Trimipramine

Trimipramine 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 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 has vascular activity and anxiolytic efficacy[1][2][3].

Product Specifications

CAS Number

[739-71-9]

UNSPSC

12352005

Hazard Statement

H225-H301+H311+H331-H370

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.html

Solubility

10 mM in DMSO

Smiles

CC(CN1C2=CC=CC=C2CCC3=C1C=CC=C3)CN(C)C

Molecular Formula

C20H26N2

Molecular Weight

294.43

Precautions

P210-P233-P240-P241-P242-P243-P260-P261-P264-P270-P271-P280-P302+P352-P303+P361+P353-P304+P340-P308+P311-P330-P361+P364-P370+P378-P403+P233-P403+P235-P405-P501

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.