COR659

Research use only, not for human use.

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.

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):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.(In Vivo):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.

Methyl 2-(4-chlorobenzamido)-4-ethyl-5-methylthiophene-3-carboxylate

GPCR/G Protein

Cannabinoid Receptor

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544450-68-2

337.8

C16H16ClNO3S

>98% (HPLC)

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O=C(C1=C(NC(C2=CC=C(Cl)C=C2)=O)SC(C)=C1CC)OC

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(-20℃)

With Ice Pack

≥ 2 years