| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| Other Sizes |
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| ln Vitro |
When it comes to 5-HT2 receptors, trimipramine maleate has a far stronger affinity than 5-HT1C receptors [1]. Trimipramine maleate has an IC50 value of 2.11 μM and 4.99 μM, respectively, which indicates that it moderately inhibits human NAT and SERT [2]. It can stand in for trimipramine maleate's antidepressant goal (1 mM-1 μM, 0.1 μM; 10 minutes; HEK293 cells) [2].
|
|---|---|
| ln Vivo |
Trimipraminemaleate (5 mg/kg/d; 14 d; long-term medication) has the following physiological effects: 1. Elevate the 5-HT concentration in the area. Olfactory 2 and the prefrontal cortex have the highest levels of 5-HT, followed by the hippocampus. decreased density of 5-HT2 grabbers in the striatum DA D2 and frontal brain. 3. The hypothalamus and nodule. As a result, it has been demonstrated that both 5-HT2 and DA D2 receptors have increased rates of dopamine (DA) and 5-HT production [3].
|
| Animal Protocol |
Animal/Disease Models: Male Wistar rats (220-250 g); osmotic minipump [3] implanted subcutaneously (sc) (sc) in the dorsal thoracic interscapular area
Doses: 5 mg/kg/day Route of Administration: delivered by osmotic minipump; 14 days Experimental Results: The number of 5-HT2 receptors in the frontal cortex and DA D2 receptors in the striatum was diminished, thereby blocking the uptake of 5-HT and dopamine (DA). |
| References |
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| Additional Infomation |
Trimipramine Maleate is the maleate salt form of trimipramine, a tricyclic secondary amine of the dibenzazepine class, with an antidepressant property. Trimipramine maleate appears to inhibit serotonin transport and norepinephrine uptake by nerve terminals. This increases available norepinephrine or serotonin and prolongs its action.
Tricyclic antidepressant similar to IMIPRAMINE, but with more antihistaminic and sedative properties. See also: Trimipramine (has active moiety). |
| Molecular Formula |
C20H26N2.C4H4O4
|
|---|---|
| Molecular Weight |
410.506
|
| Exact Mass |
410.22
|
| CAS # |
521-78-8
|
| Related CAS # |
Trimipramine;739-71-9;Trimipramine-d3 maleate;1185245-93-5
|
| PubChem CID |
5282318
|
| Appearance |
White to off-white solid powder
|
| Density |
1.029g/cm3
|
| Boiling Point |
411.8ºC at 760mmHg
|
| Melting Point |
141-143ºC
|
| Flash Point |
183.3ºC
|
| LogP |
3.897
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
30
|
| Complexity |
436
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC(CN1C2=CC=CC=C2CCC3=CC=CC=C31)CN(C)C.C(=C\C(=O)O)\C(=O)O
|
| InChi Key |
YDGHCKHAXOUQOS-BTJKTKAUSA-N
|
| InChi Code |
InChI=1S/C20H26N2.C4H4O4/c1-16(14-21(2)3)15-22-19-10-6-4-8-17(19)12-13-18-9-5-7-11-20(18)22;5-3(6)1-2-4(7)8/h4-11,16H,12-15H2,1-3H3;1-2H,(H,5,6)(H,7,8)/b;2-1-
|
| Chemical Name |
(Z)-but-2-enedioic acid;3-(5,6-dihydrobenzo[b][1]benzazepin-11-yl)-N,N,2-trimethylpropan-1-amine
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~243.60 mM)
H2O : ~14.29 mg/mL (~34.81 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.09 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.09 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.09 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 5.88 mg/mL (14.32 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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