A phenothiazine with diverse biological activities
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Triflupromazine is a phenothiazine with diverse biological activities.1,2,3,4 It binds to muscarinic receptors in isolated rat corpus striatum (IC50 = 100 μM in a radioligand binding assay).1 Triflupromazine inhibits serotonin (5-HT) uptake by isolated rat brainstem synaptosomes (IC50 = 0.8 μM).2 It inhibits T. cruzi infection in mouse peritoneal macrophages when used at a concentration of 12.5 μM.3 Triflupromazine is active against S. aureus, shigellae, and vibrios (MICs = 2-100 μg/ml) in vitro and is protective against S. typhimurium infection in mice when administered at a dose of 30 μg per animal.4 Formulations containing triflupromazine were previously used as antipsychotics.
1.Snyder, S.H., Greenberg, D., and Yamumura, H.I.Antischizophrenic drugs: Affinity for muscarinic cholinergic receptor sites in the brain predicts extrapyramidal effectsJ. Psychiatr. Res.1191-95(1974) 2.Tuomisto, J.A new modification for studying 5-HT uptake by blood platelets: A re-evaluation of tricyclic antidepressants as uptake inhibitorsJ. Pharm. Pharmacol.26(2)92-100(1974) 3.De Castro, S.L., Soeiro, M.N., and De Meirelles Mde, N.Trypanosoma cruzi: Effect of phenothiazines on the parasite and its interaction with host cellsMem. Inst. Oswaldo Cruz87(2)209-215(1992) 4.Dastidar, S.G., Debnath, S., Mazumdar, K., et al.Triflupromazine: A microbicide non-antibiotic compoundActa Microbiol. Immuno. Hung.51(1-2)75-83(2004)
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