HOMEPRODUCTSCOMPANYCONTACTFAQResearchDictionaryPharmaSign Up FREE or Login

Antianginal effects of YM-16151-4 in various experimental angina models.

Abstract
The antianginal effects of YM-16151-4, a combined calcium entry blocking and beta 1-adrenoceptor blocking agent, were evaluated in various experimental angina models and compared with those of nifedipine and propranolol. In anesthetized dogs, YM-16151-4 (0.3 and 1 mg/kg intravenously, i.v.) increased coronary blood flow and reduced myocardial oxygen consumption (MVO2). In isolated dog coronary arteries, YM-16151-4 concentration-dependently inhibited 3,4-diaminopyridine-induced rhythmic contractions with an IC50 value of 91 nM. In anesthetized rats, YM-16151-4 also inhibited the ST-segment depression induced by vasopressin (0.5 U/kg i.v.) with an ED50 value of 29 mg/kg orally, (p.o.). Nifedipine was also effective in these models, but propranolol was not. In addition, YM-16151-4 (0.3 mg/kg i.v.) inhibited the ST-segment elevation in the epicardial ECG induced by coronary artery occlusion in anesthetized dogs. Propranolol (1 mg/kg i.v.) also inhibited this elevation, but nifedipine (0.003 mg/kg i.v.) did not. In anesthetized dogs, furthermore, the prolongation of PQ-interval induced by YM-16151-4 was almost the same as that induced by propranolol. These results demonstrate that YM-16151-4, in contrast to nifedipine and propranolol, is fully effective in these various types of angina models. Thus, YM-16151-4 is expected to prove a valuable antianginal agent in treatment of various types of angina pectoris, with these antianginal effects resulting from the sum of its calcium entry blocking and beta 1-adrenoceptor blocking activities.
AuthorsW Uchida, K Shibasaki, M Asano, T Takenaka
JournalJournal of cardiovascular pharmacology (J Cardiovasc Pharmacol) Vol. 21 Issue 5 Pg. 701-8 (May 1993) ISSN: 0160-2446 [Print] United States
PMID7685438 (Publication Type: Journal Article)
Chemical References
  • Calcium Channel Blockers
  • Dihydropyridines
  • Nitrophenols
  • Potassium Channels
  • YM 16151-1
  • Arginine Vasopressin
  • Propranolol
  • 4-Aminopyridine
  • Nifedipine
  • Amifampridine
Topics
  • 4-Aminopyridine (analogs & derivatives)
  • Amifampridine
  • Angina Pectoris (chemically induced, drug therapy, physiopathology)
  • Animals
  • Arginine Vasopressin
  • Atrioventricular Node (drug effects)
  • Calcium Channel Blockers (therapeutic use)
  • Coronary Circulation (drug effects)
  • Coronary Vasospasm (chemically induced, drug therapy)
  • Dihydropyridines (therapeutic use)
  • Dogs
  • Electrocardiography (drug effects)
  • Female
  • Heart Conduction System (drug effects)
  • In Vitro Techniques
  • Male
  • Muscle Contraction (drug effects)
  • Muscle, Smooth, Vascular (drug effects)
  • Nifedipine (therapeutic use)
  • Nitrophenols (therapeutic use)
  • Oxygen Consumption (drug effects)
  • Potassium Channels (drug effects)
  • Propranolol (therapeutic use)

Join CureHunter, for free Research Interface BASIC access!

Take advantage of free CureHunter research engine access to explore the best drug and treatment options for any disease. Find out why thousands of doctors, pharma researchers and patient activists around the world use CureHunter every day.
Realize the full power of the drug-disease research graph!


Choose Username:
Email:
Password:
Verify Password:
Enter Code Shown: