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	Yes	Inhibitor	Details