Pharmacokinetic and pharmacodynamic properties of some phencyclidine analogs in rats

Arthur K. Cho, Hiramatsu Masayuki Hiramatsu, Debra A. Schmitz, Nabeshima Toshitaka Nabeshima, Kameyama Tsutomu Kameyama

研究成果: Article査読

10 被引用数 (Scopus)

抄録

The pharmacodynamics and pharmacokinetics of three phencyclidine analogs, differing from phencyclidine (PCP) only in the nature of the amine structure, were determined after intravenous doses of equimolar amounts to rats. The purpose of the study was to assess the role of pharmacokinetics in the in vivo potency of the compounds. The compounds examined were phenylcyclohexyl-pyrrolidine (PCPY), diethylamine (PCDE), ethylamine (PCE), and phencyclohexylamine (PCA). The behavior responses monitored included ataxia and others previously shown to be characteristic of PCP. In contrast to their relative affinities for the MK 801 binding site, the behavioral potencies of PCE, PCDE and PCPY were comparable to PCP. The major discrepancy occurred with PCDE, whose affinity for the NMDA receptor was 1 2th of PCP. The pharmacokinetic studies showed that the discrepancy between in vivo and in vitro activity of PCDE could be partially accounted for by its conversion to PCE, a relatively potent PCP-like agent.

本文言語English
ページ(範囲)947-953
ページ数7
ジャーナルPharmacology, Biochemistry and Behavior
39
4
DOI
出版ステータスPublished - 08-1991

All Science Journal Classification (ASJC) codes

  • 生化学
  • 毒物学
  • 薬理学
  • 臨床生化学
  • 生物学的精神医学
  • 行動神経科学

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