Miyamoto A, Obi T, Nishio A
Department of Veterinary Pharmacology, Faculty of Agriculture, Kagoshima University, Japan.
Vet Res Commun. 1996;20(1):61-70. doi: 10.1007/BF00346578.
The vasomotor effects of 5-hydroxytryptamine (5-HT) on isolated equine basilar arteries were studied. 5-HT induced contractions of equine basilar arteries in a concentration-dependent manner, with a pEC50 value (with 95% confidence limits) of 7.35 (7.08-7.62). Similar results were obtained with endothelium-denuded basilar arteries. Contractions were not competitively inhibited by the 5-HT2 receptor antagonist ketanserin at low concentrations of 5-HT. Conversely, at high concentrations of 5-HT, contractions were inhibited by ketanserin in a concentration-dependent manner, with a pA2 value of 8.91 (8.62-9.20). The 5-HT1 and 5-HT2 receptor antagonist methiothepin shifted the concentration-response curve of 5-HT downwards and to the right in a concentration-dependent manner. In the presence of 10(-6) mol/L ketanserin, however, methiothepin antagonized 5-HT-induced contractions competitively with a pA2 value of 7.95 (7.59-8.31). The 5-HT3 receptor antagonist MDL 72222 had no effect on 5-HT-induced contractions. The findings of this study indicate that 5-HT1 and 5-HT2 receptors are located in equine basilar arterial smooth muscle cells, and that stimulation of these receptors results in contraction.
研究了5-羟色胺(5-HT)对离体马基底动脉的血管舒缩作用。5-HT以浓度依赖性方式诱导马基底动脉收缩,其pEC50值(95%置信限)为7.35(7.08 - 7.62)。内皮剥脱的基底动脉也得到类似结果。在低浓度5-HT时,5-HT2受体拮抗剂酮色林对收缩无竞争性抑制作用。相反,在高浓度5-HT时,酮色林以浓度依赖性方式抑制收缩,pA2值为8.91(8.62 - 9.20)。5-HT1和5-HT2受体拮抗剂美噻吨以浓度依赖性方式使5-HT的浓度 - 反应曲线向下和向右移动。然而,在存在10(-6)mol/L酮色林的情况下,美噻吨以pA2值7.95(7.59 - 8.31)竞争性拮抗5-HT诱导的收缩。5-HT3受体拮抗剂MDL 72222对5-HT诱导的收缩无影响。本研究结果表明,5-HT1和5-HT2受体位于马基底动脉平滑肌细胞中,刺激这些受体可导致收缩。