The 1,4-dihydropyridine receptor: a regulatory component of the Ca2+ channel.
Evidence that nitrendipine (2,6-dimethyl-3-carbomethoxy-5-carbomethoxy-4-(3-nitrophenyl)1,4- dihydropyridine) and other 1,4-dihydropyridines interact at a specific site to antagonize Ca2+ channel function is reviewed. This evidence derives from electrophysiologic and pharmacologic studies and is confirmed by [3H]radioligand binding to excitable tissues. The availability of 1,4-dihydropyridine activator ligands including BAY K 8644 (2,6-dimethyl-3-carbomethyl-5-nitro-4-(2-trifluoromethyl)1,4- dihydropyridine) suggests that this site is intimately concerned with Ca2+ channel regulation. The actions of the 1,4-dihydropyridine ligands are discussed with particular reference to their tissue selectivity and the functional relationships of binding sites to Ca2+ channels.
D000818:Animals; D001665:Binding Sites / Q000187:drug effects; D002118:Calcium / Q000378:metabolism; D002121:Calcium Channel Blockers / Q000494:pharmacology*; D015220:Calcium Channels; D055598:Chemical Phenomena; D002621:Chemistry; D004095:Dihydropyridines; D006801:Humans; D007473:Ion Channels / Q000502:physiology*; D009130:Muscle, Smooth / Q000378:metabolism; D009928:Organ Specificity; D011725:Pyridines / Q000378:metabolism*; D011978:Receptors, Nicotinic / Q000187:drug effects / Q000378:metabolism*; D013329:Structure-Activity Relationship
D002121:Calcium Channel Blockers; D015220:Calcium Channels; D004095:Dihydropyridines; D007473:Ion Channels; D011725:Pyridines; D011978:Receptors, Nicotinic; C038806:1,4-dihydropyridine; D002118:Calcium