Piascik M T, Sparks M S, Pruitt T A
Department of Pharmacology, University of Kentucky, College of Medicine, Lexington.
J Pharmacol Exp Ther. 1992 Sep;262(3):901-6.
The effect of chlorethylclonidine (CEC) on arterial blood pressure and heart rate (HR) has been evaluated in the conscious rat. CEC injection (25 mg/kg i.p.) caused a statistically significant decrease in mean arterial blood pressure (MAP) that was seen 24 hr after treatment. CEC also induced a decrease in HR that was maximal at 45 min but returned to pretreatment levels after 3 hr. CEC had no effect on the ability of isoproterenol to increase HR. CEC treatment had little effect on the pressor dose-response curve of either phenylephrine or BHT 920. When injected into the brain (25 mg/kg, lateral ventricle), CEC had no effect on MAP or HR. Yohimbine injected into the lateral ventricle had no effect on the response to i.p. CEC. Prazosin, used as a standard for comparison, caused a larger fall in MAP than CEC and this hypotension was associated with tachycardia and a marked shift (greater than 300-fold) in the phenylephrine pressor dose-response curve. A reactive analog of prazosin, SZL-49 [1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(2-bicyclo[2,2,2]octa- 2,5-diene-2-carbonyl)piperazine], had effects similar to prazosin on MAP and HR.(ABSTRACT TRUNCATED AT 250 WORDS)
已在清醒大鼠中评估了氯乙基可乐定（CEC）对动脉血压和心率（HR）的影响。腹腔注射CEC（25mg/kg）导致平均动脉血压（MAP）在治疗后24小时出现统计学上的显著下降。CEC还引起心率下降，在45分钟时达到最大，但3小时后恢复到治疗前水平。CEC对异丙肾上腺素增加心率的能力没有影响。CEC治疗对去氧肾上腺素或BHT 920的升压剂量反应曲线几乎没有影响。当注入脑内（25mg/kg，侧脑室）时，CEC对MAP或HR没有影响。注入侧脑室的育亨宾对腹腔注射CEC的反应没有影响。用作比较标准的哌唑嗪导致MAP下降幅度大于CEC，这种低血压与心动过速以及去氧肾上腺素升压剂量反应曲线的显著偏移（大于300倍）有关。哌唑嗪的反应性类似物SZL-49 [1-(4-氨基-6,7-二甲氧基-2-喹唑啉基)-4-(2-双环[2,2,2]辛-2,5-二烯-2-羰基)哌嗪]对MAP和HR的影响与哌唑嗪相似。（摘要截短于250字）
