Characterization of specific sigma opiate/phencyclidine (PCP)-binding sites in the human brain

Ratna Sircar, Stephen R. Zukin

Research output: Contribution to journalArticlepeer-review

21 Scopus citations


Specific [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.

Original languageEnglish (US)
Pages (from-to)259-262
Number of pages4
JournalLife Sciences
Issue numberSUPPL. 1
StatePublished - 1983
Externally publishedYes

ASJC Scopus subject areas

  • Pharmacology


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