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舒马曲坦对猫脑实质内微循环的影响。

Effects of sumatriptan on the cerebral intraparenchymal microcirculation in the cat.

作者信息

Kobari M, Fukuuchi Y, Tomita M, Tanahashi N, Konno S, Takeda H

机构信息

Department of Neurology, School of Medicine, Keio University, Tokyo, Japan.

出版信息

Br J Pharmacol. 1993 Dec;110(4):1445-8. doi: 10.1111/j.1476-5381.1993.tb13983.x.

Abstract
  1. Sumatriptan, a 5-hydroxytryptamine (5-HT)1-like receptor agonist, is effective against the headache of migraine. The effects of sumatriptan injected via the carotid artery on the cerebral microcirculation were studied in 10 anaesthetized cats. 2. The local cerebral blood volume (CBV), mean transit time of blood (MTT) and cerebral blood flow (CBF) in the parieto-temporal cortex were measured by a photoelectric method. CBV represents the cumulative dimensions of the cerebral microvessels. 3. Sumatriptan at 5 and 50 micrograms kg-1 had no significant effects on the CBV, MTT, CBF, and mean arterial blood pressure (MABP); 500 micrograms kg-1 of sumatriptan reduced the CBV, prolonged the MTT, and decreased the CBF (approximately -20%) without affecting the MABP. Sumatriptan, 5 mg kg-1, elicited transient reductions in CBV and CBF, which were attributable to the rapid and marked falls of MABP seen with this dose. 4. Thus, while a high dose of sumatriptan (500 micrograms kg-1) exhibits direct vasoconstrictor actions on the cerebral vessels, low doses of sumatriptan, within the therapeutic range, elicit no vasoconstriction. The data do not support a vasoconstrictor action of sumatriptan playing a primary role in reversing the headache of migraine.
摘要
  1. 舒马曲坦是一种5-羟色胺(5-HT)1样受体激动剂,对偏头痛性头痛有效。在10只麻醉猫中研究了经颈动脉注射舒马曲坦对脑微循环的影响。2. 采用光电法测量顶颞叶皮质局部脑血容量(CBV)、平均血流通过时间(MTT)和脑血流量(CBF)。CBV代表脑微血管的累积尺寸。3. 5和50微克/千克的舒马曲坦对CBV、MTT、CBF和平均动脉血压(MABP)无显著影响;500微克/千克的舒马曲坦可降低CBV、延长MTT并降低CBF(约-20%),而不影响MABP。5毫克/千克的舒马曲坦可引起CBV和CBF的短暂降低,这归因于该剂量下MABP的快速和显著下降。4. 因此,虽然高剂量的舒马曲坦(500微克/千克)对脑血管有直接的血管收缩作用,但治疗范围内的低剂量舒马曲坦不会引起血管收缩。这些数据不支持舒马曲坦的血管收缩作用在缓解偏头痛性头痛中起主要作用。

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The mode of action of sumatriptan is vascular? A debate.舒马曲坦的作用方式是血管性的吗?一场辩论。
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