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三环杂芳族体系。2-苯基-1,2,4-三唑并[1,5-c][1,3]苯并恶嗪-5-酮：一种新型苯二氮卓受体配体。

Tricyclic heteroaromatic systems. 2-Phenyl-1,2,4-triazolo[1,5-c][1,3]benzoxazin-5-one: a novel benzodiazepine receptor ligand.

作者信息

Catarzi D, Cecchi L, Colotta V, Martini C, Giusti L, Lucacchini A, Valle G

机构信息

Dipartimento di Scienze Farmaceutiche, Università di Firenze, Italy.

出版信息

Farmaco. 1994 Feb;49(2):89-92.

PMID:8003185
Abstract

The synthesis, unambiguous proof of structure and benzodiazepine receptor affinity and efficacy of 2-phenyl-1,2,4-triazolo[1,5-c][1,3]benzoxazin-5-one 1 are reported. The in vitro biological data indicate that 1 may be the lead compound of a new class of benzodiazepine antagonist-inverse agonist ligands.

摘要

报道了2-苯基-1,2,4-三唑并[1,5-c][1,3]苯并恶嗪-5-酮1的合成、结构的确证以及其对苯二氮卓受体的亲和力和功效。体外生物学数据表明，1可能是一类新型苯二氮卓拮抗剂-反向激动剂配体的先导化合物。

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