素马匹坦缺乏诱导的主动脉收缩或舒张:血管内皮和血管平滑肌中检测到5-HT1B受体蛋白,但主动脉中未检测到。

Receptors & channels Pub Date : 2002-01-01
Marlene L Cohen, Elizabeth J Galbreath, Kathryn W Schenck, Danqing Li, Beth J Hoffman, Anindya Bhattacharya
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引用次数: 0

摘要

由于在大鼠主动脉中报道了5-HT1B受体mRNA,并且5-HT1B受体的激活与血管收缩有关,我们探索了素马匹坦诱导的大鼠主动脉5-HT1B受体蛋白的收缩性和免疫组织化学密度。舒马曲坦(高达10(-4)M)是一种5-HT1B/1D受体激动剂,即使在L-NAME存在或PGF2 α诱导适度张力(10(-6)M)后,也不会收缩内皮完整或脱落的大鼠主动脉。舒马曲坦也不会放松主动脉预备物,与PGF2 α (3 × 10(-6) M)或苯肾上腺素(3 × 10(-7) M)预先收缩。在大鼠主动脉内皮和平滑肌中均检测到微量5-HT1B受体蛋白。然而,在供应主动脉的血管血管的血管平滑肌中发现致密的5-HT1B受体蛋白。因此,在大鼠主动脉组织提取物中检测到的5-HT1B受体mRNA很可能反映了血管小动脉中5-HT1B受体的表达。这些研究支持5-HT1B受体与血管收缩之间的联系,因为5-HT1B受体密度低的主动脉缺乏对舒马曲坦的反应,舒马曲坦是一种被认为通过5-HT1B/1D受体收缩血管的激动剂。此外,当使用5-HT1B受体mRNA来提示组织中的受体蛋白时,必须谨慎,因为这种RT-PCR产物可能主要来自小血管。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Lack of sumatriptan-induced aortic contraction or relaxation: 5-HT1B receptor protein detected in endothelium and smooth muscle of vasa vasorum but not aorta.

Since 5-HT1B receptor mRNA was reported in rat aorta, and 5-HT1B receptor activation has been linked to vascular contraction, we explored sumatriptan-induced contractility and immunohistochemical density of 5-HT1B receptor protein in rat aorta. Sumatriptan (up to 10(-4) M), a 5-HT1B/1D receptor agonist, did not contract the endothelial intact or denuded rat aorta, even in the presence of L-NAME or after induction of modest tone with PGF2 alpha (10(-6) M). Sumatriptan also did not relax aortic preparations precontract with PGF2 alpha (3 x 10(-6) M) or phenylephrine (3 x 10(-7) M). Using a polyclonal antibody directed against the 5-HT1B receptor, minimal 5-HT1B receptor protein was detected in either the endothelium or smooth muscle of the rat aorta. However, dense 5-HT1B receptor protein was found in the vascular smooth muscle of the vasa vasorum supplying the aorta. Thus, the 5-HT1B receptor mRNA detected in tissue extracts of the rat aorta most likely reflects 5-HT1B receptor expression in the arterioles of the vasa vasorum. These studies support the link between the 5-HT1B receptor and vascular contraction in that the aorta with low density of 5-HT1B receptors lacked responses to sumatriptan, an agonist thought to contract blood vessels via 5-HT1B/1D receptors. Furthermore, caution must be observed when using 5-HT1B receptor mRNA to suggest receptor protein in tissues since this RT-PCR product may be derived predominantly from small blood vessels.

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