Goldman M E, Jacobson A E, Rice K C, Paul S M
FEBS Lett. 1985 Oct 14;190(2):333-6. doi: 10.1016/0014-5793(85)81313-2.
The potency of a series of opioid and non-opioid psychotomimetic drugs to inhibit the specific binding of [3H]PCP and (+)-[3H]SKF-10,047 to rat cerebral cortical membranes was examined. (+)-PCMP, the 3-methylpiperidino analog of PCP, was a potent inhibitor of the specific binding of both ligands. All of the other 12 compounds examined, however, displayed a 3-277-fold selectivity for either [3H]PCP or (+)-[3H]SKF-10,047 binding. These results suggest that although these opioid and non-opioid psychotomimetics bind to both sites, most have significantly different affinities. The binding sites for [3H]PCP appear to be distinct from the 'sigma' binding sites labeled with (+)-[3H]SKF-10,047.
研究了一系列阿片类和非阿片类拟精神病药物抑制[3H]PCP和(+)-[3H]SKF-10,047与大鼠大脑皮层膜特异性结合的能力。(+)-PCMP是PCP的3-甲基哌啶类似物，是两种配体特异性结合的强效抑制剂。然而，所检测的其他12种化合物对[3H]PCP或(+)-[3H]SKF-10,047结合均表现出3至277倍的选择性。这些结果表明，尽管这些阿片类和非阿片类拟精神病药物都与这两个位点结合，但大多数具有明显不同的亲和力。[3H]PCP的结合位点似乎与用(+)-[3H]SKF-10,047标记的“σ”结合位点不同。
