3H-Spiroperidol binding to dopamine receptors in rat striatal membranes: influence of loxapine and its hydroxylated metabolites.

Abstract:

:The effects of loxapine and its hydroxylated metabolites 7-hydroxyloxapine and 8-hydroxyloxapine on 3H-spiroperidol binding to rat striatal membranes were investigated. Whereas 7-hydroxyloxapine and loxapine displayed strong affinities for 3H-spiroperidol binding sites, 8-hydroxyloxapine was essentially inactive. The potency of 7-hydroxyloxapine to displace 3H-spiroperidol is 1.5 times and 8 times those of haloperidol and chlorpromazine, respectively. These results suggest that the combined effects of loxapine and 7-hydroxyloxapine on the postsynaptic dopamine receptors in the brain may explain the clinical efficacy of loxapine in the treatment of schizophrenia.

journal_name

Eur J Pharmacol

authors

Coupet J,Rauh CE

doi

10.1016/0014-2999(79)90396-0

subject

Has Abstract

pub_date

1979-04-15 00:00:00

pages

215-8

issue

2

eissn

0014-2999

issn

1879-0712

pii

0014-2999(79)90396-0

journal_volume

55

pub_type

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