Dopropidil is a novel anti-anginal calcium ion modulating agent, possessing intracellular calcium antagonist activity andanti-ischemic effects in several predictive animal models.
Dopropidil is able to inhibit caffeine-induced contractions of rabbit renal arteries in a calcium-free medium (IC50=30.0 uM). Dopropidil inhibits norepinephnne (NE)-induced responses with IC50s of 2.7 and 29.8 uM, respectively. At 3 and 10 μM, Dopropidil significantly reduces the maximum increase in diastolic tension evoked by veratrine (IC50=2.8 μM)[1].
Dopropidil (1 and 2.5 mg/kg) dose-dependently reduces the electrical (ST segment elevation), biochemical (lactate production and potassium release), and mechanical (loss in myocardial segment contractility) perturbations induced by ischemia in the anesthetized dog. Intraduodenal administration of Dopropidil (50 mg/kg) significantly reduces isoproterenol-induced tachycardia. This effect is manifest at 15-120 min following administration of the compound which indicates a rapid absorption and a long duration of action. In conscious dogs Dopropidil (12-14 mg/kg p.o.) reduces resting heart rate by approximately10 beats/min[1].
[1]. J. Planellas, et al. Dopropidil, A Novel Antianginal Calcium Modulating Agent. Cardiovascular Drug Reviews. Vol.12, No.3, pp. 208-224.