Ontology highlight
ABSTRACT:
SUBMITTER: Bergson P
PROVIDER: S-EPMC3061365 | biostudies-literature | 2011 Mar
REPOSITORIES: biostudies-literature
Bergson Pamela P Lipkind Gregory G Lee Steven P SP Duban Mark-Eugene ME Hanck Dorothy A DA
Molecular pharmacology 20101213 3
Verapamil is a prototypical phenylalkylamine (PAA), and it was the first calcium channel blocker to be used clinically. It tonically blocks L-type channels in the inner pore with micromolar affinity, and its affinity increases at depolarized membrane potentials. In T-type calcium channels, verapamil blocks with micromolar affinity and has modestly increased affinity at depolarized potentials. We found that a related PAA, 4-desmethoxyverapamil (D888), is comparable with verapamil both in affinity ...[more]