Effects of amlodipine on native cardiac Na+ channels and cloned alpha-subunits of cardiac Na+ channels.
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Inoue Y, Hisatome I, Tsuboi M, Ahmmed GU, Yatsuhashi T, Uchida K, Yamanouchi Y, Santo Y, Miake J, Tanaka Y, Hamada T, Watanabe M, Igawa O, Yoshida A, Shigemasa C, Makita N, Sato R
Effects of amlodipine on native cardiac Na+ channels and cloned alpha-subunits of cardiac Na+ channels.
Arzneimittelforschung. 1999 May;49(5):394-7. doi: 10.1055/s-0031-1300433.
- PubMed ID
- 10367100 [ View in PubMed]
- Abstract
The inhibitory effects of amlodipine besilate (CAS 11470-99-6) on the native Na+ current (INa) and cloned human cardiac Na+ channel alpha subunit (hH1) were studied by whole cell patch clamp techniques. Amlodipine produced tonic block of INa in a concentration- and holding potential (HP)-dependent manner with hyperpolarization of H infinity. Amlodipine produced phasic blockade of INa, which was dependent on HP and pulse duration. Amlodipine produced tonic blockade of hH1 in a concentration-dependent manner with 1 : 1 stoichiometry, and phasic blockade of hH1 which was dependent on the pulse duration. Amlodipine blocked INa in a voltage- and frequency-dependent manner via affinity to the resting as well as inactivated conformations of the alpha subunit.
DrugBank Data that Cites this Article
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Amlodipine Voltage-dependent T-type calcium channel subunit alpha-1I Protein Humans YesInhibitorDetails