title: Modulation of the action of calcium antagonists in arteries.
abstract: This paper is a review of the experimental evidence showing that specific binding sites for dihydropyridine Ca antagonists are involved in inhibition of stimulus-dependent Ca entry into arterial cells and thereby in inhibition of the contractile response. The apparent affinity of the dihydropyridine binding site is related to the proportion of a high- and a low-affinity state which is regulated by membrane potential but could also be dependent upon other factors such as G proteins. Among Ca antagonists, a subgroup of agents exhibiting voltage dependence may be identified. Their apparent pharmacological potency is highly dependent on resting membrane potential and on the duration of the depolarizing stimulus.
authors.affiliation: Laboratoire de Pharmacodynamie Générale et de Pharmacologie, Université Catholique de Louvain, Bruxelles, Belgique.
authors.forename: T
authors.initials: T
authors.lastname: Godfraind
authors.forename: N
authors.initials: N
authors.lastname: Morel
authors.forename: M
authors.initials: M
authors.lastname: Wibo
mesh_terms: D000818:Animals; D001158:Arteries / Q000187:drug effects*; D002121:Calcium Channel Blockers / Q000494:pharmacology*; D015220:Calcium Channels / Q000187:drug effects; D006973:Hypertension / Q000188:drug therapy; D008564:Membrane Potentials; D009119:Muscle Contraction; D009131:Muscle, Smooth, Vascular / Q000187:drug effects* / Q000502:physiology
chemical_list: D002121:Calcium Channel Blockers; D015220:Calcium Channels