Trimipramine is a5-HT receptorantagonist, withpK_ibinding values of 6.39, 8.10, 4.66 for 5-HT_1C, 5-HT₂and 5-HT_1A, respectively. Trimipramine is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1,hOCT2) withIC₅₀values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively. Trimipramine has vascular activity and anxiolytic efficacy^[1][2][3].

Trimipramine displays much higher affinity for 5-HT₂than for 5-HT_1Creceptors^[1].
Trimipramine is a moderate inhibitor of the human NAT and SERT, with the IC₅₀values of 4.99 μM and 2.11 μM, respectively^[2].
SERT and NAT could represent a target for the antidepressant effects of trimipramine (1 mM, 0.1 mM, 0.01 mM, 1 μM, 0.1 μM; 10 min; HEK293 cells)^[2].

Trimipramine (5 mg/kg/d; 14 d; chronic administration) acts as functions in rats:1. Increasing concentration of regional 5-HT. 5-HT is highest in the frontal cortex and the hippocampus, followed by the olfactory tubercles and the hypothalamus. 2. Decreasing the number of frontal cortex 5-HT₂and striatal DA D₂receptors. 3. Increasing in the brain regional level of monoamines and metabolites. thus indicates a greater synthesis rate for dopamine (DA) and 5-HT coinciding with an adaptive down regulation of 5-HT₂and DA D₂receptors^[3].

294.43

C₂₀H₂₆N₂

739-71-9

曲米帕明

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