Walker J M, Bowen W D, Goldstein S R, Roberts A H, Patrick S L, Hohmann A G, DeCosta B
Department of Psychology, Brown University Providence, RI 02912.
Brain Res. 1992 May 22;581(1):33-8. doi: 10.1016/0006-8993(92)90340-f.
Binding studies suggested the selectivity of (+)-pentazocine for sigma receptors, and subsequent synthesis and testing of 3H-pentazocine confirmed its high potency and selectivity for sigma sites. Newer data have demonstrated the selectivity of (+)-pentazocine for a subtype of the sigma receptor called sigma-1. Based on these findings, the distribution of 3H-pentazocine binding sites in the guinea pig brain was examined using in vitro autoradiography. 3H-Pentazocine binding was high in the cingulate cortex, dorsal diagonal band, periaqueductal gray, cerebellum and cranial nerve nuclei. It was relatively low in the nucleus accumbens, neocortical areas and caudate nucleus. A significant correlation was found between the binding of 3H-pentazocine and [3H]1,3-di-o-tolylguanidine, a selective sigma ligand across brain regions. However, certain nuclei exhibited markedly different ratios of binding of the two ligands. Since DTG is not selective for the sigma subtypes, while (+)-pentazocine is selective for the sigma-1 type, the data are suggestive of relative differences in the distributions of sigma-1 and sigma-2 sites.
结合研究表明（+）-喷他佐辛对σ受体具有选择性，随后对[3H]（+）-喷他佐辛的合成与测试证实了其对σ位点具有高效能和选择性。最新数据表明（+）-喷他佐辛对一种名为σ-1的σ受体亚型具有选择性。基于这些发现，利用体外放射自显影技术检测了豚鼠脑中[3H]（+）-喷他佐辛结合位点的分布。[3H]（+）-喷他佐辛在扣带回皮质、斜角带核、导水管周围灰质、小脑和脑神经核中的结合水平较高。在伏隔核、新皮质区域和尾状核中结合水平相对较低。发现在脑区中，[3H]（+）-喷他佐辛与[3H]1,3-二邻甲苯基胍（一种选择性σ配体）的结合之间存在显著相关性。然而，某些核团中两种配体的结合比例存在明显差异。由于DTG对σ亚型不具有选择性，而（+）-喷他佐辛对σ-1型具有选择性，这些数据提示了σ-1和σ-2位点分布的相对差异。
