Paiva M Q, Caramona M M, Osswald W
Laboratório de Farmacologia, Faculdade de Medicina, Porto, Portugal.
Naunyn Schmiedebergs Arch Pharmacol. 1988 Dec;338(6):616-22. doi: 10.1007/BF00165625.
The prejunctional and postjunctional 5-HT receptors of the canine saphenous vein were studied. The release of 3H-noradrenaline (3H-NA) from incubated saphenous vein strips was inhibited by 5-hydroxytryptamine (5-HT) in a concentration-dependent way (5-HT concentrations: 0.01, 0.1 and 1.0 mumol.l-1), but not by the selective 5-HT1A agonist 8-hydroxy-dipropylaminotetralin (8-OH-DPAT; 1 and 10 mumol.l-1). The inhibitory effect of 5-HT was antagonized by metitepine and methysergide, but not by yohimbine, (-)-pindolol or ketanserin. In strips preincubated with 5-HT (1.2 mumol.l-1), the fractional release of 3H-NA was slightly reduced (paired experiments). 5-HT and 8-OH-DPAT caused concentration-dependent contractions of the saphenous smooth muscle. A parallel shift of the concentration-response curve for 8-OH-DPAT to the right was caused by metitepine and yohimbine, but not by ketanserin. The contractions caused by 5-HT were antagonized by metitepine and yohimbine (parallel displacement of the curves to the right), as well as by ketanserin and methysergide (with a depression of the upper part of the curve). Blockade of alpha-adrenoceptors (due to prazosin plus a low concentration of yohimbine) also resulted in a weak antagonistic effect. Ketanserin and metitepine displaced the noradrenaline concentration-response curve to the right. We conclude that the saphenous vein of the dog is endowed with prejunctional receptors of the 5-HT1 type which can not be classified as belonging either to the 1A or 1B subtype; and that at the postjunctional level 5-HT1 (possibly of the 1D subtype) and 5-HT2 receptors are present.(ABSTRACT TRUNCATED AT 250 WORDS)
对犬隐静脉的节前和节后5-羟色胺(5-HT)受体进行了研究。孵育的隐静脉条带中3H-去甲肾上腺素(3H-NA)的释放受到5-羟色胺(5-HT)浓度依赖性抑制(5-HT浓度:0.01、0.1和1.0μmol·l-1),但不受选择性5-HT1A激动剂8-羟基-二丙基氨基四氢萘(8-OH-DPAT;1和10μmol·l-1)的抑制。5-HT 的抑制作用被甲替平(metitepine)和麦角新碱(methysergide)拮抗,但不被育亨宾(yohimbine)、(-)-吲哚洛尔(pindolol)或酮色林(ketanserin)拮抗。在预先用5-HT(1.2μmol·l-1)孵育的条带中,3H-NA的分数释放略有降低(配对实验)。5-HT和8-OH-DPAT引起隐静脉平滑肌的浓度依赖性收缩。甲替平和育亨宾使8-OH-DPAT的浓度-反应曲线平行右移,但酮色林未使其右移。5-HT引起的收缩被甲替平和育亨宾(曲线平行右移)以及酮色林和麦角新碱(曲线上部压低)拮抗。α-肾上腺素能受体阻断(由于哌唑嗪加低浓度育亨宾)也产生微弱的拮抗作用。酮色林和甲替平使去甲肾上腺素浓度-反应曲线右移。我们得出结论,犬隐静脉具有5-HT1型节前受体,不能归类为1A或1B亚型;在节后水平存在5-HT1(可能是1D亚型)和5-HT2受体。(摘要截短于250字)