Byrd J C, Bykov V, Rothman R B
Department of Psychiatry, University of Pittsburgh, Pennsylvania 15213.
Neuropeptides. 1987 Aug-Sep;10(2):201-5. doi: 10.1016/0143-4179(87)90022-9.
Phencyclidine (PCP) is a widely abused drug of the arylcyclohexylamine class which is capable of producing symptoms of acute psychosis in man. PCP interacts with a specific CNS receptor, for which a putative endogenous peptide ligand has been identified. We have investigated whether PCP receptor binding parameters are modulated by activity in central opiate pathways. We have found that chronic administration of both an opiate agonist (etonitazene) and an opiate antagonist (naloxone) are able to decrease the affinity of the PCP receptor for TCP, a thienyl derivative of PCP. Furthermore, naloxone, but not etonitazene, resulted in a significant increase in the Bmax of TCP binding to the PCP receptor. These results suggest that neural activity mediated by CNS opioids systems is capable of affecting the binding parameters of the PCP receptor.
苯环己哌啶（PCP）是一种被广泛滥用的芳基环己胺类药物，它能够在人体中产生急性精神病症状。PCP与一种特定的中枢神经系统（CNS）受体相互作用，已鉴定出一种假定的内源性肽配体。我们研究了PCP受体结合参数是否受中枢阿片途径活性的调节。我们发现，长期给予阿片激动剂（依托尼嗪）和阿片拮抗剂（纳洛酮）均能降低PCP受体对TCP（PCP的噻吩基衍生物）的亲和力。此外，纳洛酮而非依托尼嗪导致TCP与PCP受体结合的最大结合容量（Bmax）显著增加。这些结果表明，中枢神经系统阿片系统介导的神经活动能够影响PCP受体的结合参数。
