Il Farmaco

Synthesis and antagonistic activity at muscarinic receptor subtypes of some derivatives of diphenidol

…, P Angeli, M Buccioni, S Burnelli, A Cavalli, G Marucci…

Index: Varoli, Lucilla; Angeli, Piero; Buccioni, Michela; Burnelli, Silvia; Cavalli, Andrea; Marucci, Gabriella; Recanatini, Maurizio Farmaco, 2003 , vol. 58, # 9 p. 651 - 657

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Citation Number: 5

Abstract

A series of new derivatives, related to diphenidol and to its 2-carbonyl analogue, were designed as antimuscarinic agents. The synthesized compounds were evaluated both as hydrochlorides and as methiodides by functional tests at guinea-pig heart (M2), guinea-pig ileum (M3) and rabbit vas deferens (putative M4). Two derivatives (3a and 5a) showed an M3-selective profile similar to that of the reference compounds, though they resulted less ...