Mollace V, De Francesco E A, Fersini G, Nisticò G
Institute of Pharmacology, Faculty of Medicine of Catanzaro, University of Regio Calabria, Italy.
Funct Neurol. 1991 Apr-Jun;6(2):101-6.
The cardiovascular responses induced by intracerebroventricular or intravenous administration of ketanserin in normotensive rats were evaluated. Ketanserin, which is an antagonist at 5-HT2 receptors, when microinfused into the third cerebral ventricle, did not induce significant cardiovascular effects, except for a slight and transitory hypotensive response after the microinfusion of the highest dose (200 micrograms). However, at doses which were unable to affect directly blood pressure or heart rate, ketanserin, microinfused into the same site, antagonized the pressor response induced by peripheral administration of methoxamine, an alpha 1-adrenoceptor agonist. Furthermore, peripheral administration of ketanserin produced dose-dependent hypotension and bradycardia and antagonized the pressor effect of an intravenous bolus injection of methoxamine. In conclusion, the present experiments confirmed the ability of ketanserin to produce cardiovascular effects when administered peripherally and provides evidence for an involvement of ketanserin-sensitive receptors in the brain in the regulation of phasic responses during experimentally induced hypertension.
评估了在正常血压大鼠中脑室内或静脉注射酮色林所诱导的心血管反应。酮色林是一种5 - HT2受体拮抗剂,当微量注入第三脑室时,除了在注入最高剂量(200微克)后出现轻微且短暂的降压反应外,未诱导出明显的心血管效应。然而,在无法直接影响血压或心率的剂量下,微量注入同一部位的酮色林可拮抗外周给予甲氧基明(一种α1 -肾上腺素能受体激动剂)所诱导的升压反应。此外,外周给予酮色林会产生剂量依赖性的低血压和心动过缓,并拮抗静脉推注甲氧基明的升压作用。总之,本实验证实了酮色林外周给药时产生心血管效应的能力,并为大脑中对实验性诱导高血压期间的相位反应调节起作用的酮色林敏感受体提供了证据。