Synthesis and cataleptic effects of optically active dihydrohaloperidols and dihydrobromoperidols.
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.
Takeshita
M
M
Tohoku College of Pharmacy, Sendai, Japan. takemist@mail.cc.tohoku.ac-jp
Miura
M
M
Hongo
T
T
Ohkubo
T
T
Sugawara
K
K
Kosaka
K
K
Takeshita
Y
Y
Araki
T
T
Oshima
Y
Y
D000818:Animals; D002375:Catalepsy / Q000139:chemically induced*; D006220:Haloperidol / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D015394:Molecular Structure; D009043:Motor Activity / Q000187:drug effects*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D006220:Haloperidol; C006820:bromperidol