Multiple mode of binding of phencyclidines: High affinity association between phencyclidine receptors in rat brain and a monovalent ion-sensitive polypeptide

作者: Rachel Haring , Yoel Kloog , Na-ava harshak-Felixbrodt , Mordechai Sokolovsky

DOI: 10.1016/0006-291X(87)90303-2

关键词: HippocampusCerebrumPhencyclidineLigand (biochemistry)ChemistryStereochemistryPiperidineBinding siteReceptorIn vitroBiophysicsCell biologyBiochemistryMolecular biology

摘要: Two populations of phencyclidine (PCP) binding sites are shown to exist in the rat brain: a high-affinity monovalent ion-sensitive site (Kd 10-14 nM for [3H]TCP, [3H]N-[1-(2-thienyl)cyclohexyl]piperidine), which exists both frontal cortex and hippocampus, lower affinity 80-130 [3H]TCP) is found hippocampus but not cortex. The nature interactions between ion-binding high PCP receptors depend on ligand structure (PCP or TCP) ion involved (K' Na'). associated with an Mr 90,000 polypeptide whose labeling by [3H]azido selectively inhibited ions.

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