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=CC2=C(C=C1)C(CN(C)C2)C3=CC(Cl)=C(Cl)C=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.
Approval Year
Doses
| Dose | Population | Adverse events |
|---|---|---|
75 mg 1 times / day multiple, oral (max) Studied dose Dose: 75 mg, 1 times / day Route: oral Route: multiple Dose: 75 mg, 1 times / day Sources: |
unhealthy, ADULT n = 14 Health Status: unhealthy Condition: depression Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 14 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 (max) Studied dose Dose: 75 mg, 1 times / day Route: oral Route: multiple Dose: 75 mg, 1 times / day Sources: |
unhealthy, ADULT n = 14 Health Status: unhealthy Condition: depression Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 14 Sources: |
| Sweating | 1 pt Disc. AE |
75 mg 1 times / day multiple, oral (max) Studied dose Dose: 75 mg, 1 times / day Route: oral Route: multiple Dose: 75 mg, 1 times / day Sources: |
unhealthy, ADULT n = 14 Health Status: unhealthy Condition: depression Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 14 Sources: |
Sample Use Guides
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
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
Fri Dec 15 15:23:19 GMT 2023
by
admin
on
Fri Dec 15 15:23:19 GMT 2023
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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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-
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157489
Created by
admin on Fri Dec 15 15:23:19 GMT 2023 , Edited by admin on Fri Dec 15 15:23:19 GMT 2023
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8U71XY6JQK
Created by
admin on Fri Dec 15 15:23:19 GMT 2023 , Edited by admin on Fri Dec 15 15:23:19 GMT 2023
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34041-84-4
Created by
admin on Fri Dec 15 15:23:19 GMT 2023 , Edited by admin on Fri Dec 15 15:23:19 GMT 2023
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| Related Record | Type | Details | ||
|---|---|---|---|---|
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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 |