Pharmacokinetic and pharmacodynamic properties of some phencyclidine analogs in rats

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

Research output: Contribution to journalArticle

8 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)947-953
Number of pages7
JournalPharmacology, Biochemistry and Behavior
Volume39
Issue number4
DOIs
Publication statusPublished - 01-01-1991
Externally publishedYes

Fingerprint

Pharmacodynamics
Phencyclidine
Pharmacokinetics
Rats
Dizocilpine Maleate
Ataxia
N-Methyl-D-Aspartate Receptors
Amines
Binding Sites
diethylamine
ethylamine
2,2',4,4',5-pentachlorodiphenyl ether
pyrrolidine

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Toxicology
  • Pharmacology
  • Clinical Biochemistry
  • Biological Psychiatry
  • Behavioral Neuroscience

Cite this

Cho, Arthur K. ; Masayuki Hiramatsu, Hiramatsu ; Schmitz, Debra A. ; Nabeshima, Toshitaka ; Tsutomu Kameyama, Kameyama. / Pharmacokinetic and pharmacodynamic properties of some phencyclidine analogs in rats. In: Pharmacology, Biochemistry and Behavior. 1991 ; Vol. 39, No. 4. pp. 947-953.
@article{b41c1575f6f44c27b88566f5f9861e00,
title = "Pharmacokinetic and pharmacodynamic properties of some phencyclidine analogs in rats",
abstract = "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.",
author = "Cho, {Arthur K.} and {Masayuki Hiramatsu}, Hiramatsu and Schmitz, {Debra A.} and Toshitaka Nabeshima and {Tsutomu Kameyama}, Kameyama",
year = "1991",
month = "1",
day = "1",
doi = "10.1016/0091-3057(91)90058-A",
language = "English",
volume = "39",
pages = "947--953",
journal = "Pharmacology Biochemistry and Behavior",
issn = "0091-3057",
publisher = "Elsevier Inc.",
number = "4",

}

Pharmacokinetic and pharmacodynamic properties of some phencyclidine analogs in rats. / Cho, Arthur K.; Masayuki Hiramatsu, Hiramatsu; Schmitz, Debra A.; Nabeshima, Toshitaka; Tsutomu Kameyama, Kameyama.

In: Pharmacology, Biochemistry and Behavior, Vol. 39, No. 4, 01.01.1991, p. 947-953.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Pharmacokinetic and pharmacodynamic properties of some phencyclidine analogs in rats

AU - Cho, Arthur K.

AU - Masayuki Hiramatsu, Hiramatsu

AU - Schmitz, Debra A.

AU - Nabeshima, Toshitaka

AU - Tsutomu Kameyama, Kameyama

PY - 1991/1/1

Y1 - 1991/1/1

N2 - 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.

AB - 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.

UR - http://www.scopus.com/inward/record.url?scp=0026091167&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0026091167&partnerID=8YFLogxK

U2 - 10.1016/0091-3057(91)90058-A

DO - 10.1016/0091-3057(91)90058-A

M3 - Article

VL - 39

SP - 947

EP - 953

JO - Pharmacology Biochemistry and Behavior

JF - Pharmacology Biochemistry and Behavior

SN - 0091-3057

IS - 4

ER -