Interactions of local anesthetics with neuronal 1,4-dihydropyridine binding sites.
A series of local anesthetics competed with 1,4-dihydropyridine [3H]PN 200,110 binding to synaptosomes from guinea pig cerebral cortex synaptosomes. Dibucaine (10(-3)M) increased the dissociation rate of bound [3H]PN 200,110 consistent with an indirect, rather than competitive, interaction between local anesthetics and the 1,4-dihydropyridine site. The binding activities were compared to those previously available for local anesthetic competition with [3H]batrachotoxinin benzoate binding at a Na+ channel site. A linear correlation was observed between the two sets of activities with significantly higher activities being exhibited at the Na+ channel site. This relationship is consistent with the significant structural homologies exhibited between Na+ and Ca2+ channels.
Kwon
Y W
YW
Department of Biochemical Pharmacology, School of Pharmacy, State University of New York at Buffalo 14260.
Triggle
D J
DJ
D000779:Anesthetics, Local / Q000494:pharmacology*; D000818:Animals; D001665:Binding Sites; D001667:Binding, Competitive; D015220:Calcium Channels / Q000187:drug effects*; D002540:Cerebral Cortex / Q000187:drug effects* / Q000378:metabolism; D003992:Dibucaine / Q000494:pharmacology; D006168:Guinea Pigs; D008297:Male; D011869:Radioligand Assay; D015222:Sodium Channels / Q000187:drug effects; D013329:Structure-Activity Relationship
D000779:Anesthetics, Local; D015220:Calcium Channels; D015222:Sodium Channels; D003992:Dibucaine