Autoradiographic study on the pharmacological characteristics of [3H]3-OH-PCP binding sites in rat brain

Toshihito Suzuki, Toshifumi Yamamoto, Takafumi Hori, Atsuomi Baba, Hiroyasu Shiraishi, Takehiko Ito, John E. Piletz, Ing Kang Ho

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Abstract

The pharmacological characteristics and the regional distribution of [3H]3-OH-PCP (1-[1(3-hydroxyphenyl)-cyclohexyl)piperidine) binding were investigated in rat brain by quantitative autoradiography. Kinetic analysis of [3H]3-OH-PCP binding revealed fast and slow components, in the association and dissociation studies. The regional distribution of binding closely corresponded to those of binding sites labeled by [3H]N-[1-(2-thienyl)-cyclohexyl]3,4-piperidine (TCP) and [3H](+)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten- 5,10-imine maleate (MK 801). High densities of [3H]3-OH-PCP binding sites were found in the stratum radiatum and oriens of field CA1 in the hippocampus and in the outer layers of cerebral cortices. In contrast, low levels of binding were seen in the brain stem and the granular cell layer of the cerebellum. [3H]3-OH-PCP binding was strongly inhibited by MK 801 and 3-OH-PCP, while the potency of (+)-SKF 10047 in inhibiting [3H]3-OH-PCP binding was less in the cerebral cortex and hippocampus. The antagonists for the glutamate, glycine and polyamine recognition sites at the NMDA/PCP receptor complex displaced [3H]3-OH-PCP binding sites with a potency similar to that of [3H]MK 801. These findings suggest that the [3H]3-OH-PCP binding site is similar or identical to the PCP binding site labeled by [3H]TCP and [3H]MK 801.

Original languageEnglish
Pages (from-to)243-255
Number of pages13
JournalEuropean Journal of Pharmacology
Volume310
Issue number2-3
DOIs
Publication statusPublished - Aug 29 1996
Externally publishedYes

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Keywords

  • 3-OH-PCP (1-[1(3-hydroxyphenyl)-cyclohexyl]piperidine)
  • Autoradiography
  • Brain, rat
  • NMDA receptor
  • Phencyclidine

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Pharmacology

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