Details
| Stereochemistry | RACEMIC |
| Molecular Formula | C17H17Cl2NO.ClH |
| Molecular Weight | 358.69 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.COC1=CC=C2C(CN(C)CC2=C1)C3=CC=C(Cl)C(Cl)=C3
InChI
InChIKey=PEHOXCSPLOXNOK-UHFFFAOYSA-N
InChI=1S/C17H17Cl2NO.ClH/c1-20-9-12-7-13(21-2)4-5-14(12)15(10-20)11-3-6-16(18)17(19)8-11;/h3-8,15H,9-10H2,1-2H3;1H
| Molecular Formula | C17H17Cl2NO |
| Molecular Weight | 322.229 |
| Charge | 0 |
| Count |
|
| Stereochemistry | RACEMIC |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Optical Activity | ( + / - ) |
| 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 |
Diclofensine is an antidepressant with equipotent inhibitive effects on the neuronal uptake of norepinephrine (NE), serotonin, and dopamine. It is devoid of monoamine-releasing or monoaminoxidase-inhibiting properties. Diclofensine was found to be an effective antidepressant in human trials, with relatively few side effects, but was ultimately dropped from clinical development.
CNS Activity
Originator
Sources: https://www.google.com.ar/patents/US3947456
Curator's Comment: # Hoffman-La Roche Inc.
Approval Year
Doses
| Dose | Population | Adverse events |
|---|---|---|
75 mg 1 times / day multiple, oral Studied dose Dose: 75 mg, 1 times / day Route: oral Route: multiple Dose: 75 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Disc. AE: Agitation, Sweating... AEs leading to discontinuation/dose reduction: Agitation (1 pt) Sources: Sweating (1 pt) |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Agitation | 1 pt Disc. AE |
75 mg 1 times / day multiple, oral Studied dose Dose: 75 mg, 1 times / day Route: oral Route: multiple Dose: 75 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Sweating | 1 pt Disc. AE |
75 mg 1 times / day multiple, oral Studied dose Dose: 75 mg, 1 times / day Route: oral Route: multiple Dose: 75 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/7028532
Treatment of depression: a 50 mg daily dose of diclofensine would be sufficient for the majority of the patients. The dosage can be safely increased up to 150 mg daily but this offers few therapeutic advantages.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/2968488
Diclofensine, in concentrations of 0.01, 0.1 and 1 uM caused a marked decrease of 3H-DA uptake in rat arcuate-periventricular nucleus-median eminence synaptosomes. Diclofensine (50 uM) caused a 3 fold enhancement of K+-evoked endogenous DA release from tuberoinfundibular dopaminergic (TIDA) neurons.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 17:56:03 GMT 2025
by
admin
on
Mon Mar 31 17:56:03 GMT 2025
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| Record UNII |
8U71XY6JQK
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| Record Status |
Validated (UNII)
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| Record Version |
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157489
Created by
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8U71XY6JQK
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34041-84-4
Created by
admin on Mon Mar 31 17:56:03 GMT 2025 , Edited by admin on Mon Mar 31 17:56:03 GMT 2025
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ENANTIOMER -> RACEMATE | |||
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ENANTIOMER -> RACEMATE | |||
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PARENT -> SALT/SOLVATE |
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ACTIVE MOIETY |