COR659

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

COR659 是一种 2-酰氨基噻吩衍生物，能够抑制大鼠的酒精和巧克力自我给药，可能是通过 GABAB 受体的正变构调节和大麻素 CB1 受体的拮抗/反向激动作用。

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):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.

COR659 apparently exerts its effects via a composite mechanism, including positive allosteric modulation of the GABAB receptor and an action at the cannabinoid CB1 receptor.

COR659 (0, 2.5, 5 and 10 mg/kg) treatment is completely ineffective on lever-responding (FR10) for regular food pellets in food-deprived Wistar rats.COR659 is able to suppress lever-responding for a sucrose solution in sP rats and a chocolate solution in Wistar rats. Animal Model:Male sP and Wistar rats.Dosage:0, 2.5, 5 and 10 mg/kg. Administration:Intraperitoneally (administered 30 min before the start of the self-administration, reinstatement, and locomotor activity sessions.).Result:The magnitude of the reducing effect of the compound on number oflever-responses for alcohol averaged approximately 30, 55, and 70%, in comparison to the vehicle-treated rat group, in the rat groups treated with 2.5, 5, and 10 mg/kg COR659, respectively.The magnitude of the reducing effect of COR659 on number of lever-responses for alcohol averaged approximately 20, 40, and 80%, in comparison to the vehicletreated rat group, in the rat groups treated with 2.5, 5, and 10 mg/kg COR659, respectively.

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

GPCR/G Protein

Cannabinoid Receptor

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544450-68-2

337.82

C16H16ClNO3S

>98% (HPLC)

In Vitro:?DMSO : 25 mg/mL (74.00 mM)

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