COR659 是一种有效的GABAB的阳性变构调节剂。COR659具有缓解大鼠对酒精和巧克力成瘾的作用。

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.

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].

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].

544450-68-2

C16H16ClNO3S

337.82

DMSO:33.33 mg/mL (98.66 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years