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8-羟基-2-(二-N-丙基氨基)四氢萘(8-OH-DPAT)对自发性高血压大鼠的降压作用

Hypotensive action of 8-hydroxy-2-(di-N-propylamino)tetralin (8-OH-DPAT) in spontaneously hypertensive rats.

作者信息

Martin G E, Lis E V

出版信息

Arch Int Pharmacodyn Ther. 1985 Feb;273(2):251-61.

PMID:3159366
Abstract

8-Hydroxy-2-(di-N-propylamino)tetralin (8-OH-DPAT), a reported serotonin receptor agonist, was found to produce drops both in mean arterial blood pressure (MAP) and heart rate in unanesthetized spontaneously hypertensive rats. The hypotensive episodes were elicited whether the compound was given intraperitoneally (minimum hypotensive dose = 0.02 mg/kg), orally (7.5 mg/kg or intracerebroventricularly (0.014 mg/kg). No bradycardia, however, was elicited following intracerebral infusions of 8-OH-DPAT. The bradycardia and hypotension were moderate in duration (1-4 hr). The serotonin receptor blocking agents cyproheptadine (5 mg/kg i.p.) and methergoline (1.0 mg/kg i.p.) failed to reduce either of the cardiovascular actions of 8-OH-DPAT. Methiothepin (0.5 mg/kg), another serotonin receptor blocker which produces falls in MAP itself, failed to attenuate 8-OH-DPAT-induced hypotension, but did block 8-OH-DPAT-induced bradycardia. 8-OH-DPAT exerts potent hypotensive and bradycardic effects in the unanesthetized spontaneously hypertensive rat. Whether this effect is the result of serotonin receptor activation is not yet clear.

摘要

8-羟基-2-(二正丙基氨基)四氢萘(8-OH-DPAT)是一种已报道的血清素受体激动剂,发现在未麻醉的自发性高血压大鼠中,它会使平均动脉血压(MAP)和心率下降。无论该化合物是腹腔注射(最小降压剂量=0.02mg/kg)、口服(7.5mg/kg)还是脑室内注射(0.014mg/kg),都会引发降压发作。然而,脑室内注射8-OH-DPAT后并未引发心动过缓。心动过缓和低血压的持续时间适中(1-4小时)。血清素受体阻断剂赛庚啶(5mg/kg腹腔注射)和麦角新碱(1.0mg/kg腹腔注射)未能减轻8-OH-DPAT的任何一项心血管作用。甲硫噻嗪(0.5mg/kg)是另一种本身会使MAP下降的血清素受体阻断剂,它未能减弱8-OH-DPAT诱导的低血压,但确实阻断了8-OH-DPAT诱导的心动过缓。8-OH-DPAT在未麻醉的自发性高血压大鼠中发挥强大的降压和心动过缓作用。这种作用是否是血清素受体激活的结果尚不清楚。

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