Details
Stereochemistry | ACHIRAL |
Molecular Formula | C10H10Cl2N2O.ClH |
Molecular Weight | 281.566 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.ClC1=CC=C(OCC2=NCCN2)C=C1Cl
InChI
InChIKey=AOMZMOWSWJHDRD-UHFFFAOYSA-N
InChI=1S/C10H10Cl2N2O.ClH/c11-8-2-1-7(5-9(8)12)15-6-10-13-3-4-14-10;/h1-2,5H,3-4,6H2,(H,13,14);1H
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 |
Molecular Formula | C10H10Cl2N2O |
Molecular Weight | 245.105 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionSources: https://www.google.ch/patents/US4141985Curator's Comment: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/6256788
Sources: https://www.google.ch/patents/US4141985
Curator's Comment: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/6256788
Fenmetozole is an alpha-2 adrenergic receptor antagonist which was developed for the treatment of schizophrenic and/or depressed patients, however never reached the market. It was also shown that the drug may reduce symptoms of minimal brain dysfunction in children and antagonize the effect of barbiturates and ethanol.
CNS Activity
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2095158 Sources: https://www.ncbi.nlm.nih.gov/pubmed/2875186 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
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OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
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Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no | ||||
no | ||||
yes [IC50 8.4866 uM] |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no |
PubMed
Title | Date | PubMed |
---|---|---|
Clinical trial of imidazoline (DH-524) as an antidepressant. I. Browsing phase. | 1969 Jul |
|
Clinical trial of imidazoline (DH-524) as an anti-depressant. | 1971 Jun |
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Selective antagonism of central nervous system depressants by DH-524; a comparative study with bemegride. | 1973 Oct 1 |
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Antagonism of depressant activity of ethanol by DH-524; a comparative study with Bemegride, Doxapram and d-amphetamine. | 1975 Mar |
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Fenmetazole (DH-524): euphoriant classified by cerebral electrometry. | 1975 Oct |
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Interactions between alcohol and other drugs on open-field and temperature measurements in gerbils. | 1977 May |
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Alcohol-discrimination in gerbils: interactions with bemegride, DH-524, Amphetamine, and delta9-THC. | 1977 May |
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Alcohol-discrimination in gerbils: interactions with bemegride, DH-524, Amphetamine, and delta9-THC. | 1977 May |
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An evaluation of the selectivity of fenmetozole (DH-524) reversal of ethanol-induced changes in central nervous system function. | 1980 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.google.ch/patents/US4141985
Administer 250 to 450 milligrams of fenmetozole hydrochloride per day for 3-4 weeks (schizophrenic and/or depressed patients) or orally at a daily dosage rate of about 3 mg/kg/day using three divided dosages (in children with Minimal Brain Dysfunction).
Route of Administration:
Oral
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 14:59:13 UTC 2023
by
admin
on
Fri Dec 15 14:59:13 UTC 2023
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Record UNII |
AIW7IL0D0B
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Record Status |
Validated (UNII)
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Record Version |
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NCI_THESAURUS |
C265
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32048
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23712-05-2
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CHEMBL50472
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C81486
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AIW7IL0D0B
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DTXSID40178378
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ACTIVE MOIETY |