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• W2029243562 abstract "Nomifensine (8-amino-2-methyl-4-phenyl-1,2,3,4-tetrahydroisoquinoline hydrogen maleate) is a thymoleptic drug with a moderate centrally stimulating component. Its effects on noradrenaline (NA) and serotonin (5-HT) uptake by crude synaptosome preparations from both whole rat brain and from hypothalamus have been studied and compared with those of several tricyclic antidepressants and d-amphetamine. Nomifensine inhibition of NA uptake by synaptosomal fractions from rat hypothalamus (IC50 = 7.0 × 10−7 M) was similar to that of nortriptyline and protriptyline. In contrast to tricyclic antidepressants, nomifensine was found to be a powerful inhibitor of NA uptake in synaptosomes obtained from whole brain (IC50 = 9.0 × 10−8 M). Nomifensine had only a moderate effect on 5-HT accumulation (IC50 = 2.8 × 10−5 M), comparable with that of desipramine. The inhibition of uptake of both NA and 5-HT by nomifensine was of a competitive type. It is suggested that the centrally stimulating component of nomifensine, which is lacking in most thymoleptic drugs, is based upon its strong inhibition of catecholamine re-uptake into noradrenergic as well as dopaminergic nerve endings. Nomifensine has no releasing effects on the efflux of NA from rat brain synaptosomes, thus differing clearly from d-amphetamine and other indirectly acting sympathicomimetic agents." @default.
• W2029243562 created "2016-06-24" @default.
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• W2029243562 date "1974-12-01" @default.
• W2029243562 modified "2023-09-27" @default.
• W2029243562 title "Effect of nomifensine (Hoe 984), a new antidepressant, on uptake of noradrenaline and serotonin and on release of noradrenaline in rat brain synaptosomes" @default.
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• W2029243562 doi "https://doi.org/10.1016/0006-2952(74)90344-x" @default.
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