Synthesis, Phencyclidine-like Pharmacology, and Antiischemic Potential of Meta-Substituted 1-(1-Phenylcyclohexyl)-1,2,3,6-tetrahydropyridines

Andrew Thurkauf, Brian de Costa, Mariena V. Mattson, A. E. Jacobson, Charles P. France, James H. Woods, Madelon T. Price, John W. Olney, Kenner C. Rice

Research output: Contribution to journalArticlepeer-review

9 Scopus citations

Abstract

A series of 1-[1-arylcyclohexy1]-1,2,3,6-tetrahydropyridines were prepared by the reaction between 1-(1-cyano-cyclohexy1)-1,2,3,6-tetrahydropyridine (1) and an appropriately substituted Grignard reagent. The resulting compounds were tested for their phencyclidine binding site affinities. Selected compounds were then tested for their ability to produce ketamine appropriate responding in monkeys and/or to show neuroprotective effects in a baby rat hypoxia/ ischemia model. While it was found that binding site affinity correlated well with discriminative stimulus effects, it was found to be a poor indicator of neuroprotective efficacy within this series.

Original languageEnglish (US)
Pages (from-to)2211-2215
Number of pages5
JournalJournal of Medicinal Chemistry
Volume33
Issue number8
DOIs
StatePublished - 1990
Externally publishedYes

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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