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

doi:10.1002/(SICI)1520-636X(1997)9:5/6<443::AID-CHIR8>3.0.CO;2-6

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

PHA - Molecular Pharmaceutical Science

Research output: Contribution to journal › Article › peer-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 language	English
Pages (from-to)	443-445
Number of pages	3
Journal	Chirality
Volume	9
Issue number	5-6
DOIs	https://doi.org/10.1002/(SICI)1520-636X(1997)9:5/6<443::AID-CHIR8>3.0.CO;2-6
Publication status	Published - 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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10.1002/(SICI)1520-636X(1997)9:5/6<443::AID-CHIR8>3.0.CO;2-6

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Cite this

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title = "Synthesis and cataleptic effects of optically active dihydrohaloperidols and dihydrobromoperidols",

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.",

keywords = "(R)- dihydrobromoperidol, (R)-dihydrohaloperidol, (S)-dihydrobromoperidol, (S)-dihydrohaloperidol, Catalepsy, Dyskinesia, Motor deficit",

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

year = "1997",

doi = "10.1002/(SICI)1520-636X(1997)9:5/6<443::AID-CHIR8>3.0.CO;2-6",

language = "English",

volume = "9",

pages = "443--445",

journal = "Chirality",

issn = "0899-0042",

publisher = "Wiley-Liss Inc.",

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}

TY - JOUR

T1 - Synthesis and cataleptic effects of optically active dihydrohaloperidols and dihydrobromoperidols

AU - Takeshita, Mitsuhiro

AU - Miura, Masatomo

AU - Hongo, Takahiko

AU - Ohkubo, Tadashi

AU - Sugawara, Kazunobu

AU - Kosaka, Kazuhiko

AU - Araki, Tsutomu

AU - Oshima, Yoshiteru

PY - 1997

Y1 - 1997

N2 - 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.

AB - 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.

KW - (R)- dihydrobromoperidol

KW - (R)-dihydrohaloperidol

KW - (S)-dihydrobromoperidol

KW - (S)-dihydrohaloperidol

KW - Catalepsy

KW - Dyskinesia

KW - Motor deficit

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