Synthesis and structure-activity relationships of 5, 6, 7, 8-tetrahydro-4 H-thieno [3, 2-b] azepine derivatives: Novel arginine vasopressin antagonists

H Cho, K Murakami, H Nakanishi…

Index: Cho, Hidetsura; Murakami, Kengo; Nakanishi, Hiroyuki; Isoshima, Hirotaka; Hayakawa, Kazuhide; Uchida, Itsuo Heterocycles, 1998 , vol. 48, # 5 p. 919 - 927

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Citation Number: 33

Abstract

A variety of novel heterocyclic compounds having thienoazepine, pyrroloazepine, furoazepine, and thienodiazepine skeletons were synthesized, most of which exhibited potent antagonism of [3H]-AVP specific binding in assays using rat liver (V1), rat kidney (V2), human platelet plasma membranes, and recombinant human CHO cells (V2), as well as antagonizing AVP-induced hypertension in rats (V1, intravenous) and showing a diuretic ...

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