Clorgiline Explained

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, but it has found use in scientific research.^[4] It has been found to bind with high affinity to the σ₁ receptor (K_i = 3.2 nM)^[5] and with very high affinity to the I₂ imidazoline receptor (K_i = 40 pM).^[6]

Unlike selegiline, clorgiline does not appear to be a monoaminergic activity enhancer (MAE).^{[7] [8] [9] [10]}

Clorgiline is also a multidrug efflux pump inhibitor. Holmes et al., 2012 reverse azole fungicide resistance using clorgiline, showing promise for its use in multiple fungicide resistance.

Notes and References

1. Book: Elks J . The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. 14 November 2014. Springer. 978-1-4757-2085-3. 304–.
2. Book: Morton IK, Hall JM . Concise Dictionary of Pharmacological Agents: Properties and Synonyms . 6 December 2012. Springer Science & Business Media. 978-94-011-4439-1. 80–.
3. Book: Stone TW . Acetylcholine, Sigma Receptors, CCK and Eicosanoids, Neurotoxins. January 1993. Taylor & Francis. 978-0-7484-0063-8. 124–.
4. Book: Murphy DL, Karoum F, Pickar D, Cohen RM, Lipper S, Mellow AM, Tariot PN, Sunderland T . MAO — the Mother of all Amine Oxidases . Differential trace amine alterations in individuals receiving acetylenic inhibitors of MAO-A (Clorgyline) or MAO-B (Selegiline and pargyline) . 6 . 52 . 39–48 . 1998 . 9564606 . 10.1007/978-3-7091-6499-0_5 . 978-3-211-83037-6 . Journal of Neural Transmission. Supplement .
5. Book: Yossef I . Sigma Receptors. 1994. Academic Press. 978-0-12-376350-1. 84.
6. Piletz JE, Halaris A, Ernsberger PR . Psychopharmacology of imidazoline and alpha 2-adrenergic receptors: implications for depression . Critical Reviews in Neurobiology . 9 . 1 . 29–66 (43) . 1994 . 8828003 .
7. Shimazu S, Miklya I . Pharmacological studies with endogenous enhancer substances: β-phenylethylamine, tryptamine, and their synthetic derivatives . Prog Neuropsychopharmacol Biol Psychiatry . 28 . 3 . 421–427 . May 2004 . 15093948 . 10.1016/j.pnpbp.2003.11.016 .
8. Knoll J . Deprenyl (selegiline): the history of its development and pharmacological action . Acta Neurol Scand Suppl . 95 . 57–80 . 1983 . 6428148 . 10.1111/j.1600-0404.1983.tb01517.x . free .
9. Knoll J . The pharmacological profile of (-)deprenyl (selegiline) and its relevance for humans: a personal view . Pharmacology & Toxicology . 70 . 5 Pt 1 . 317–321 . May 1992 . 1608919 . 10.1111/j.1600-0773.1992.tb00480.x .
10. Yen TT, Dalló J, Knoll J . The aphrodisiac effect of low doses of (-) deprenyl in male rats . Pol J Pharmacol Pharm . 34 . 5-6 . 303–308 . 1982 . 6821215 .