Smith C F, Rowland P B
Department of Biology, Reckitt & Colman plc, Hull, North Humberside, England.
Arch Int Pharmacodyn Ther. 1989 May-Jun;299:144-54.
We have investigated the effects of dopamine on the response of the mouse isolated vas deferens to electrical stimulation and, contrary to previous investigators, have found that there are specific dopamine receptors present in this tissue. A range of dopamine antagonists have been examined vs the effects of dopamine and the Ke values obtained indicate that the receptor present is of the DA2 subtype. Domperidone, spiperone and haloperidol possess a very high affinity for the receptor, whereas the selective DA1-antagonist SCH 23390 has only low affinity. Bromocriptine was found to possess both alpha 2- and dopamine agonist activity in this preparation and it is also possible to demonstrate dopamine agonist activity of noradrenaline. In the presence of alpha 2-antagonists, the mouse vas deferens is an extremely simple preparation suitable for the rapid screening of compounds for DA2-agonist or antagonist activity.
我们研究了多巴胺对小鼠离体输精管电刺激反应的影响,与之前的研究者不同,我们发现该组织中存在特定的多巴胺受体。已检测了一系列多巴胺拮抗剂对多巴胺作用的影响,所得的Ke值表明存在的受体为DA2亚型。多潘立酮、螺哌隆和氟哌啶醇对该受体具有非常高的亲和力,而选择性DA1拮抗剂SCH 23390只有低亲和力。在该制剂中发现溴隐亭同时具有α2和多巴胺激动剂活性,并且也有可能证明去甲肾上腺素的多巴胺激动剂活性。在存在α2拮抗剂的情况下,小鼠输精管是一种极其简单的制剂,适用于快速筛选具有DA2激动剂或拮抗剂活性的化合物。