Martin G E, Bacino C B, Papp N L
Peptides. 1981 Summer;2(2):213-7. doi: 10.1016/s0196-9781(81)80036-8.
Methergoline, an antagonist of cerebral serotonin receptors, has been shown to significantly reduce the rise in rectal temperature (Tre) produced by the intracerebral microinjection of beta-endorphin. In this study the role of serotonin in the increase in Tre elicited by beta-endorphin was further examined using three additional serotonin antagonists. beta-Endorphin was administered twice to rats using a crossover design in which half of the animals were first pretreated with the vehicle solution and half with the antagonist. Serotonin antagonists used were: methergoline, methysergide, cinanserin and cyproheptadine. Although methergoline did cause a marked reduction in the beta-endorphin-induced rise in Tre, neither methysergide, nor cinanserin, nor cyproheptadine produced a marked reduction in the hyperthermia. Since methergoline also interacts with the dopamine receptor, the effect of a dopamine antagonist, haloperidol, on the endorphin-evoked response was also examined. Haloperidol failed to attenuate the rise in Tre. The reason for the apparent discrepancy in the action of these serotonin antagonists is unclear. Further research may reveal distinct subpopulations of serotonin receptors at which these antagonists exert differential effects.
麦角新碱是一种脑血清素受体拮抗剂,已被证明能显著降低脑室内微量注射β-内啡肽所引起的直肠温度(Tre)升高。在本研究中,使用另外三种血清素拮抗剂进一步研究了血清素在β-内啡肽引起的Tre升高中的作用。采用交叉设计对大鼠给予两次β-内啡肽,其中一半动物先用赋形剂溶液预处理,另一半先用拮抗剂预处理。所用的血清素拮抗剂有:麦角新碱、甲基麦角新碱、辛那色林和赛庚啶。虽然麦角新碱确实能显著降低β-内啡肽引起的Tre升高,但甲基麦角新碱、辛那色林和赛庚啶均未使体温过高明显降低。由于麦角新碱也与多巴胺受体相互作用,因此还研究了多巴胺拮抗剂氟哌啶醇对内啡肽诱发反应的影响。氟哌啶醇未能减弱Tre的升高。这些血清素拮抗剂作用明显差异的原因尚不清楚。进一步的研究可能会揭示这些拮抗剂发挥不同作用的不同血清素受体亚群。