Synthesis and cataleptic effects of optically active dihydrohaloperidols and dihydrobromoperidols

Mitsuhiro Takeshita, Masatomo Miura, Takahiko Hongo, Tadashi Ohkubo, Kazunobu Sugawara, Kazuhiko Kosaka, Tsutomu Araki, Yoshiteru Oshima

Research output: Contribution to journalArticlepeer-review

3 Citations (Scopus)

Abstract

Optically active dihydrohaloperidols and dihydrobromoperidols, the major metabolites of haloperidol and bromoperidol, clinically used as neuroleptic drugs in humans, were asymmetrically synthesized by Jaen's method. The motor effects of all the reduced haloperidol and bromoperidol metabolites were evaluated by the mouse catalepsy test. The results indicate that administration of the optically active dihydrohaloperidols and dihydrobromoperidols as well as haloperidol and bromoperidol can cause significant motor deficits in mice.

Original languageEnglish
Pages (from-to)443-445
Number of pages3
JournalChirality
Volume9
Issue number5-6
DOIs
Publication statusPublished - 1997

Keywords

  • (R)- dihydrobromoperidol
  • (R)-dihydrohaloperidol
  • (S)-dihydrobromoperidol
  • (S)-dihydrohaloperidol
  • Catalepsy
  • Dyskinesia
  • Motor deficit

ASJC Scopus subject areas

  • Analytical Chemistry
  • Catalysis
  • Pharmacology
  • Drug Discovery
  • Spectroscopy
  • Organic Chemistry

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