Chemistry:LM22A-4
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Short description: Chemical compound
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Formula | C15H21N3O6 |
Molar mass | 339.348 g·mol−1 |
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LM22A-4 is a synthetic, selective small-molecule partial agonist of TrkB (EC50 for TrkB activation = 200–500 pM; IC50 for inhibition of BDNF binding to TrkB = 47 nM; IA = ~85%), the main receptor of brain-derived neurotrophic factor.[1][2][3] It has been found to possess poor blood-brain-barrier penetration when administered systemically, so LM22A-4 has been given to animals instead via intranasal administration, with central nervous system TrkB activation observed.[3][4] The compound produces neurogenic and neuroprotective effects in animals,[3][5][6] and shows beneficial effects on respiration in animal models of Rett syndrome.[2][citation needed][7]
See also
References
- ↑ "Small molecule BDNF mimetics activate TrkB signaling and prevent neuronal degeneration in rodents". The Journal of Clinical Investigation 120 (5): 1774–85. May 2010. doi:10.1172/JCI41356. PMID 20407211.
- ↑ 2.0 2.1 Neurotrophic Factors. Springer Science & Business Media. 25 March 2014. pp. 490–491. ISBN 978-3-642-45106-5. https://books.google.com/books?id=BN24BAAAQBAJ&pg=PA490.
- ↑ 3.0 3.1 3.2 Annual Reports in Medicinal Chemistry. Elsevier Science. 24 September 2014. pp. 68–. ISBN 978-0-12-800372-5. https://books.google.com/books?id=OCOOAwAAQBAJ&pg=PA68.
- ↑ Molecular Basis of Memory. Elsevier Science. 30 January 2014. pp. 183–. ISBN 978-0-12-420200-9. https://books.google.com/books?id=g4gpAgAAQBAJ&pg=PA183.
- ↑ Alzheimer's Disease: Targets for New Clinical Diagnostic and Therapeutic Strategies. CRC Press. 26 April 2012. pp. 189–. ISBN 978-1-4398-2708-6. https://books.google.com/books?id=cpza1iyDWLcC&pg=PA189.
- ↑ "Possible protective action of neurotrophic factors and natural compounds against common neurodegenerative diseases". Neural Regeneration Research 9 (16): 1506–8. August 2014. doi:10.4103/1673-5374.139474. PMID 25317165.
- ↑ Behavioral Genetics of the Mouse: Volume 2, Genetic Mouse Models of Neurobehavioral Disorders. Cambridge University Press. 25 September 2014. pp. 139–. ISBN 978-1-316-06140-4. https://books.google.com/books?id=6kdcBAAAQBAJ&pg=PA139.
Original source: https://en.wikipedia.org/wiki/LM22A-4.
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