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.
For research use only. We do not sell to patients.
- CAS No.: 739-71-9
- Formula: C20H26N2
- Molecular Weight:294.43
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Trimipramine
MoreAll 5-HT Receptor Isoforms
More
Biological Activity
|
5-HT1A Receptor |
5-HT1C Receptor |
5-HT1C Receptor 6.39 (pKi) |
5-HT2 Receptor 8.10 (pKi) |
5-HT1A Receptor 4.66 (pKi) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
27.7 μM
Compound: trimipramine
|
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
|
[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.
-
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).
Chemical Information
-
CAS No. 739-71-9
-
Molecular Weight 294.43
-
Formula C20H26N2
-
SMILES
CC(CN1C2=CC=CC=C2CCC3=C1C=CC=C3)CN(C)C
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
-
Journal Impact Factor
-
Most Recent
-
Chirality
Evaluation of Acetonitrile in Combination With Alcohols as Modifiers in Chiral Supercritical Fluid Chromatography. [Abstract]2026 Mar 5;38(3):e70092. PMID: 41786509
Purity & Documentation
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)
Trimipramine Related Classifications
HY-B1213A Related Classifications
Powered by Bioz