Phencyclidine decreases binding capacity of serotonin2 receptor in vitro

T. Nabeshima, Y. Noda, H. Furukawa, T. Kameyama

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16 Citations (Scopus)


We have investigated that effects of phencyclidine (PCP) on [3H]-spiperone binding to synaptic membrane in the presence of sulpiride to distinguish serotonin (5-HT2) receptor from dopamine2 receptor. The amount of [3H]-spiperone specific binding was larger in the frontal and occipital cortices than in other areas. PCP strongly inhibited the [3H]spiperone binding at the concentration of 20 nM. Mescaline also weakly inhibited that, but not other hallucinogenic reagents such as methamphetamine, cyclazocine, scopolamine and atropine at the same concentration. In the presence of 20 n3M PCP a significant decrease of Bmax and no change of Kd in the [3H]-spiperone specific binding was observed. Present results are consistent with the hypothesis that PCP may be a potent and selective agonist at 5-HT2 binding sites. Although PCP known as hallucinogen interacts strongly with 5-HT2 receptor, it is still too premature to draw any conclusions regarding a possible relationship between 5-HT binding and hallucinogenic potency.

Original languageEnglish
Pages (from-to)175-186
Number of pages12
JournalResearch Communications in Substances of Abuse
Issue number3
Publication statusPublished - 1984
Externally publishedYes

All Science Journal Classification (ASJC) codes

  • Medicine (miscellaneous)


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