Müller-Schweinitzer E
Naunyn Schmiedebergs Arch Pharmacol. 1976;292(2):113-8. doi: 10.1007/BF00498580.
Changes in tension of spiral strips from dog saphenous, external carotid and basilar arteries were monitored isometrically. Serotonin (5-HT) contracted the 3 arterial preparations in about the same concentration range. Compared with noradrenaline (NA) (100%) the efficacy of 5-HT was about 60% on saphenous, 150% on external carotid and about 500% on basilar arteries. Ergotamine (E) stimulated the 3 vascular preparations in concentrations about 100 times lower than 5-HT. Compared with NA the efficacy of E was about 20% on saphenous, 50% on external carotid and 200% on basilar arteries. Compared with 5-HT (100%) however, E had similar constrictor activities in the 3 arteries. It seemed likely therefore that 5-HT receptors are involved in the vasoconstrictor activity of E. Evidence for this was obtained in experiments in which cyproheptadine (Cy), a 5-HT antagonist, was used. For antagonism of E concentrations of Cy about 6 times higher than those required to inhibit 5-HT were necessary, whereas for antagonism of NA about 500 times higher Cy concentrations were necessary. The results suggest that on canine arterial vascular smooth muscle the constrictor activity of E is mediated mainly through serotoninergic receptor sites.
采用等长测量法监测犬隐静脉、颈外动脉和基底动脉螺旋条带的张力变化。血清素(5-羟色胺,5-HT)在大致相同的浓度范围内使这3种动脉制剂收缩。与去甲肾上腺素(NA)(100%)相比,5-HT对隐静脉的效力约为60%,对颈外动脉为150%,对基底动脉约为500%。麦角胺(E)刺激这3种血管制剂的浓度比5-HT低约100倍。与NA相比,E对隐静脉的效力约为20%,对颈外动脉为50%,对基底动脉为200%。然而,与5-HT(100%)相比,E在这3种动脉中具有相似的收缩活性。因此,5-HT受体似乎参与了E的血管收缩活性。这一点在使用5-HT拮抗剂赛庚啶(Cy)的实验中得到了证实。对于E的拮抗作用,所需Cy的浓度比抑制5-HT所需浓度高约6倍,而对于NA的拮抗作用,所需Cy浓度则高约500倍。结果表明,在犬动脉血管平滑肌上,E的收缩活性主要通过5-羟色胺能受体位点介导。