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MedChemExpress - Model Trimipramine maleate -521-78-8

Trimipramine maleate is a 5-HT receptor antagonist, with pKi binding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively[1]. Trimipramine maleate is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC50 values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively[2]. Trimipramine maleate has vascular activity and anxiolytic efficacy[3].

Trimipramine maleate

MCE China：Trimipramine maleate

Brand：MedChemExpress (MCE)

Cat. No.HY-B1213

CAS：521-78-8

Purity：99.82%

Storage：4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Trimipramine maleate is a 5-HT receptor antagonist, with pKi binding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively. Trimipramine maleate is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC50 values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively. Trimipramine maleate has vascular activity and anxiolytic efficacy.

In Vitro：Trimipramine maleate displays much higher affinity for 5-HT2 than for 5-HT1C receptors[1]. Trimipramine maleate is a moderate inhibitor of the human NAT and SERT, with the IC50 values of 4.99 μM and 2.11 μM, respectively[2]. SERT and NAT could represent a target for the antidepressant effects of trimipramine maleate (1 mM, 0.1 mM, 0.01 mM, 1 μM, 0.1 μM; 10 min; HEK293 cells)[2].

In Vivo：Trimipramine maleate (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-HT2 and striatal DA D2 receptors. 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-HT2 and DA D2 receptors[3].

IC50 & Target：5-HT1C Receptor 6.39 (pKi) 5-HT2 Receptor 8.10 (pKi) sPLA2 4.66 (pKi)

References：

[1]. Jenck F, et al. Evidence for a role of 5-HT1C receptors in the antiserotonergic properties of some antidepressant drugs. Eur J Pharmacol. 1993 Feb 9;231(2):223-9. [Content Brief]

[2]. Haenisch B, et al. Inhibitory potencies of trimipramine and its main metabolites at human monoamine and organic cation transporters. Psychopharmacology (Berl). 2011 Sep. 217(2):289-95. [Content Brief]

[3]. Juorio AV, et al. The effects of chronic trimipramine treatment on biogenic amine metabolism and on dopamine D2, 5-HT2 and tryptamine binding sites in rat brain. Gen Pharmacol. 1990;21(5):759-62. [Content Brief]

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MedChemExpress - Model Trimipramine maleate -521-78-8

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Trimipramine maleate