化合物A-381393 T5397

Product Introduction
Bioactivity


英文名: A-381393

描述: A-381393 是选择性、可透过血脑屏障的多巴胺 D4受体拮抗剂，对人多巴胺 D4.4，D4.2和 D4.7受体的 Ki 分别为 1.5，1.9 和 1.6 nM，选择性是对 D1，D2，D3，D5多巴胺受体的 2700 多倍，对 5-HT2A 的选择性适中，Ki=370 nM。

体外活性: A-381393 potently bound to the membrane from cells expressing recombinant human dopamine D4.4 receptor (Ki=1.5 nM), which was 20-fold higher than that of clozapine (Ki=30.4 nM). A-381393 exhibited highly selective binding for the dopamine D4.4 receptor (>2700-fold) when compared to D1, D2, D3, and D5 dopamine receptors. A-381393 potently inhibited the functional activity of agonist-induced GTP-gamma-S binding assay and 1 microM dopamine-induced-Ca2+ flux in human dopamine D4.4 receptor-expressing cells, but not in human dopamine D2L or D3 receptor cells [1]. A-381393 blocked both c-Fos expression and ERK1/2 phosphorylation produced by PD168077. Treatment with A-381393 alone significantly reduced the amount of Fos immunoreactivity as compared to basal expression observed in vehicle-treated controls [2].

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

溶解度: DMSO : 50 mg/mL (156.04 mM)


关键字: inhibit | A381393 | Dopamine Receptor | A 381393 | Inhibitor | A-381393

相关产品: Ecopipam | Thioridazine hydrochloride | Citicoline | Pimozide-d4 | 9-FLUORENOL | Neuromedin N acetate(92169-45-4 free base) | Pramipexole dihydrochloride hydrate | PNU-177864 hydrochloride | 5-HT6/7 antagonist 1 | BisfluoroModafinil

相关库: Anti-Neurodegenerative Disease Compound Library | Neurotransmitter Receptor Compound Library | Anti-Parkinson's Disease Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Neuronal Signaling Compound Library | CNS-Penetrant Compound Library | Inhibitor Library | GPCR Compound Library | Bioactive Compound Library

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