Discovery and main pharmacological properties of mibefradil (Ro 40-5967), the first selective T-type calcium channel blocker.
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Clozel JP, Ertel EA, Ertel SI
Discovery and main pharmacological properties of mibefradil (Ro 40-5967), the first selective T-type calcium channel blocker.
J Hypertens Suppl. 1997 Dec;15(5):S17-25.
- PubMed ID
- 9481612 [ View in PubMed]
- Abstract
PROPERTIES OF MIBEFRADIL: Mibefradil is a novel calcium channel antagonist with structural and pharmacological characteristics clearly distinct from those of classical calcium antagonists. It is a potent vasodilator with a high selectivity for the coronary vasculature over the peripheral vasculature and the myocardium. Most importantly, this compound can relax vascular muscle and slow the heart rate without reducing cardiac contractility. In addition, it does not stimulate neurohormonal reflexes and it exhibits a good pharmacological profile characterized by a long duration of action. MECHANISM OF ACTION: The mechanism of action of mibefradil is characterized by the selective blockade of transient, low-voltage-activated (T-type) calcium channels over long-lasting, high-voltage-activated (L-type) calcium channels, which is probably responsible for many of its unique properties. CLINICAL USE OF MIBEFRADIL: Although calcium antagonists are mainly used for the treatment of hypertension and angina pectoris, there is strong preclinical evidence that mibefradil may also be beneficial in the treatment of congestive heart failure.
DrugBank Data that Cites this Article
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Mibefradil Voltage-dependent T-type calcium channel subunit alpha-1G Protein Humans YesInhibitorDetails Mibefradil Voltage-dependent T-type calcium channel subunit alpha-1H Protein Humans YesInhibitorDetails Mibefradil Voltage-dependent T-type calcium channel subunit alpha-1I Protein Humans YesInhibitorDetails