Trimipramine (maleate)

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].

Product Specifications

CAS Number

[521-78-8]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335, H360

Target

5-HT Receptor; Bacterial

Type

Reference compound

Related Pathways

Anti-infection; GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/Trimipramine-maleate.html

Purity

99.97

Solubility

DMSO : ≥ 100 mg/mL|H2O : 14.29 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

CC(CN(C)C)CN1C2=C(C=CC=C2)CCC3=C1C=CC=C3.O=C(O)/C=C\C(O)=O

Molecular Formula

C24H30N2O4

Molecular Weight

410.51

Precautions

H302, H315, H319, H335, H360

References & Citations

[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.|[2]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.|[3]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.