Effect of neuroleptics on indoleamine-N-methyltransferase activity and brain metabolism of bufotenin

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dc.contributor.authorGomes U.C.R.
dc.contributor.authorMcCarthy B.W.
dc.contributor.authorShanley B.C.
dc.date.accessioned2011-05-15T16:01:18Z
dc.date.available2011-05-15T16:01:18Z
dc.date.issued1981
dc.description.abstractA range of neuroleptics, non-neuroleptic phenothiazines and antidepressants were tested for their ability to inhibit purified rabbit lung indoleamine-N-methyltransferase (INMT) and to modify the metabolism of [3H]bufotenin administered intraventricularly. Benperidol and droperidol proved to be the most potent inhibitors of INMT among the compounds tested. On the other hand trifluperidol and haloperidol showed no inhibitory activity at concentrations up to 2.5 mM, while chlorpromazine, thioridazine, pericyazine and perphenazine were effective only at 250 μM or 2.5 mM. Oxidative deamination was shown to be an important pathway in normal rat brain for the metabolism of bufotenin. Of the drugs tested only chlorpromazine elevated the brain [3H]bufotenin/[3H]-5-HIAA ratio whereas pimozide and thiothixene caused a decrease. These findings suggest that neuroleptic drugs in general do not exert their anti-psychotic effects by inhibiting the synthesis or accelerating the oxidative deamination of N,N-dimethylated indoleamines.
dc.description.versionArticle
dc.identifier.citationBiochemical Pharmacology
dc.identifier.citation30
dc.identifier.citation6
dc.identifier.issn62952
dc.identifier.other10.1016/0006-2952(81)90128-3
dc.identifier.urihttp://hdl.handle.net/10019.1/11914
dc.subjectantidepressant agent
dc.subjectneuroleptic agent
dc.subjectradioisotope
dc.subjecttritium
dc.subjectanimal experiment
dc.subjectbrain
dc.subjectbufotenine h 3
dc.subjectcentral nervous system
dc.subjectdrug comparison
dc.subjectdrug metabolism
dc.subjectindoleamine n methyltransferase
dc.subjectintravenous drug administration
dc.subjectlung
dc.subjectnervous system
dc.subjectrabbit
dc.subjectrat
dc.subjectrespiratory system
dc.subjectAnimal
dc.subjectAntidepressive Agents
dc.subjectAntipsychotic Agents
dc.subjectBrain
dc.subjectBufotenin
dc.subjectMale
dc.subjectMethyltransferases
dc.subjectRabbits
dc.subjectSerotonin
dc.subjectSupport, Non-U.S. Gov't
dc.subjectTryptamines
dc.titleEffect of neuroleptics on indoleamine-N-methyltransferase activity and brain metabolism of bufotenin
dc.typeArticle
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