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  • Title: Stereoselective and non-stereoselective effects of D 600 (methoxyverapamil) in smooth muscle preparations.
    Author: Jim K, Harris A, Rosenberger LB, Triggle DJ.
    Journal: Eur J Pharmacol; 1981 Nov 19; 76(1):67-72. PubMed ID: 7198582.
    Abstract:
    Mechanical responses in guinea-pig ileal longitudinal, rat vasa deferentia and rat portal vein smooth muscle strips elicited by receptor activation (muscarinic or alpha-adrenergic) or by K+ depolarization were blocked by D 600 (methoxyverapamil). Stereoselectivity was observed with the (-)-enantiomer being more potent than the (+)-enantiomer (the ratio varying from 6 to 180). The tonic (slow) component of response was more sensitive than the phasic (fast) component. D 600 competitively blocked binding of (-)-[3H]QNB and [3H]WB 4101 to muscarinic and alpha-adrenergic receptors respectively, but in marked contrast to the effects on mechanical responses antagonism of ligand binding was non-stereoselective. It is suggested that stereoselectivity of action of D 600 may be a useful criterion to distinguish between its several sites of action.
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