2. 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.

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Trimipramine Chemical Structure

Trimipramine Chemical Structure

CAS No. : 739-71-9

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Trimipramine Related Antibodies

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Description

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].

IC50 & Target

pKi: 6.39 (5-HT1C), 8.10 (5-HT2), 4.66 (5-HT1A) IC50: 4.99 μM (hNAT), 2.11 μM (hSERT), 3.72 μM (OCT1), 8.00 μM (hOCT2)
In Vitro

Trimipramine displays much higher affinity for 5-HT2 than for 5-HT1C receptors[1].
Trimipramine 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 (1 mM, 0.1 mM, 0.01 mM, 1 μM, 0.1 μM; 10 min; HEK293 cells)[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Trimipramine Related Antibodies
In Vivo

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-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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Wistar rats (220-250 g); implanted osmotic minipump subcutaneously in the dorsal thoracic interscapular region[3]
Dosage: 5 mg/kg/day
Administration: Delivered by smotic minipump; 14 days
Result: Decreased the number of frontal cortex 5-HT2 and striatal DA D2 receptors, thus blocked the uptake of 5-HT and dopamine (DA).
Clinical Trial
Molecular Weight

294.43

Formula

C20H26N2
CAS No.
SMILES

CC(CN1C2=CC=CC=C2CCC3=C1C=CC=C3)CN(C)C
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Purity & Documentation
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Keywords:

Trimipramine739-71-9Inhibitorinhibitorinhibit

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