5-羟色胺1B受体介导大鼠尾动脉对5-羟色胺的强烈收缩反应。
5-HT1B receptors mediate potent contractile responses to 5-HT in rat caudal artery.
作者信息
Craig D A, Martin G R
机构信息
Analytical Pharmacology Group, Wellcome Research Laboratories, Beckenham, Kent.
出版信息
Br J Pharmacol. 1993 Jul;109(3):609-11. doi: 10.1111/j.1476-5381.1993.tb13615.x.
Abstract
5-Hydroxytryptamine (5-HT) evoked potent contractile responses in phenoxybenzamine-treated ring segments of rat caudal artery, partially contracted with U46619. Responses were mimicked by 5-HT1-selective agonists with the potency order: RU24969 > 5-carboxamidotryptamine > 5-HT = CP-93,129 >> sumatriptan. 8-Hydroxy-N,N-dipropylaminotetralin was virtually inactive. Responses were unaffected by spiperone (0.1 microM) and mesulergine (1.0 microM), but were antagonized competitively by (+/-)-cyanopindolol affording agonist-independent pKB estimates of 8.4 to 8.9. The pharmacological profile of this receptor is consistent with that of the 5-HT1B subtype. Since the 5-HT1B receptor is the rodent homologue of the 5-HT1D beta subtype, it might be anticipated that 5-HT1D beta receptors will be found to mediate vasoconstrictor responses in non-rodent species.
摘要
5-羟色胺（5-HT）在经苯氧苄胺处理、用U46619部分收缩的大鼠尾动脉环段中引发了强烈的收缩反应。5-HT1选择性激动剂可模拟这些反应，其效力顺序为：RU24969 > 5-羧酰胺色胺 > 5-HT = CP-93,129 >> 舒马曲坦。8-羟基-N,N-二丙基氨基四氢萘实际上无活性。反应不受螺哌隆（0.1微摩尔）和美舒麦角（1.0微摩尔）的影响，但被（±）-氰吲哚洛尔竞争性拮抗，得到的非激动剂依赖性pKB估计值为8.4至8.9。该受体的药理学特征与5-HT1B亚型一致。由于5-HT1B受体是5-HT1Dβ亚型的啮齿动物同源物，因此可以预期在非啮齿动物物种中会发现5-HT1Dβ受体介导血管收缩反应。
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