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100mg | ||
250mg | ||
500mg |
ln Vitro |
Compared to 5-HT1C receptors, trimipramine has a substantially higher affinity for 5-HT2 receptors [1]. Trimipramine has an IC50 value of 2.11 μM for human SERT and 4.99 μM for human NAT, making it a moderate inhibitor of these enzymes [2]. The antidepressant effects of trimipramine (1 mM, 0.1 mM, 0.01 mM, 1 μM, 0.1 μM; 10 min; HEK293 cells) may have an effect on SERT and NAT [2].
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ln Vivo |
The following are the long-term effects of trimipramine (5 mg/kg/d; 14 days) in rats: 1. Concentration of 5-HT rises regionally. The hippocampus and frontal cortex had the highest levels of 5-HT, followed by the hypothalamus and olfactory tubercle. 2. Decrease the quantity of DA D2 receptors in the striatum and 5-HT2 receptors in the frontal brain. 3. elevated metabolite and monoamine levels in specific brain areas. Therefore, it is hypothesized that there is a higher rate of dopamine (DA) and 5-HT production, which is compatible with adaptive down-regulation of D2 and 5-HT2 receptors [3].
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Animal Protocol |
Animal/Disease Models: Male Wistar rat (220-250 g); osmotic minipump is implanted subcutaneously (sc) (sc) in the dorsal thoracic interscapular area [3]
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 |
[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.
[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. [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. |
Molecular Formula |
C20H26N2
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Molecular Weight |
294.442
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Exact Mass |
294.2096
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CAS # |
739-71-9
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Related CAS # |
Trimipramine maleate;521-78-8;Trimipramine-d3 (N-methyl-d3)
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
CC(CN(C)C)CN1C2=CC=CC=C2CCC3=CC=CC=C31
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Synonyms |
Surmontil, Rhotrimine, Stangyl; Trimipramine
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.3963 mL | 16.9814 mL | 33.9628 mL | |
5 mM | 0.6793 mL | 3.3963 mL | 6.7926 mL | |
10 mM | 0.3396 mL | 1.6981 mL | 3.3963 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.