PMID: 8584621Oct 1, 1995Paper

Effect of haloperidol and its metabolites on dopamine and noradrenaline uptake in rat brain slices

Psychopharmacology
J Fang, P H Yu

Abstract

The effects of haloperidol and its metabolites on dopamine (DA) and noradrenaline (NA) uptake were investigated. Both direct uptake of [3H]DA and [3H]NA into the rat striatal and hippocampus slices and binding of a specific DA uptake inhibitor [3H]GBR-12935 were employed in the present study. Haloperidol pyridinium (HP+), haloperidol 1,2,3,6-tetrahydropyridine (HTP), 4-(4-chlorophenyl)-1,2,3,6-tetrahydropyridine (CPTP) and reduced haloperidol (RHAL) are potent inhibitors of DA uptake. HTP N-oxide (HTPNO) exhibits a relatively weak effect on DA uptake. Other metabolites of haloperidol, i.e. 4-(4-chlorophenyl)-4-hydroxypyridine (CPHP) and haloperidol N-oxide (HNO), as well as haloperidol itself possess negligible inhibitory effect on DA uptake. HP+ has been shown to be an amine releaser. It is possible that HP+ may induce amphetamine-like neurotoxicity. The effects of the metabolites of haloperidol on [3H]NA uptake are similar to those on [3H]DA uptake. HP+ appears to be different from MPP+, which is a more potent [3H]NA uptake blocker than on [3H]DA uptake. Although haloperidol exhibits no DA uptake inhibitory effect, it has a high affinity for the [3H]GBR-12935 binding site. The possible pharmacological implications such inhibi...Continue Reading

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Citations

Dec 9, 1998·Drug Metabolism Reviews·E UsukiN Castagnoli
Mar 17, 2007·Progress in Neuro-psychopharmacology & Biological Psychiatry·Tetsuhito MurataYuji Wada
Oct 16, 2015·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Marijn C W KroesGuillén Fernández
Apr 29, 2004·Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences·Norio Yasui-FurukoriTomonori Tateishi
Jan 1, 1995·Journal of Psychopharmacology·G B BakerR A Bornstein
Nov 26, 2003·Therapeutic Drug Monitoring·Norio Yasui-FurukoriTomonori Tateishi

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