Characterization of specific sigma opiate/phencyclidine (PCP)-binding sites in the human brain
1983; Elsevier BV; Volume: 33; Linguagem: Inglês
10.1016/0024-3205(83)90492-7
ISSN1879-0631
AutoresRatna Sircar, Stephen R. Zukin,
Tópico(s)Neuropeptides and Animal Physiology
ResumoSpecific [3H]phencyclidine (PCP)-binding studies were carried out in homogenates prepared from different regions of post-mortem human brains derived from subjects free of any neurological disease. Scatchard analysis revealed a single class of [3H]PCP-binding sites. Binding was found to be stereospecific i.e. markedly greater ability of the potent PCP agonist dexoxadrol to displace specifically bound 10 nM [3H]PCP as compared to its behaviorally inactive enantiomer levoxadrol. Stereospecific binding was abolished by preincubation of homogenate with trypsin or by heating the homogenate to 90°C for 15 min. Various sigma opiates displaced specifically bound [3H]PCP binding in a rank order similar to that seen in rat brain. Thus a baseline has been established to enable future elucidation of the possible role of these sites in psychiatric illnesses.
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