Clorgiline
Clorgiline (INN), or clorgyline (BAN), is a monoamine oxidase inhibitor (MAOI) structurally related to pargyline which is described as an antidepressant.[1][2] Specifically, it is an irreversible and selective inhibitor of monoamine oxidase A (MAO-A).[3] Clorgiline was never marketed,[1] but it has found use in scientific research.[4] It has been found to bind with high affinity to the σ1 receptor (Ki = 3.2 nM)[3][5] and with very high affinity to the I2 imidazoline receptor (Ki = 40 pM).[6]
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| Formula | C13H15Cl2NO |
| Molar mass | 272.17 g·mol−1 |
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Clorgiline is also a multidrug efflux pump inhibitor.[7] Holmes et al., 2012 reverse azole fungicide resistance using clorgiline, showing promise for its use in multiple fungicide resistance.[7]
References
- Elks J (14 November 2014). The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. pp. 304–. ISBN 978-1-4757-2085-3.
- Morton I, Hall JM (6 December 2012). Concise Dictionary of Pharmacological Agents: Properties and Synonyms. Springer Science & Business Media. pp. 80–. ISBN 978-94-011-4439-1.
- Stone TW (January 1993). Acetylcholine, Sigma Receptors, CCK and Eicosanoids, Neurotoxins. Taylor & Francis. pp. 124–. ISBN 978-0-7484-0063-8.
- Murphy DL, Karoum F, Pickar D, Cohen RM, Lipper S, Mellow AM, et al. (1998). "Differential trace amine alterations in individuals receiving acetylenic inhibitors of MAO-A (clorgyline) or MAO-B (selegiline and pargyline)". Journal of Neural Transmission. Supplementum. Journal of Neural Transmission. Supplement. 52: 39–48. doi:10.1007/978-3-7091-6499-0_5. ISBN 978-3-211-83037-6. PMID 9564606.
- Itzhak Y (1994). Sigma Receptors. Academic Press. p. 84. ISBN 978-0-12-376350-1.
- Critical Reviews in Neurobiology. CRC Press. 1995. p. 43.
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- • Prasad, Rajendra; Banerjee, Atanu; Shah, Abdul Haseeb (2017). "Resistance to antifungal therapies". Essays in Biochemistry. Portland Press (Biochemical Society). 61 (1): 157–166. CiteSeerX 10.1.1.1066.1806. doi:10.1042/ebc20160067. ISSN 0071-1365. PMID 28258238. S2CID 3414820.
- • Holmes, Ann R.; Keniya, Mikhail V.; Ivnitski-Steele, Irena; Monk, Brian C.; Lamping, Erwin; Sklar, Larry A.; Cannon, Richard D. (2012). "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". Antimicrobial Agents and Chemotherapy. American Society for Microbiology. 56 (3): 1508–1515. doi:10.1128/aac.05706-11. ISSN 0066-4804. PMC 3294898. PMID 22203607. S2CID 21170509.
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