用[3H]叠氮苯环己哌啶进行光亲和标记揭示的大鼠脑苯环己哌啶（PCP）受体的区域异质性。

Regional heterogeneity of rat brain phencyclidine (PCP) receptors revealed by photoaffinity labeling with [3H] azido phencyclidine.

作者信息

Haring R, Kloog Y, Sokolovsky M

出版信息

Biochem Biophys Res Commun. 1985 Sep 30;131(3):1117-23. doi: 10.1016/0006-291x(85)90206-2.

Abstract

Photoaffinity labeling of rat brain phencyclidine (PCP) receptors with [3H] azido phencyclidine ([3H]AZ-PCP) reveals the existence of five polypeptides which are specifically labeled by the affinity probe (Mr's 90,000, 62,000, 49,000, 40,000 and 33,000). These labeled components are unevenly distributed in rat brain. In the frontal cortex, thalamus and olfactory bulb, the major bands labeled are the Mr's 90 K and 62 K polypeptides; in the cerebellum most of the labeling is in the 90 K and 33 K bands; and in the hippocampus all but the Mr 40 K band are heavily labeled. Together with dexoxadrol/[3H]PCP competition binding data, which indicated the existence of high and low affinity dexoxadrol/PCP binding sites, these results suggest regional heterogeneity of PCP receptors. The regional distribution of the high affinity dexoxadrol binding sites correlates best with that of the Mr 90 K polypeptide.

摘要

用[3H]叠氮苯环己哌啶（[3H]AZ - PCP）对大鼠脑苯环己哌啶（PCP）受体进行光亲和标记，发现存在5种被亲和探针特异性标记的多肽（分子量分别为90,000、62,000、49,000、40,000和33,000）。这些被标记的成分在大鼠脑中分布不均。在额叶皮质、丘脑和嗅球中，主要被标记的条带是分子量为90K和62K的多肽；在小脑中，大部分标记位于90K和33K条带；而在海马体中，除了40K条带外，其他条带均被大量标记。结合脱氧羟哌替啶/[3H]PCP竞争结合数据（该数据表明存在高亲和力和低亲和力的脱氧羟哌替啶/PCP结合位点），这些结果提示PCP受体存在区域异质性。高亲和力脱氧羟哌替啶结合位点的区域分布与90K多肽的区域分布相关性最佳。