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咖啡因可减弱新型腺苷A2A受体激动剂瑞加腺苷(CVT-3146)诱导的冠状动脉舒张持续时间及血流动力学变化。

Caffeine attenuates the duration of coronary vasodilation and changes in hemodynamics induced by regadenoson (CVT-3146), a novel adenosine A2A receptor agonist.

作者信息

Zhao Gong, Messina Eric, Xu Xiaobin, Ochoa Manuel, Sun Hai-Ling, Leung Kwan, Shryock John, Belardinelli Luiz, Hintze Thomas H

机构信息

Department of Pharmacology and Preclinical Development, CV Therapeutics, Inc., Palo Alto, California, USA.

出版信息

J Cardiovasc Pharmacol. 2007 Jun;49(6):369-75. doi: 10.1097/FJC.0b013e318046f364.

Abstract

Effects of caffeine on regadenoson-induced coronary vasodilation and changes in hemodynamics were examined in conscious dogs. Sixteen dogs were chronically instrumented for measurements of coronary blood flow (CBF), mean arterial pressure (MAP), and heart rate (HR). Regadenoson (5 microg/kg, IV) increased CBF from 34 +/- 2 to 191 +/- 7 mL/min. The duration of the 2-fold increase in CBF was 515 +/- 71 seconds. Regadenoson decreased MAP by 15 +/- 2% and increased HR by 114 +/- 14%. Regadenoson-induced maximum increases in CBF were not significantly lower in the presence of caffeine at 1, 2, 4, and 10 mg/kg (2 +/- 3, 0.7 +/- 3, 16 +/- 5, and 13 +/- 8%, respectively; all P > 0.05). Caffeine at 1, 2, 4, and 10 mg/kg significantly decreased the duration of the 2-fold increase in CBF induced by regadenoson by 17% +/- 4%, 48% +/- 8%, 62% +/- 5%, and 82% +/- 5%, respectively (all P < 0.05). Caffeine at 4 and 10 mg/kg significantly attenuated the effects of regadenoson on MAP and HR. The results indicate that 1 to 10 mg/kg caffeine dose-dependently reduced the duration, but not the peak increase of CBF caused by 5 microg/kg regadenoson.

摘要

在清醒犬中研究了咖啡因对瑞加腺苷诱导的冠状动脉血管舒张及血流动力学变化的影响。16只犬被长期植入仪器以测量冠状动脉血流量(CBF)、平均动脉压(MAP)和心率(HR)。瑞加腺苷(5微克/千克,静脉注射)使CBF从34±2毫升/分钟增加至191±7毫升/分钟。CBF增加两倍的持续时间为515±71秒。瑞加腺苷使MAP降低15±2%,使HR增加114±14%。在存在1、2、4和10毫克/千克咖啡因的情况下,瑞加腺苷诱导的CBF最大增加量无显著降低(分别为2±3%、0.7±3%、16±5%和13±8%;所有P>0.05)。1、2、4和10毫克/千克的咖啡因分别使瑞加腺苷诱导的CBF增加两倍的持续时间显著缩短17%±4%、48%±8%、62%±5%和82%±5%(所有P<0.05)。4和10毫克/千克的咖啡因显著减弱了瑞加腺苷对MAP和HR的影响。结果表明,1至10毫克/千克的咖啡因剂量依赖性地缩短了由5微克/千克瑞加腺苷引起的CBF增加的持续时间,但未降低其峰值增加量。

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