Landwehrmeyer B, Mengod G, Palacios J M
Department of Pathology, University of Basel, Switzerland.
Brain Res Mol Brain Res. 1993 Apr;18(1-2):187-92. doi: 10.1016/0169-328x(93)90188-u.
Dopamine D3 receptors (Sokoloff et al., 1990) have been shown to be related to dopamine D2 receptors and have been suggested to play a role in mediating the antipsychotic effects of neuroleptics. So far studies on the expression of D3 mRNA and of binding sites with pharmacological characteristics of D3 receptors have been restricted to rat brain. Using in situ hybridization histochemistry, we demonstrate that D3 mRNAs are enriched in human n, accumbens and in the islands of Calleja. In addition, D3 mRNA was detected at very low levels in anterior caudate and putamen with a rostro-caudally decreasing gradient and in hypothalamic mammillary nuclei. In receptor autoradiographic binding studies, the islands of Calleja were found to be labeled by [125I]iodosulpride and [3H]CV 205 502 but not by [3H]raclopride and [3H]YM 09151-2. Pharmacological analysis of binding of the D2/D3 ligand [3H]CV 205 502 in n. accumbens and caudate-putamen is consistent with the presence of D3 receptor sites in ventral striatum. Overall distribution and pharmacology of D3 sites in human and rat brain appear to be similar. Presence and distribution of D3 receptors in human brain are compatible with the notion that D3 receptors might be involved in mediating the clinical effects of antipsychotics.
多巴胺D3受体（索科洛夫等人，1990年）已被证明与多巴胺D2受体相关，并被认为在介导抗精神病药物的抗精神病作用中发挥作用。到目前为止，关于D3 mRNA表达以及具有D3受体药理学特性的结合位点的研究仅限于大鼠脑。通过原位杂交组织化学，我们证明D3 mRNA在人类伏隔核和Calleja岛中富集。此外，在尾状核前部和壳核中检测到极低水平的D3 mRNA，其从嘴侧到尾侧呈递减梯度，在下丘脑乳头体核中也有检测到。在受体放射自显影结合研究中，发现Calleja岛被[125I]碘舒必利和[3H]CV 205 502标记，但未被[3H]雷氯必利和[3H]YM 09151 - 2标记。对伏隔核和尾状核 - 壳核中D2/D3配体[3H]CV 205 502结合的药理学分析与腹侧纹状体中存在D3受体位点一致。人类和大鼠脑中D3位点的总体分布和药理学似乎相似。人类脑中D3受体的存在和分布与D3受体可能参与介导抗精神病药物临床作用的观点相符。
