Gundlach A L, McDonald D, Beart P M
J Neurochem. 1982 Sep;39(3):890-4. doi: 10.1111/j.1471-4159.1982.tb07978.x.
The binding of [3H]spiperone, a neuroleptic/dopamine receptor ligand, to membranes of the ventral tegmental area of the rat was studied in vitro and found to be rapid, saturable, reversible, and of high affinity. Specific binding was displaced by the dopaminergic agonists dopamine, apomorphine, and 2-amino-6,7-dihydroxytetralin, and stereospecifically by the neuroleptic drugs butaclamol and flupenthixol. Bromocryptine and other ergots displaced the binding, as did the D-2 antagonists domperidone, molindone, metoclopramide, and sulpiride. Noradrenergic, histaminergic, and serotonergic components of the binding were not detected in displacement studies with various agonists and antagonists. These data are consistent with the hypothesis that [3H]spiperone labels dopamine receptors in the ventral tegmental area that are not linked to adenylate cyclase and are therefore likely to be of the D-2 type.
在体外研究了神经安定药/多巴胺受体配体[3H]螺哌隆与大鼠腹侧被盖区膜的结合,发现其结合迅速、可饱和、可逆且具有高亲和力。多巴胺能激动剂多巴胺、阿扑吗啡和2-氨基-6,7-二羟基四氢萘可取代特异性结合,而神经安定药布他拉莫和氟哌噻吨可立体特异性地取代。溴隐亭和其他麦角生物碱可取代该结合,D-2拮抗剂多潘立酮、莫林酮、甲氧氯普胺和舒必利也可如此。在用各种激动剂和拮抗剂进行的置换研究中,未检测到结合的去甲肾上腺素能、组胺能和5-羟色胺能成分。这些数据与以下假设一致,即[3H]螺哌隆标记腹侧被盖区中与腺苷酸环化酶不相关的多巴胺受体,因此可能是D-2型受体。