依匹哌唑 T2306

Product Introduction
Bioactivity


英文名: Brexpiprazole

描述: Brexpiprazole (OPC-34712) 是人5-HT1A 和多巴胺受体的部分激动剂，Ki 分别为0.12 和 0.3 nM。它也是5-HT2A 受体的拮抗剂，Ki 为 0.47 nM，可作为非典型抗精神病药。

细胞实验: 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)

体外活性: 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].

体内活性: Brexpiprazole is able to ameliorate PCP- 191 induced cognitive deficits in mice, via 5-HT1A receptors[2].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 23 mg/mL (53 mM)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)


关键字: Dopamine Receptor | 5-HT Receptor | Serotonin Receptor | Beta Receptor | PC12 | 5-hydroxytryptamine Receptor | Inhibitor | Adrenergic Receptor | recognition deficits | OPC34712 | OPC 34712 | antipsychotic | orally active | inhibit | neurite outgrowth | Brexpiprazole

相关产品: Brexpiprazole S-oxide D8 | Tedatioxetine hydrobromide | Dihydrexidine | Syrosingopine | D3R/MOR antagonist 2 | Timiperone | GR 103691 | L-745870 trihydrochloride | 5-HT1A modulator 1 | Tolnapersine

相关库: Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | Angiogenesis related Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | GPCR Compound Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | EMA Approved Drug Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途