For research use only.
Catalog No.S4377 Synonyms: Melipramine HCl
Molecular Weight(MW): 316.87
Imipramine is a tricyclic antidepressant (TCA) of the dibenzazepine group, mainly used in the treatment of major depression and enuresis (inability to control urination).
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|Description||Imipramine is a tricyclic antidepressant (TCA) of the dibenzazepine group, mainly used in the treatment of major depression and enuresis (inability to control urination).|
Imipramine in the microsomal incubation results in a predicted value for human clearance of 8.6 to 11 ml/min/kg, a slight underestimate of reported mean human blood clearance values (14–15 ml/min/kg).  Imipramine is metabolized into N-desmethylimipramine (84%), 2-hydroxyimipramine (10%), and 10-hydroxyimipramine (6%) in human hepatic microsomes.  Imipramine (3 μM) inhibits HERG-encoded potassium channels in a reversible manner in CHO cells. Imipramine (3 μM) inhibits HERG tail currents (IHERG) following test pulses to +20 mV with an IC50 of 3.4 μM and a Hill coefficient of 1.17 in CHO cells. Imipramine can completely block native cardiac IKr at 1μm in guinea-pig myocytes. 
|In vivo||Imipramine (10 mg/kg b.i.d.) reverses the decreased sucrose intake of rats exposed to chronic mild stress. Imipramine (10 mg/kg b.i.d.) completely reverses stress caused decrease in D2-receptor binding in the limbic forebrain (but not the striatum).  Imipramine (15 mg/kg, IP) exerts anxiolytic-like effects in the two elevated T-maze tasks in male Wistar rats. Imipramine (15 mg/kg, IP) enhances both avoidance and escape latencies in male Wistar rats. Imipramine (15 mg/kg, IP) decreases locomotor activity measured in a square arena in male Wistar rats. |
-  Obach RS, et al. Drug Metab Dispos, 1997, 25(12), 1359-1369.
-  Lemoine A, et al. Mol Pharmacol, 1993, 43(5), 827-832.
-  Teschemacher AG, et al. Br J Pharmacol, 1999, 128(2), 479-485.
|In vitro||DMSO||63 mg/mL (198.81 mM)|
|Water||63 mg/mL (198.81 mM)|
|Ethanol||63 mg/mL (198.81 mM)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
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