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Antihypertensive activity of OPC-13340, a new potent and long-acting dihydropyridine calcium antagonist, in rats.

Abstract
The antihypertensive action of OPC-13340, a new dihydropyridine, was studied in rats and compared with the action of nicardipine and other dihydropyridines. OPC-13340 showed more potent and longer hypotensive action than nicardipine when administered either intravenously (i.v.) or orally in normotensive and hypertensive rats. Among 6 compounds tested, (OPC-13340, nifedipine, nitrendipine, nisoldipine, nicardipine and diltiazem), OPC-13340 was the most potent and long-acting when administered orally to spontaneously hypertensive rats (SHR). Tachycardia after administration of OPC-13340 was less or diminished earlier than that of nicardipine. Oral administration of OPC-13340 (3 mg/kg) once daily for 13 days did not cause any rebound phenomena in SHR. The compound inhibited Ca- or K-induced contractions in isolated rat aorta and shortened action potential duration in guinea pig papillary muscle, suggesting Ca channel blocking action. OPC-13340 might be useful as a drug for once-daily therapy of essential hypertension.
AuthorsN Nakayama, K Ikezono, T Mori, S Yamashita, S Nakayama, Y Tanaka, T Hosokawa, Y Minami, K Masutani, Y Yamamura
JournalJournal of cardiovascular pharmacology (J Cardiovasc Pharmacol) Vol. 15 Issue 5 Pg. 836-44 (May 1990) ISSN: 0160-2446 [Print] United States
PMID1692946 (Publication Type: Journal Article)
Chemical References
  • Antihypertensive Agents
  • Calcium Channel Blockers
  • Dihydropyridines
  • pranidipine
  • Calcium
Topics
  • Action Potentials (drug effects)
  • Animals
  • Antihypertensive Agents
  • Blood Pressure (drug effects)
  • Calcium (pharmacology)
  • Calcium Channel Blockers (pharmacology)
  • Dihydropyridines (pharmacology)
  • Guinea Pigs
  • Heart Rate (drug effects)
  • Hypertension, Renovascular (physiopathology)
  • In Vitro Techniques
  • Male
  • Muscle Contraction (drug effects)
  • Muscle, Smooth, Vascular (drug effects)
  • Papillary Muscles (drug effects)
  • Rats
  • Rats, Inbred SHR
  • Rats, Inbred Strains

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