Spano P F, Trabucchi M
Gerontology. 1978;24 Suppl 1:106-14. doi: 10.1159/000212304.
Various ergot alkaloids and derivatives were investigated for their interaction with dopaminergic receptors at the level of the rat corpus striatum and nucleus accumbens. Dihydro(DH)-ergotoxine, DH-ergocornine, DH-ergocryptine, DH-ergocristine, 2-Br-alpha-ergocryptine, ergotamine and DH-ergotamine were shown to inhibit, at micromolar concentrations, the dopamine-stimulated adenylate cyclase activity of rat striatal and nucleus accumbens homogenates. Interestingly, the inhibitory effect of the ergot drugs was higher in the nucleus accumbens than in the striatum. Moreover, the ergot drugs were more active in displacing 3H-haloperidol than 3H-dopamine from striatal membranes. The results, which are in apparent contradiction with previously obtained behavioral, pharmacological and clinical data, are discussed in the light of the possible presence in the central nervous system of distinct dopaminergic receptors with different conformations.
研究了多种麦角生物碱及其衍生物在大鼠纹状体和伏隔核水平与多巴胺能受体的相互作用。已表明，二氢（DH）-麦角隐亭、DH-麦角柯宁、DH-麦角环肽、DH-麦角克碱、2-溴-α-麦角隐亭、麦角胺和DH-麦角胺在微摩尔浓度下可抑制大鼠纹状体和伏隔核匀浆中多巴胺刺激的腺苷酸环化酶活性。有趣的是，麦角药物在伏隔核中的抑制作用高于纹状体。此外，麦角药物从纹状体膜上置换3H-氟哌啶醇比置换3H-多巴胺更有效。鉴于中枢神经系统中可能存在不同构象的不同多巴胺能受体，对这些结果进行了讨论，这些结果与先前获得的行为、药理学和临床数据明显矛盾。
