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ID: ALA3244156

Journal: J Med Chem

Title: Analgesic and tranquilizing activity of 5,8-disubstituted 1-tetralone Mannich bases.

Authors: Welch WM, Harbert CA, Sarges R, Stratten WP, Weissman A.

Abstract: 5,8-Disubstituted 1-tetralone Mannich bases represent semirigid variants of classical (i.e., chlorpromazine) neuroleptic agents. 8-Chloro-5-methoxy-2-morpholinomethyl-1-tetralone exhibits neuroleptic potency in the thiothixene range in animal models. Of greater potential interest, however, is the analgesic potency of the 8-chloro-5-methoxy-2-pyrrolidinomethyl analogue which was in the morphine range. This compound did not induce tolerance nor was its activity reversed by naloxone. Structure-activity relationships of the series are discussed.

CiteXplore: 853506

DOI: 10.1021/jm00215a016