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一种氨基四氢萘衍生物TL-68引起的中枢介导的低血压和心动过缓。

Centrally mediated hypotension and bradycardia induced by an aminotetralin derivative: TL-68.

作者信息

Sharabi F M, Long J P, Rusterholz D B, Hoffman W E, Lee T, Cannon G J

出版信息

Res Commun Chem Pathol Pharmacol. 1978 Jun;20(3):457-73.

PMID:674826
Abstract

An aminotetralin derivate, N,N-dipropyl-2-amino-1,2,3,4-tetrahydronaphthalene (TL-68) induced a prolonged decrease in blood pressure and heart rate when administered i.v. in anesthetized cats. The compound inhibited the blood pressure and heart rate responses induced by central stump stimulation of the sciatic nerve indicating inhibition of sympathetic transmission. TL-68 caused a weak inhibition of the positive chronotropic response induced by stimulation of the cardioaccelerator nerve. When comparatively low doses of TL-68 were injected into the left vertebral artery, a considerable dose-dependent decrease in blood pressure and heart rate developed. The same doses had only small or negligible effects on blood pressure and heart rate when given intravenously. When TL-68 was injected into a lateral cerebral ventricle of unanesthetized rats, a significant hypotension and bradycardia was observed which could be prevented by prior intraventricular injection of phentolamine. The results suggest that this compound exerts its effect through a central mechanism of action, perhaps by stimulation of alpha-adrenoreceptors.

摘要

一种氨基四氢萘衍生物,N,N-二丙基-2-氨基-1,2,3,4-四氢萘(TL-68),静脉注射给麻醉猫时会导致血压和心率长时间下降。该化合物抑制了坐骨神经中枢残端刺激所诱导的血压和心率反应,表明其对交感神经传递有抑制作用。TL-68对心脏加速神经刺激所诱导的正性变时反应有微弱抑制作用。当将相对低剂量的TL-68注入左椎动脉时,会出现明显的剂量依赖性血压和心率下降。相同剂量静脉给药时对血压和心率的影响很小或可忽略不计。当将TL-68注入未麻醉大鼠的侧脑室时,观察到明显的低血压和心动过缓,预先脑室内注射酚妥拉明可预防这种情况。结果表明,该化合物通过中枢作用机制发挥作用,可能是通过刺激α-肾上腺素受体。

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