Details
Stereochemistry | ACHIRAL |
Molecular Formula | C13H15Cl2NO.ClH |
Molecular Weight | 308.631 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CN(CCCOC1=C(Cl)C=C(Cl)C=C1)CC#C
InChI
InChIKey=BBAZDLONIUABKI-UHFFFAOYSA-N
InChI=1S/C13H15Cl2NO.ClH/c1-3-7-16(2)8-4-9-17-13-6-5-11(14)10-12(13)15;/h1,5-6,10H,4,7-9H2,2H3;1H
Clorgiline is a monoamine oxidase (MAO) inhibitor. Specifically, it is an irreversible and selective inhibitor of MAO-A. Clorgiline was under investigation for antidepressant and anxiolytic potential but has never been marketed, likely due to efficacy concerns. It continues to see routine use as a molecular probe in biomedical research examining a number of neurological disease and cancer models. In addition to inhibiting the MAO-A receptor, it has also been found to bind to the sigma1 receptor, and with high affinity to the I2 imidazoline receptor.
CNS Activity
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: P21397 Gene ID: 4128.0 Gene Symbol: MAOA Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/9564606 |
1.4 nM [IC50] | ||
Target ID: Q99720|||Q7Z653 Gene ID: 10280.0 Gene Symbol: SIGMAR1 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/20060423 |
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Target ID: Q9Y2I1|||Q9UFW3 Gene ID: 11188.0 Gene Symbol: NISCH Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/12652347 |
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Target ID: CHEMBL1951 |
1.4 nM [IC50] | ||
Target ID: Q99720|||Q7Z653 Gene ID: 10280.0 Gene Symbol: SIGMAR1 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/20060423 |
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Target ID: Q9Y2I1|||Q9UFW3 Gene ID: 11188.0 Gene Symbol: NISCH Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/12652347 |
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 |
PubMed
Title | Date | PubMed |
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Treatment with clorgyline and pargyline differentially decreases clonidine-induced hypotension and bradycardia. | 1984 Sep |
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Pharmacological characteristics of tremor, rigidity and hypokinesia induced by reserpine in rat. | 1987 Sep |
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Differential trace amine alterations in individuals receiving acetylenic inhibitors of MAO-A (clorgyline) or MAO-B (selegiline and pargyline). | 1998 |
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The monoamine oxidase A inhibitor clorgyline is a broad-spectrum inhibitor of fungal ABC and MFS transporter efflux pump activities which reverses the azole resistance of Candida albicans and Candida glabrata clinical isolates. | 2012 Mar |
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A novel selective LSD1/KDM1A inhibitor epigenetically blocks herpes simplex virus lytic replication and reactivation from latency. | 2013 Feb 5 |
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Acute effects of resveratrol to enhance cocaine-induced dopamine neurotransmission in the striatum. | 2013 May 10 |
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Screening of a chemical library reveals novel PXR-activating pharmacologic compounds. | 2015 Jan 5 |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/9564606
Patients suffering depression were administered 30 mg/day of Clorgyline for three or more weeks. However, this regime produced negligible changes in trace amine excretion including, phenylethylamine, para-tyramine, and meta-tyramine.
Route of Administration:
Unknown
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/24040395
T24, HCT116, and HL60 cells were incubated overnight and treated with 1 micro-, 0.3 µM or 0.1 µM of 5-Aza-CdR, respectively for 24 hours. After removal of 5-Aza-CdR, cells were treated with 10 µM clorgyline every day for 21 days. Multiple doses of clorgyline were tested: 1 µM, 10 µM, and 100 µM. Clorgyline was found to impair cell growth in a dose-dependent manner and the optimal dose was identified as 10 microM.
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241-760-5
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17780-75-5
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DBSALT002700
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H38V165133
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PARENT (SALT/SOLVATE)
SUBSTANCE RECORD