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 potent.
Synthesis and antagonistic activity at muscarinic receptor subtypes of some derivatives of diphenidol
ANGELI, Piero;BUCCIONI, Michela;MARUCCI, Gabriella;
2003-01-01
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 potent.File in questo prodotto:
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