1. GPCR/G Protein
    Neuronal Signaling
    Anti-infection
  2. 5-HT Receptor
    Bacterial
  3. Trimipramine maleate

Trimipramine maleate 

Cat. No.: HY-B1213 Purity: 99.84%
Handling Instructions

Trimipramine maleate is a 5-HT receptor antagonist, with pKis of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively.

For research use only. We do not sell to patients.

Trimipramine maleate Chemical Structure

Trimipramine maleate Chemical Structure

CAS No. : 521-78-8

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10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
100 mg USD 60 In-stock
Estimated Time of Arrival: December 31
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Description

Trimipramine maleate is a 5-HT receptor antagonist, with pKis of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively.

IC50 & Target

5-HT1C Receptor

6.39 (pKi)

5-HT2 Receptor

8.10 (pKi)

sPLA2

4.66 (pKi)

In Vitro

Trimipramine displays much higher affinity for 5-HT2 than for 5-HT1C receptors[1].

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

In Vivo

The chronic administration of Trimipramine (5 mg/kg/day), as delivered by the osmotic minipump in 14 days produce significant increases in the regional concentration of 5-HT. The increases are highest in the frontal cortex and the hippocampus, followed by the olfactory tubercles and the hypothalamus. The Trimipramine treatment also produces marked increases in brain 5-HIAA concentrations ranging from 63% in the hippocampus to 25% in the nucleus accumbens with intermediate values for the hypothalamus, olfactory tubercles, frontal cortex and nucleus accumbens. Trimipramine treatment produces significant increases in DA concentrations in the nucleus accumbens, striaturn, and olfactory tubercles reaching 43, 21 and 11% respectively. Chronic administration of Trimipramine produces a marked reduction in the number of frontal cortex 5-HT2 and striatal DA D2 receptors. The chronic administration of Trimipramine produces an increase in the brain regional level of monoamines and metabolites indicating a greater synthesis rate for DA and 5-HT coinciding with an adaptive down regulation of 5-HT2 and DA D2 receptors[2].

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

Clinical Trial
Molecular Weight

410.51

Formula

C₂₄H₃₀N₂O₄

CAS No.

521-78-8

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (243.60 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4360 mL 12.1800 mL 24.3599 mL
5 mM 0.4872 mL 2.4360 mL 4.8720 mL
10 mM 0.2436 mL 1.2180 mL 2.4360 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.09 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.09 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.09 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[2]

Rats[2]
Male Wistar rats weighing 220-250 g at the beginning of the experiment are used. The animals, housed in groups of 6-8 have free access to food and water and are kept on a 12 hr light/dark cycle (light on at 6a.m.) at a temperature. The rats are anaesthetized with pentobarbital (50 mg/kg i.p.) and an osmotic minipump is implanted subcutaneously in the dorsal thoracic interscapular region. Each pump delivers 5 mg/kg/day of Trimipramine or amitriptyline. Control rats are implanted with pumps filled with 0.9%, saline. The total volume of solution in the pump is sufficient for at least 14 days delivery of drugs. After implantation, the incision is cleaned and sutured and the animals kept warm until they recovered from anaesthesia[2].

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

References
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Keywords:

Trimipramine5-HT ReceptorBacterialSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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