Shintomi K, Ogawa Y, Yoshimoto K, Narita H
Nihon Yakurigaku Zasshi. 1986 May;87(5):537-49. doi: 10.1254/fpj.87.537.
Effects of nicergoline on the cerebral and peripheral circulation were compared with those of dihydroergotoxine (DHE) and papaverine (PAP) in anesthetized and/or immobilized cats. The i.a. injection of nicergoline (0.032 approximately 32 micrograms/kg), similarly to PAP, caused dose-dependent increases in intramaxillary artery (as the human intracarotid artery) blood flow (IMBF) and femoral artery blood flow, but the injection of DHE had no effect on these blood flows. The i.v. injection of nicergoline (32 approximately 128 micrograms/kg) caused a dose-dependent fall in blood pressure (BP) and a transient slight decrease in cerebral vascular resistance, but did not affect IMBF, regional cerebral blood flow (r-CBF), intracranial pressure (ICP) and heart rate (HR). The i.v. injection of DHE produced a slight fall in BP and a marked long-lasting decrease in HR, without affecting other parameters. The i.v. injection of PAP (4 mg/kg) induced marked increases in IMBF, r-CBF, ICP and HR and caused a transient fall followed by a marked elevation in BP. The p.o. administration of nicergoline (0.06 approximately 4 mg/kg) caused a dose-dependent fall in BP and selective inhibition of pressure response to adrenaline (ID50: 0.25 mg/kg). The administration of DHE produced marked inhibition of pressure responses to both adrenaline and noradrenaline, accompanied with a slight fall in BP. Furthermore, the administration of nicergoline (3 approximately 100 mg/kg) induced a dose-dependent fall in BP in SHR. These results suggest that the cerebral and peripheral circulatory effects of nicergoline may be due to direct vasodilating action and alpha-blocking action in the animals.
在麻醉和/或固定的猫身上,比较了尼麦角林与双氢麦角毒碱(DHE)和罂粟碱(PAP)对脑循环和外周循环的影响。腹腔注射尼麦角林(0.032至约32微克/千克),与PAP相似,可引起上颌动脉(相当于人体颈内动脉)血流量(IMBF)和股动脉血流量呈剂量依赖性增加,但注射DHE对这些血流量无影响。静脉注射尼麦角林(32至约128微克/千克)可引起血压(BP)呈剂量依赖性下降,脑血管阻力短暂轻微降低,但不影响IMBF、局部脑血流量(r-CBF)、颅内压(ICP)和心率(HR)。静脉注射DHE可使BP略有下降,HR显著持久降低,而不影响其他参数。静脉注射PAP(4毫克/千克)可使IMBF、r-CBF、ICP和HR显著增加,并导致BP短暂下降后显著升高。口服尼麦角林(0.06至约4毫克/千克)可引起BP呈剂量依赖性下降,并选择性抑制对肾上腺素的压力反应(半数抑制剂量:0.25毫克/千克)。给予DHE可显著抑制对肾上腺素和去甲肾上腺素的压力反应,并伴有BP略有下降。此外,给予尼麦角林(3至100毫克/千克)可使自发性高血压大鼠(SHR)的BP呈剂量依赖性下降。这些结果表明,在动物中,尼麦角林对脑循环和外周循环的影响可能归因于直接血管舒张作用和α阻断作用。