Van der Vliet A, Van der Werf J F, Bast A, Timmerman H
Department of Pharmacochemistry, Subfaculty of Chemistry, Vrije Universiteit, Amsterdam, The Netherlands.
J Pharm Pharmacol. 1988 Aug;40(8):577-9. doi: 10.1111/j.2042-7158.1988.tb05308.x.
The inhibition of histamine release after depolarization of rat cerebral cortex slices by electrical stimulation and mediated by the postulated presynaptic autoreceptor (H3) depends strongly on the conditions of stimulation. Using electrically stimulated slices of the cortex a rightwards shift of the concentration-response curve of histamine (an H3 agonist) was observed on increasing the frequency of stimulation. The pA2 value of the H3 antagonist impromidine was, however, not altered at different stimulation frequencies; for a partial agonist only the maximal effect was influenced. These results indicate the existence of a receptor reserve at the H3 autoreceptor.
通过电刺激使大鼠大脑皮层切片去极化后，假定的突触前自身受体（H3）介导的组胺释放抑制作用在很大程度上取决于刺激条件。使用电刺激的皮层切片时，随着刺激频率增加，观察到组胺（一种H3激动剂）的浓度-反应曲线向右移动。然而，H3拮抗剂英普咪定的pA2值在不同刺激频率下并未改变；对于部分激动剂，仅最大效应受到影响。这些结果表明H3自身受体存在受体储备。
