Details
Stereochemistry | ACHIRAL |
Molecular Formula | C16H19N5O.2ClH |
Molecular Weight | 370.277 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.Cl.CN1CCN(CC1)C2=NN=C3OC4=CC=CC=C4N(C)C3=C2
InChI
InChIKey=ZZVWCKAYZSAUKR-UHFFFAOYSA-N
InChI=1S/C16H19N5O.2ClH/c1-19-7-9-21(10-8-19)15-11-13-16(18-17-15)22-14-6-4-3-5-12(14)20(13)2;;/h3-6,11H,7-10H2,1-2H3;2*1H
Molecular Formula | C16H19N5O |
Molecular Weight | 297.355 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Molecular Formula | ClH |
Molecular Weight | 36.461 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Pipofezine (Azafen or Azaphen) is a tricyclic antidepressant (TCA) approved in Russia for the treatment of depression. It was introduced in the late 1960s and is still used today. Pipofezine has been shown to act as a potent inhibitor of the reuptake of serotonin. In addition to its antidepressant action, pipofezine has sedative effects as well, suggesting antihistamine activity. Other properties such as anticholinergic or antiadrenergic actions are less clear but are likely. The main advantage of Azafen compared with other tricyclic antidepressants is that this drug has a low toxic effect on the body, including the heart, and it does not block cholinergic receptors and does not change the activity of monoamine oxidase. The maximum concentration in the blood is reached after 1-2 hours after taking the drug. Absorbed in the gastrointestinal tract, metabolism occurs in the liver, and is excreted by Azaphene kidneys.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: GO:0051610 Sources: https://www.ncbi.nlm.nih.gov/pubmed/7198493 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | Azaphen Approved UseTreatment of depression |
Sample Use Guides
The initial dose for adults is 25–50 mg in 2 divided doses (morning and afternoon). With good endurance gradually increase the dose to 150–200 mg/day (3–4 hours, last admission at bedtime), in some cases - up to 400 mg/day. The optimal daily dose - 150–200 mg, the maximum daily dose - 400–500 mg. When the desired effect of switching to maintenance dose - 25–75 mg/day. The course of treatment - up to 1 year (at least 1–1.5 months).
After establishing the optimal daily dose using tablets Azaphen 25 mg, administered Azafen MB (modified-release tablets) 150 mg of 1 times (morning) or 2 times (morning and evening) based on efficacy and tolerance.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/7198493
Inkasan and azaphen were the most potent inhibitors of the 3H-serotonin uptake (65-70% inhibition at a concentration of 50 u M. Azaphen and chlorimipramine were the only ones to inhibit the uptake of 3H-GABA at a concentration of 50 uM.
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 08:05:10 GMT 2023
by
admin
on
Sat Dec 16 08:05:10 GMT 2023
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Record UNII |
MFB4TD413U
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Record Status |
Validated (UNII)
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159976
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24853-80-3
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MFB4TD413U
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DTXSID10179554
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100000177091
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11096-84-7
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Azaphen
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Related Record | Type | Details | ||
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ACTIVE MOIETY |