McCarthy B G, Peroutka S J
Headache. 1989 Jul;29(7):420-2. doi: 10.1111/j.1526-4610.1989.hed2907420.x.
The potency of dihydroergotamine (DHE) was determined at 13 neurotransmitter receptors using radioligand binding techniques. DHE is a potent agent (i.e. affinity value less than 100 nM) at 5-hydroxytryptamine1A (5-HT1A), 5-HT1C, 5-HT1D, 5-HT2, dopamine2, alpha1- and alpha2-adrenergic binding sites. DHE displays moderate affinity (i.e. affinity values = 100 - 1000 nM) for beta-adrenergic and dopamine1 sites and is completely inactive at 5-HT3, muscarinic and benzodiazepine receptors. These results were then compared to similar data on sumatriptan (formerly called GR 43175), a novel acute anti-migraine agent. The only pharmacological property shared by both agents is high affinity for 5-HT1D and 5-HT1A receptors. Therefore, these data suggest that 5-HT1D and/or 5-HT1A receptors may play an important role in the pathophysiology of migraine.
采用放射性配体结合技术，在13种神经递质受体上测定了双氢麦角胺（DHE）的效价。DHE在5-羟色胺1A（5-HT1A）、5-HT1C、5-HT1D、5-HT2、多巴胺2、α1和α2肾上腺素能结合位点上是一种强效剂（即亲和力值小于100 nM）。DHE对β肾上腺素能和多巴胺1位点表现出中等亲和力（即亲和力值=100 - 1000 nM），而在5-HT3、毒蕈碱和苯二氮卓受体上则完全无活性。然后将这些结果与新型急性抗偏头痛药物舒马曲坦（原称GR 43175）的类似数据进行比较。两种药物唯一共有的药理学特性是对5-HT1D和5-HT1A受体具有高亲和力。因此，这些数据表明5-HT1D和/或5-HT1A受体可能在偏头痛的病理生理学中起重要作用。
