A region in IVS5 of the human cardiac L-type calcium channel is required for the use-dependent block by phenylalkylamines and benzothiazepines

HK Motoike, I Bodi, H Nakayama, A Schwartz… - Journal of Biological …, 1999 - ASBMB
Mutations in motif IVS5 and IVS6 of the human cardiac calcium channel were made using
homologous residues from the rat brain sodium channel 2a.[3 H] PN200-110 and allosteric
binding assays revealed that the dihydropyridine and benzothiazepine receptor sites
maintained normal coupling in the chimeric mutant channels. Whole cell voltage clamp
recording fromXenopus oocytes showed a dramatically slowed inactivation and a complete
loss of use-dependent block for mutations in the cytoplasmic connecting link to IVS5 (HHT …