Sigma, PCP, and NMDA Receptors, 133
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Pii: S0166-4328(00)00333-8
The effects of several N-methyl-D-aspartate (NMDA) receptorand sigma receptor-related compounds on the discriminative stimulus effects of phencyclidine (PCP) were examined in rats trained to discriminate PCP (1.5 mg/kg, i.p.) from saline under a two-lever fixed ratio 20 schedule of food reinforcement. PCP produced a dose-dependent increase in PCP-appropriate responding. A non-competitive NMDA r...
متن کاملThe selective sigma ligand MS-377 attenuates the blockade by phencyclidine of NMDA-induced intracellular calcium.
The role of MS-377, a novel selective sigma1 ligand currently being developed for the treatment of schizophrenia, in modulating the activities of phencyclidine (PCP) on NMDA-induced calcium increase was examined in primary cultured neocortical neurons using calcium-imaging technique combined with a confocal laser scanning microscope. PCP significantly blocked NMDA-induced increases in intracell...
متن کاملNeuroscience and the near-death experience: roles for the NMSA-PCP receptor, the sigma receptor and the endopsychosins.
The Near-Death Experience (NDE) is a dissociative mental state with characteristic features. These can be reproduced by ketamine which acts at sigma sites and blocks N-methyl-D-aspartate (NMDA) linked phencyclidine (PCP) receptors to reduce ischaemic damage. Endogenous ligands, alpha and beta-endopsychosin, have been detected for these receptors which suggests an explanation for some NDE's: the...
متن کاملThe Ketamine Analogue Methoxetamine and 3- and 4-Methoxy Analogues of Phencyclidine Are High Affinity and Selective Ligands for the Glutamate NMDA Receptor
In this paper we determined the pharmacological profiles of novel ketamine and phencyclidine analogues currently used as 'designer drugs' and compared them to the parent substances via the resources of the National Institute of Mental Health Psychoactive Drug Screening Program. The ketamine analogues methoxetamine ((RS)-2-(ethylamino)-2-(3-methoxyphenyl)cyclohexanone) and 3-MeO-PCE (N-ethyl-1-(...
متن کاملDifferential regulation of sigma and PCP receptors after chronic administration of haloperidol and phencyclidine in mice.
The existence of multiple receptor sites for the psychotomimetic agents phencyclidine (PCP) and some opiate-benzomorphans such as (+)N-allylnormetazocine ([+]SKF 10,047) in the mammalian central nervous system is well documented. These are: 1) sigma/PCP (sigma p) site, which binds both PCP and psychotomimetic opiates but not antipsychotics such as haloperidol, 2) PCP site, which selectively bin...
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تاریخ انتشار 1993