HT1A and dopamine D2 receptors.
説明 | Brexpiprazole (OPC-34712) is a partial agonist of human 5-hydroxytryptamine (5-HT) 5-HT1A and dopamine D2 receptors. |
ターゲット&IC50 | D2L:0.3 nM(Ki), 5-HT1A:0.12 nM(Ki), Noradrenaline α1B (human):0.17 nM(Ki), 5-HT2A receptor:0.47 nM(Ki), α2C-adrenoceptor:0.59 nM(Ki) |
In vitro | 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[1]. |
In vivo | Brexpiprazole is able to ameliorate PCP- 191 induced cognitive deficits in mice, via 5-HT1A receptors[2]. |
細胞研究 | 2.5 ng/ml of NGF(nerve growth factor) is used to study the potentiating effects of brexpiprazole on neurite outgrowth. Twenty-four hours after plating, the medium is replaced with DMEM medium containing 0.5% FBS and 1% penicillin-streptomycin with NGF (2.5 ng/ml), with or without brexpiprazole (0.001, 0.01, 0.1 or 1.0 μM). Four days after incubation with NGF (2.5 ng/ml) with or without drugs, morphometric analysis is performed on digitized images of live cells taken under phase-contrast illumination, with an inverted microscope linked to a camera. (Only for Reference) |
別名 | OPC-34712 |
分子量 | 433.57 |
分子式 | C25H27N3O2S |
CAS No. | 913611-97-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 23 mg/mL (53 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
You can also refer to dose conversion for different animals. 詳細
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
Brexpiprazole 913611-97-9 GPCR/G Protein Neuroscience Adrenergic Receptor Dopamine Receptor 5-HT Receptor Serotonin Receptor Beta Receptor PC12 OPC-34712 5-hydroxytryptamine Receptor Inhibitor recognition deficits OPC34712 OPC 34712 antipsychotic orally active inhibit neurite outgrowth inhibitor