Trimipramine
Based on 1 publication(s) in Google Scholar
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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- CAS No.: 739-71-9
- 화학식: C20H26N2
- 분자량:294.43
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보관:
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Publications Citing Use of MedChemExpress (MCE) Trimipramine
MoreAll 5-HT Receptor Isoforms
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Biological Activity
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5-HT1A Receptor |
5-HT1C Receptor |
5-HT1C Receptor 6.39 (pKi) |
5-HT2 Receptor 8.10 (pKi) |
5-HT1A Receptor 4.66 (pKi) |
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Cell Line
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Type | Value | Description | References |
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| HEK293 | IC50 |
27.7 μM
Compound: trimipramine
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Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
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[PMID: 18788725] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar rats (220-250 g); implanted osmotic minipump subcutaneously in the dorsal thoracic interscapular region[3]
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Dosage:5 mg/kg/day
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Administration:Delivered by smotic minipump; 14 days
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Result:Decreased the number of frontal cortex 5-HT2 and striatal DA D2 receptors, thus blocked the uptake of 5-HT and dopamine (DA).
Chemical Information
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CAS No. 739-71-9
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분자량 294.43
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화학식 C20H26N2
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SMILES
CC(CN1C2=CC=CC=C2CCC3=C1C=CC=C3)CN(C)C
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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Chirality
Evaluation of Acetonitrile in Combination With Alcohols as Modifiers in Chiral Supercritical Fluid Chromatography. [Abstract]2026 Mar 5;38(3):e70092. PMID: 41786509
순도&문서
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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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