Beart P M, McDonald D, Cincotta M, de Vries D J, Gundlach A L
Gen Pharmacol. 1986;17(1):57-62. doi: 10.1016/0306-3623(86)90011-x.
The affinities of several ergot derivatives for 5-HT1 and 5-HT2 receptors were evaluated using [3H]5-HT and [3H]mianserin, and membranes prepared from rat frontal cortex. CQ 32-084, which had a Ki value against the 5-HT2 component of [3H]mianserin binding of 9 nM, had little effect on [3H]5-HT binding and was selective for the 5-HT2 receptor. Lisuride and LY-158A also displayed preferential affinity for the 5-HT2 receptor. Dihydroergocryptine, CM 29-712, lergotrile and LY-062 were more selective for the 5-HT1 receptor. Bromocriptine showed little selectivity for either subtype. Overall, the ergot derivatives displayed markedly different affinities and selectivities for central 5-HT receptors suggesting that their serotonergic actions should be considered when evaluating their pharmacological spectrum of activity.
利用[3H]5-羟色胺（5-HT）和[3H]米安色林，并使用从大鼠额叶皮质制备的膜，评估了几种麦角衍生物对5-HT1和5-HT2受体的亲和力。CQ 32-084对[3H]米安色林结合的5-HT2成分的Ki值为9 nM，对[3H]5-HT结合几乎没有影响，且对5-HT2受体具有选择性。利舒脲和LY-158A也对5-HT2受体表现出优先亲和力。双氢麦角隐亭、CM 29-712、麦角腈和LY-062对5-HT1受体更具选择性。溴隐亭对两种亚型均无明显选择性。总体而言，麦角衍生物对中枢5-HT受体表现出明显不同的亲和力和选择性，这表明在评估其药理活性谱时应考虑它们的5-羟色胺能作用。
