Hall M D, Jenner P, Kelly E, Marsden C D
Br J Pharmacol. 1983 Jun;79(2):599-610. doi: 10.1111/j.1476-5381.1983.tb11035.x.
Specific [3H]-spiperone and [3H]-N,n-propylnorapomorphine (NPA) binding was measured in striatum and substantia nigra of the rat following unilateral 6-hydroxydopamine (6-OHDA) lesions of the medial forebrain bundle, kainic acid lesions of the substantia nigra or striatum, and following decortication. Binding sites labelled by [3H]-spiperone in striatum were found to lie on striatal cell bodies and on the terminals of cortico-striate glutamate fibres, but not on presynaptic dopamine terminals. In contrast, binding sites labelled by [3H]-NPA were demonstrated on striatal cell bodies and on the terminals of nigro-striata dopamine fibres, but not on cortical afferents. In substantia nigra, specific [3H]-spiperone binding sites were found only on non-dopamine cell bodies. No clear evidence was found for their existence on dopamine cell bodies, the terminals of strio-nigral fibres or the terminals of cortico-nigral fibres. In contrast, specific binding sites for [3H]-NPA were found on dopamine cell bodies and the terminals of strio-nigral fibres. Localization on non-dopamine cell bodies or on cortico-nigral fibres was not demonstrated. These studies support the concept of differential localization of agonist and antagonist binding sites.
在大鼠内侧前脑束单侧6-羟基多巴胺（6-OHDA）损伤、黑质或纹状体的 kainic 酸损伤以及去皮质后，测定了纹状体和黑质中特异性[3H]-螺哌隆和[3H]-N，N-丙基去甲阿扑吗啡（NPA）的结合情况。发现纹状体中由[3H]-螺哌隆标记的结合位点位于纹状体细胞体和皮质-纹状体谷氨酸纤维的终末，但不在突触前多巴胺终末上。相比之下，由[3H]-NPA标记的结合位点在纹状体细胞体和黑质-纹状体多巴胺纤维的终末上得到证实，但不在皮质传入纤维上。在黑质中，特异性[3H]-螺哌隆结合位点仅在非多巴胺细胞体上发现。在多巴胺细胞体、纹状体-黑质纤维的终末或皮质-黑质纤维的终末上未发现其存在的明确证据。相比之下，在多巴胺细胞体和纹状体-黑质纤维的终末上发现了[3H]-NPA的特异性结合位点。未证实其在非多巴胺细胞体或皮质-黑质纤维上的定位。这些研究支持激动剂和拮抗剂结合位点差异定位的概念。
