化合物CVT-10216 T15022

Product Introduction
Bioactivity


英文名: CVT-10216

描述: CVT-10216 是可逆的、选择性的醛脱氢酶 2（ALDH-2）抑制剂，IC50为 29 nM。对 ALDH-1的抑制作用较弱，IC50为 1.3 μM。 它可以减少偏爱酒精的大鼠过量饮酒，并表现出抗焦虑作用。

体内活性: CVT-10216 is a highly selective, reversible inhibitor of ALDH-2 that reduces excessive alcohol drinking.?Anxiety plays a role in alcoholism. As reflected in social interaction behavior in four unrelated rodent models: endogenous anxiety-like behavior in na?ve Fawn-Hooded rats, repeated alcohol-withdrawal-induced anxiety, restraint stress-induced anxiety and drug-induced anxiety.?CVT-10216 counteracted anxiety in all models except that produced by the 5-HT(2C) agonist, mCPP.?CVT-10216 exhibited both acute and prophylactic inhibitions of repeated alcohol-withdrawal-induced anxiety.?Importantly, anxiogenic behavior induced by the benzodiazepine receptor inverse agonist, DMCM, was counteracted dose-dependently by CVT-10216.CVT-10216 (intraperitoneal injection; 3.75 or 15 mg/kg) are determined 5 h into the third withdrawal, it has the anxiolytic effect of 15 mg/kg CVT-10216 in this model. ?However it has no significant effects on locomotor activity. CVT-10216 (intraperitoneal injection; 3.75, 7.5, or 15 mg/kg) shows a increase in social interaction as a dose-dependent manner, punctuated by a 2-fold increase in social interaction after 15 mg/kg in Fawn-Hooded rats[1].

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

溶解度: DMF : 25 mg/mL (53.71 mM)
DMSO : 20 mg/mL (42.97 mM)


关键字: anxiolytic | CVT-10216 | CVT 10216 | inhibit | Aldehyde Dehydrogenase (ALDH) | alcohol-preferring | CVT10216 | Inhibitor | social | interaction

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相关库: ReFRAME Related Library | Anti-Cancer Metabolism Compound Library | Glutamine Metabolism Compound Library | Anti-Metabolism Disease Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Highly Selective Inhibitor Library | Metabolism Compound Library | NO PAINS Compound Library | Bioactive Compound Library

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