For research use only.
Catalog No.S4377 Synonyms: Melipramine HCl
CAS No. 113-52-0
Imipramine (Melipramine) 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 (Melipramine) 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)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04520217||Not yet recruiting||Drug: 4% Imipramine Cream|Drug: Base Cream||Photosensitivity|Microvesicle Particle||Wright State Physicians||August 2021||Phase 1|
|NCT00693680||Completed||Dietary Supplement: Zincas Forte|Dietary Supplement: Placebo||Major Depression||Polish Academy of Sciences|Jagiellonian University||January 2005||Not Applicable|
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