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  • Title: 3H-Spiroperidol binding to dopamine receptors in rat striatal membranes: influence of loxapine and its hydroxylated metabolites.
    Author: Coupet J, Rauh CE.
    Journal: Eur J Pharmacol; 1979 Apr 15; 55(2):215-8. PubMed ID: 456420.
    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.
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