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Synthesis and pharmacological evaluation of sulfamide-based analogues of anandamide

机译:磺胺类酰胺基类似物的合成及药理评价

摘要

Arachidonyl and linoleyl sulfamide derivatives have been synthesized and their potential cannabimi- udmetic properties evaluated in in vitro functional and binding assays. Replacement of the ethanolamide udmoiety of anandamide by –CH2NHSO2NH–R considerably reduces the CB1 receptor activity and only udsome of the compounds showed modest cannabinoid properties in binding assays. The new compounds udwere also tested as inhibitors of the FAAH enzyme but were inactive.
机译:已经合成了花生四烯酸和亚油基磺酰胺衍生物,并在体外功能和结合试验中评估了它们的潜在大麻仿生特性。用–CH2NHSO2NH–R取代乙醇酰胺的ethanol南酰胺显着降低了CB1受体的活性,只有 udome的某些化合物在结合测定中显示出适度的大麻素性质。还测试了新化合物作为FAAH酶的抑制剂,但没有活性。

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