COR659

COR659CAS号: 544450-68-2分子式: C16H16ClNO3S分子量: 337.82描述纯度储存/保存方法可溶性/溶解性In vitro(体外研究)In vivo(体内研究)

产品描述
描述
COR659 is a 2-acylaminothiophene derivative able to suppress alcohol and chocolate self-administration in rats, likely via positive allosteric modulation of the GABAB receptor and antagonism/inverse agonism at the cannabinoid CB1 receptor.
纯度
98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
可溶性/溶解性
DMSO:33.33 mg/mL (98.66 mM)
生物活性
In vitro(体外研究)
In vitro [35S]GTPγS binding assays on stimulated GABAB and CB1 receptors, in combination with alcohol and chocolate self-administration experiments in rats, were employed to assess the pharmacological profile of this novel set of analogues, using COR659 as reference compound[1].
In vivo(体内研究)
10-Day treatment with COR659(0, 2.5, 5, and 10 mg/kg; i.p.) produced a dose-related reduction of both alcohol and chocolate self-administration, with limited loss of efficacy on continuing treatment. Acute COR659 suppressed reinstatement of alcohol seeking. Among the 9 tested analogues, only COR657 (methyl 2-(benzoylamino)-4-ethyl-5-methylthiophene-3-carboxylate) decreased alcohol self-administration similarly to COR659; all other compounds produced modest, or even no, effect on alcohol self-administration. COR659 excluded, no compound altered chocolate self-administration[2].