Trimipramine maleate is a 5-HT receptor antagonist, with blood-brain barrier permeability. Trimipramine maleate has pK i binding values of 6.39, 8.10, 4.66 for 5-HT 1C , 5-HT 2 and 5-HT 1A , respectively. Trimipramine maleate is also a potent and selective inhibitor targeting human noradrenaline ( hNAT ), serotonin ( hSERT ) and organic cation transporters ( hOCT1 , hOCT2 ) with IC 50 values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively. Trimipramine maleate has vascular activity and anxiolytic efficacy.
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