Dopropidil

Dopropidil is a novel anti-anginal calcium ion modulating agent, possessing intracellular calcium antagonist activity and anti-ischemic effects in several predictive animal models.

Signaling Pathways >> Membrane Transporter/Ion Channel >> Calcium Channel

Research Areas >> Cardiovascular Disease

Calcium[1]

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].

Rabbits[1] Groups of rabbits given a normal diet or one containing Cholesterol (1 %) are treated with vehicle, Diltiazem (10 mg/kg per day,p.o.), or Dopropidil (30 mg/kg per day, p.o.) over a 14-week period. Animals are then killed and certain blood vessels examined macroscopically, microscopically, and pharmacologically for reactivity to certain vasoactive agents.

[1]. J. Planellas, et al. Dopropidil, A Novel Antianginal Calcium Modulating Agent. Cardiovascular Drug Reviews. Vol.12, No.3, pp. 208-224.

Neomycin sulfate | Nifedipine | Acetylcholine chloride | Ionomycin | (S)-(-)-Bay K 8644 | Nimodipine | Mibefradil dihydrochloride | Levetiracetam | CDN 1163 | Dantrolene sodium | Thapsigargin | Flufenamic Acid | ABT 639 | Ranolazine dihydrochloride | Cromolyn (sodium)

MOLECULAR FORMULA :

C20-H35-N-O2

MOLECULAR WEIGHT :

321.56

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

>600 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #4430332