Characterization of binding sites for two classes of calcium channel antagonists in human forebrain.
1,4-Dihydropyridine ([3H]PN200-110) and phenylalkylamine ([3H](-)D-888) bound with high affinity to human brain cortex homogenates. The ligand selectivity pattern indicates that [3H]PN200-110 binding was inhibited by related 1,4-dihydropyridine analogues but not by phenylalkylamines. On the other hand, phenylalkylamines were potent inhibitors of [3H](-)D-888 binding in human brain. The radioautographic distribution of [3H]PN200-110 and [3H](-)D-888 binding sites demonstrates that 1,4-dihydropyridine and phenylalkylamine sites were similarly distributed in human forebrain.
D000814:Aniline Compounds / Q000378:metabolism; D001345:Autoradiography; D001665:Binding Sites; D001921:Brain / Q000378:metabolism*; D002121:Calcium Channel Blockers / Q000378:metabolism*; D004095:Dihydropyridines; D006801:Humans; D066298:In Vitro Techniques; D017275:Isradipine; D007700:Kinetics; D008566:Membranes / Q000378:metabolism; D010069:Oxadiazoles / Q000494:pharmacology; D011725:Pyridines / Q000378:metabolism
D000814:Aniline Compounds; D002121:Calcium Channel Blockers; D004095:Dihydropyridines; D010069:Oxadiazoles; D011725:Pyridines; C038806:1,4-dihydropyridine; D017275:Isradipine