Matsumoto M, Yoshioka M, Togashi H, Minami M, Nagao A, Saito H
First Department of Pharmacology, Hokkaido University School of Medicine, Sapporo, Japan.
Hokkaido Igaku Zasshi. 1988 Jan;63(1):36-43.
The present study was undertaken to elucidate the effects of a new synthesized phenylpiperazine derivative SGB-1534 on mean arterial blood pressure and heart rate in stroke-prone spontaneously hypertensive rats(SHRSP). SGB-1534 (0.05 and 0.5 mg/kg, i.v.) produced a significantly greater decrease in mean arterial blood pressure in SHRSP than in normotensive Wistar Kyoto rats(WKY). Heart rate also tended to decrease in parallel with the decrease in mean arterial blood pressure in SHRSP. In this study, it was revealed that SGB-1534 has an antihypertensive effect in SHRSP. An attempt was made to elucidate the hypotensive mechanism of SGB-1534 using WKY. SGB-1534 (0.5 mg/kg, i.v.) significantly inhibited pressor responses to norepinephrine (5 micrograms/kg, i.v.) and methoxamine (50 micrograms/kg, i.v.). SGB-1534 (0.5 mg/kg, i.v.) did not affect the preganglionic sympathetic adrenal nerve activity. The present findings suggest that the action site of SGB-1534 is not in the central nervous system, but in the peripheral alpha 1-adrenoceptors in rats.
本研究旨在阐明一种新合成的苯基哌嗪衍生物SGB - 1534对易患中风的自发性高血压大鼠（SHRSP）平均动脉血压和心率的影响。SGB - 1534（0.05和0.5毫克/千克，静脉注射）使SHRSP的平均动脉血压下降幅度显著大于正常血压的Wistar Kyoto大鼠（WKY）。在SHRSP中，心率也倾向于随平均动脉血压的下降而平行降低。在本研究中，发现SGB - 1534对SHRSP有降压作用。尝试使用WKY阐明SGB - 1534的降压机制。SGB - 1534（0.5毫克/千克，静脉注射）显著抑制了对去甲肾上腺素（5微克/千克，静脉注射）和甲氧明（50微克/千克，静脉注射）的升压反应。SGB - 1534（0.5毫克/千克，静脉注射）不影响节前交感肾上腺神经活动。目前的研究结果表明，SGB - 1534的作用部位不在中枢神经系统，而在大鼠的外周α1 - 肾上腺素能受体。
