Chemistry:Clorgiline

From HandWiki

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]

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.[11] Holmes et al., 2012 reverse azole fungicide resistance using clorgiline, showing promise for its use in multiple fungicide resistance.[11]

References

  1. 1.0 1.1 The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. 14 November 2014. pp. 304–. ISBN 978-1-4757-2085-3. https://books.google.com/books?id=0vXTBwAAQBAJ&pg=PA304. 
  2. Concise Dictionary of Pharmacological Agents: Properties and Synonyms. Springer Science & Business Media. 6 December 2012. pp. 80–. ISBN 978-94-011-4439-1. https://books.google.com/books?id=tsjrCAAAQBAJ&pg=PA80. 
  3. 3.0 3.1 Acetylcholine, Sigma Receptors, CCK and Eicosanoids, Neurotoxins. Taylor & Francis. January 1993. pp. 124–. ISBN 978-0-7484-0063-8. https://books.google.com/books?id=0xmt5kSpJEcC&pg=PA124. 
  4. "Differential trace amine alterations in individuals receiving acetylenic inhibitors of MAO-A (Clorgyline) or MAO-B (Selegiline and pargyline)". MAO — the Mother of all Amine Oxidases. Journal of Neural Transmission. Supplement. 52. 1998. pp. 39–48. doi:10.1007/978-3-7091-6499-0_5. ISBN 978-3-211-83037-6. 
  5. Sigma Receptors. Academic Press. 1994. p. 84. ISBN 978-0-12-376350-1. https://books.google.com/books?id=ndRqAAAAMAAJ. 
  6. "Psychopharmacology of imidazoline and alpha 2-adrenergic receptors: implications for depression". Critical Reviews in Neurobiology 9 (1): 29–66 (43). 1994. PMID 8828003. https://books.google.com/books?id=EP9FAQAAIAAJ. 
  7. "Pharmacological studies with endogenous enhancer substances: β-phenylethylamine, tryptamine, and their synthetic derivatives". Prog Neuropsychopharmacol Biol Psychiatry 28 (3): 421–427. May 2004. doi:10.1016/j.pnpbp.2003.11.016. PMID 15093948. 
  8. "Deprenyl (selegiline): the history of its development and pharmacological action". Acta Neurol Scand Suppl 95: 57–80. 1983. doi:10.1111/j.1600-0404.1983.tb01517.x. PMID 6428148. 
  9. "The pharmacological profile of (-)deprenyl (selegiline) and its relevance for humans: a personal view". Pharmacology & Toxicology 70 (5 Pt 1): 317–321. May 1992. doi:10.1111/j.1600-0773.1992.tb00480.x. PMID 1608919. 
  10. "The aphrodisiac effect of low doses of (-) deprenyl in male rats". Pol J Pharmacol Pharm 34 (5–6): 303–308. 1982. PMID 6821215. 
  11. 11.0 11.1