PMID: 11902808Mar 21, 2002Paper

The long-lasting anti-anginal effects of CP-060S in a rat model of arginine vasopressin-induced myocardial ischaemia

The Journal of Pharmacy and Pharmacology
Yuichiro AdachiKazuhiko Tamura

Abstract

The anti-anginal effect of CP-060S, a new cardioprotective agent that prevents myocardial Na+-, Ca2+-overload and has Ca2+-channel blocking activity, was evaluated in a rat model of arginine8-vasopressin (AVP)-induced cardiac ischaemia. Infusion of AVP (0.2 IU kg(-1)) depressed the electrocardiogram (ECG) ST segment, an index of myocardial ischaemia. Vehicle, CP-060S and diltiazem were given orally 1, 2, 4, 8, 12 and 24 h before the administration of AVP. CP-060S, at 3 mg kg(-1) and 10 mg kg(-1), suppressed AVP-induced ST-segment depression for 2 h and 12 h, respectively. In contrast, diltiazem, at 10 and 30 mg kg(-1), suppressed AVP-induced ST-segment depression for only 1 h. The persistent suppression of the AVP-induced ST-segment depression by CP-060S correlated with the time course of changes in its plasma concentration. The minimum effective concentration of CP-060S was estimated to be 30 ng mL(-1) (approximately 50 nM), consistent with its vasorelaxant potency in rat isolated aortic strips (concentration producing 50% relaxation of KCl contraction, IC50 = 32.6+/-8.3 nM). Intravenously administered CP-060S, at 300 microg kg(-1) and diltiazem at 500 microg kg(-1) showed similar haemodynamic changes, whereas CP-060S, at 300 ...Continue Reading

References

Sep 1, 1970·Japanese Journal of Pharmacology·Y HiramatsuY Kurosawa
Feb 18, 1982·The American Journal of Cardiology·R W PiephoR K Browne
May 1, 1993·Journal of Cardiovascular Pharmacology·W UchidaT Takenaka
Dec 1, 1994·British Journal of Pharmacology·Y KitaK Maeda
May 6, 1996·European Journal of Pharmacology·Y HirasawaY Kita
Jul 2, 1997·European Journal of Pharmacology·Y OhyaM Fujishima
Mar 26, 1998·Journal of Cardiovascular Pharmacology·Y SuzukiT Kato
Apr 21, 1998·European Journal of Pharmacology·Y SuzukiT Kato
Mar 17, 1999·European Journal of Pharmacology·Y AdachiO Kuromaru
Sep 16, 2000·European Journal of Pharmacology·K SatoH Karaki
Jul 27, 2001·Fundamental & Clinical Pharmacology·M FukazawaK Tamura

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