Chivers J K, Hall M D, Kelly E, Jenner P, Marsden C D
J Pharm Pharmacol. 1984 Jul;36(7):484-8. doi: 10.1111/j.2042-7158.1984.tb04434.x.
Following intravenous administration of [3H]spiperone or [3H]N,n-propylnorapomorphine (NPA) to rats, radioactivity derived from the ligands accumulated in the striatum and superior colliculus when compared with cerebellar levels. The accumulation of [3H]spiperone in both areas was prevented by intraperitoneal administration of (+)-butaclamol, haloperidol and sulpiride but not by (-)-butaclamol, cinanserin, propranolol or prazosin. The accumulation of [3H]NPA was prevented by administration of (+)-butaclamol, haloperidol and apomorphine but not by (-)-butaclamol. In in-vitro experiments, membrane preparations from the superior colliculus showed a small number of specific binding sites for both [3H]spiperone and [3H]NPA. The dissociation constant (KD) for [3H]NPA was not different from that for striatal preparations but that for [3H]spiperone was 10-fold higher. We conclude that dopamine receptors may be present within the superior colliculus.
给大鼠静脉注射[3H]司哌啶酮或[3H]N,N-丙基去甲阿扑吗啡(NPA)后,与小脑水平相比,来自配体的放射性在纹状体和上丘中积累。腹腔注射(+)-布他拉莫、氟哌啶醇和舒必利可阻止[3H]司哌啶酮在这两个区域的积累,但(-)-布他拉莫、西那色林、普萘洛尔或哌唑嗪则不能。(+)-布他拉莫、氟哌啶醇和阿扑吗啡可阻止[3H]NPA的积累,但(-)-布他拉莫则不能。在体外实验中,上丘的膜制剂显示出少量[3H]司哌啶酮和[3H]NPA的特异性结合位点。[3H]NPA的解离常数(KD)与纹状体制剂的解离常数无差异,但[3H]司哌啶酮的解离常数高10倍。我们得出结论,上丘内可能存在多巴胺受体。