TY - JOUR
T1 - Phencyclidine (angle dust)/σ'opiate' receptor
T2 - Visualization by tritium-sensitive film
AU - Quirion, R.
AU - Hammer, R. P.
AU - Herkenham, M.
AU - Pert, C. B.
PY - 1981
Y1 - 1981
N2 - [3H]Phencyclidine ([3H]PCP) binds specifically to an apparently single class of binding sites on slide-mounted sections of rat olfactory bulb (Kd=46 nM; Bmax=10.5 fmol per slice). Bound [3H]PCP can be displaced by nonradioactive PCP and a series of its analogs with relative potencies that correlate closely (P<0.001) with values determined in a rat discrimination test that utilized PCP as a cue. Although morphine, naloxone, and opiate peptides do not displace bound [3H]PCP, psychotomimetic benzomorphans, classed as 'σ opiates', are quite potent displacers in vitro and have PCP-like behavioral properties in vivo. These results suggest that phencyclidine and the σ opiates act at the same sites. [3H]PCP binding sites were visualized by using tritium-sensitive LKB film analyzed by computerized densitometry and color coding. The [3H]PCP binds most densely to cortical areas, diffusely in neocortex, and somewhat heterogeneously in the laminae of the hippocampal formation and dentate gyrus. Most of the brainstem and spinal cord show low specific [3H]PCP binding, with gray matter generally showing more binding than white.
AB - [3H]Phencyclidine ([3H]PCP) binds specifically to an apparently single class of binding sites on slide-mounted sections of rat olfactory bulb (Kd=46 nM; Bmax=10.5 fmol per slice). Bound [3H]PCP can be displaced by nonradioactive PCP and a series of its analogs with relative potencies that correlate closely (P<0.001) with values determined in a rat discrimination test that utilized PCP as a cue. Although morphine, naloxone, and opiate peptides do not displace bound [3H]PCP, psychotomimetic benzomorphans, classed as 'σ opiates', are quite potent displacers in vitro and have PCP-like behavioral properties in vivo. These results suggest that phencyclidine and the σ opiates act at the same sites. [3H]PCP binding sites were visualized by using tritium-sensitive LKB film analyzed by computerized densitometry and color coding. The [3H]PCP binds most densely to cortical areas, diffusely in neocortex, and somewhat heterogeneously in the laminae of the hippocampal formation and dentate gyrus. Most of the brainstem and spinal cord show low specific [3H]PCP binding, with gray matter generally showing more binding than white.
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U2 - 10.1073/pnas.78.9.5881
DO - 10.1073/pnas.78.9.5881
M3 - Article
C2 - 6272322
AN - SCOPUS:0019619625
SN - 0027-8424
VL - 78
SP - 5881
EP - 5885
JO - Proceedings of the National Academy of Sciences of the United States of America
JF - Proceedings of the National Academy of Sciences of the United States of America
IS - 9 II
ER -