一种在内皮细胞上介导豚鼠离体颈静脉舒张的5-羟色胺受体类似于5-羟色胺1D亚型。
An endothelial 5-HT receptor that mediates relaxation in guinea-pig isolated jugular vein resembles the 5-HT1D subtype.
作者信息
Gupta P
机构信息
Department of Biomedical Research, Wyeth Research (UK) Ltd., Maidenhead, Berkshire.
出版信息
Br J Pharmacol. 1992 Jul;106(3):703-9. doi: 10.1111/j.1476-5381.1992.tb14398.x.
Abstract
- Endothelium-dependent and -independent, concentration-related, relaxations to 5-hydroxytryptamine (5-HT) are described in a preparation of guinea-pig isolated jugular vein. 2. An endothelial 5-HT receptor was studied in the presence of mesulergine (at 10.0 microM, a concentration sufficient to antagonize 5-HT2 receptor-mediated contractions and endothelium-independent relaxations to 5-HT). Relaxations mediated by the endothelial 5-HT receptor were resistant to antagonism by mesulergine. 3. Several 5-HT receptor agonists activated the endothelial receptor with the following rank order of potency: 5-carboxamidotryptamine (5-CT) greater than 5-HT greater than methysergide greater than or equal to alpha-methyl-5-HT greater than sumatriptan greater than 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) greater than 2-methyl-5-HT. 4. Relaxations to 5-HT were not blocked by (+/-)-pindolol (1.0 microM), (-)-propranolol (1.0 microM), spiperone (1.0 microM), ondansetron (1.0 microM) or ICS 205-930 (10.0 microM). 5. Both 5-HT and sumatriptan evoked endothelium-dependent relaxations which were sensitive to antagonism (pA2 and apparent pA2 values respectively) by methiothepin (8.1 and 8.6), metergoline (7.4 and 7.5), PAPP (8.2 and 8.2), yohimbine (7.1 and 6.8), rauwolscine (6.8 and 6.7), but not by corynanthine (10.0 microM). 6. These observations are consistent with a 5-HT1D receptor-mediated effect, and provide further support for the concept that differences exist between endothelial 5-HT receptors in different tissues and species.
摘要
- 在豚鼠离体颈静脉标本中描述了内皮依赖性和非依赖性的、浓度相关的对5-羟色胺（5-HT）的舒张反应。2. 在美舒麦角（浓度为10.0微摩尔，足以拮抗5-HT2受体介导的收缩和对5-HT的非内皮依赖性舒张）存在的情况下研究了内皮5-HT受体。由内皮5-HT受体介导的舒张对美舒麦角的拮抗作用具有抗性。3. 几种5-HT受体激动剂激活内皮受体，其效力顺序如下：5-羧酰胺色胺（5-CT）＞5-HT＞甲基麦角新碱≥α-甲基-5-HT＞舒马曲坦＞8-羟基-2-（二正丙基氨基）四氢萘（8-OH-DPAT）＞2-甲基-5-HT。4. 对5-HT的舒张反应不受（±）-吲哚洛尔（1.0微摩尔）、（-）-普萘洛尔（1.0微摩尔）、螺哌隆（1.0微摩尔）、昂丹司琼（1.0微摩尔）或ICS 205-930（10.0微摩尔）的阻断。5. 5-HT和舒马曲坦均引起内皮依赖性舒张，对甲硫噻庚因（pA2和表观pA2值分别为8.1和8.6）、麦角苄酯（7.4和7.5）、PAPP（8.2和8.2）、育亨宾（7.1和6.8）、萝芙素（6.8和6.7）的拮抗敏感，但对育亨宾（10.0微摩尔）不敏感。6. 这些观察结果与5-HT1D受体介导的效应一致，并为不同组织和物种的内皮5-HT受体之间存在差异这一概念提供了进一步支持。
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