LM22A-4

LM22A-4
Clinical data
ATC code	None;
Identifiers
	IUPAC name 1-N,3-N,5-N-tris(2-Hydroxyethyl)benzene-1,3,5-tricarboxamide;
CAS Number	37988-18-4;
PubChem CID	2054170;
ChemSpider	1548402;
CompTox Dashboard (EPA)	DTXSID201045819 ;
Chemical and physical data
Formula	C15H21N3O6
Molar mass	339.348 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C1=C(C=C(C=C1C(=O)NCCO)C(=O)NCCO)C(=O)NCCO;
	InChI InChI=1S/C15H21N3O6/c19-4-1-16-13(22)10-7-11(14(23)17-2-5-20)9-12(8-10)15(24)18-3-6-21/h7-9,19-21H,1-6H2,(H,16,22)(H,17,23)(H,18,24); Key:RGWJKANXFYJKHN-UHFFFAOYSA-N;

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]

References

^ Massa, Stephen M.; Yang, Tao; Xie, Youmei; Shi, Jian; Bilgen, Mehmet; Joyce, Jeffrey N.; Nehama, Dean; Rajadas, Jayakumar; Longo, Frank M. (2010). "Small molecule BDNF mimetics activate TrkB signaling and prevent neuronal degeneration in rodents". Journal of Clinical Investigation. 120 (5): 1774–1785. doi:10.1172/JCI41356. ISSN 0021-9738. PMC 2860903. PMID 20407211.
^ ^a ^b Gary Lewin; Bruce D. Carter (25 March 2014). Neurotrophic Factors. Springer Science & Business Media. pp. 490–491. ISBN 978-3-642-45106-5.
^ ^a ^b ^c Annual Reports in Medicinal Chemistry. Elsevier Science. 24 September 2014. pp. 68–. ISBN 978-0-12-800372-5.
^ Molecular Basis of Memory. Elsevier Science. 30 January 2014. pp. 183–. ISBN 978-0-12-420200-9.
^ Renee D. Wegrzyn; Alan S. Rudolph (26 April 2012). Alzheimer's Disease: Targets for New Clinical Diagnostic and Therapeutic Strategies. CRC Press. pp. 189–. ISBN 978-1-4398-2708-6.
^ Numakawa, Tadahiro (2014). "Possible protective action of neurotrophic factors and natural compounds against common neurodegenerative diseases". Neural Regeneration Research. 9 (16): 1506. doi:10.4103/1673-5374.139474. ISSN 1673-5374. PMC 4192965.{{cite journal}}: CS1 maint: unflagged free DOI (link)
^ Susanna Pietropaolo; Frans Sluyter; Wim E. Crusio (25 September 2014). Behavioral Genetics of the Mouse: Volume 2, Genetic Mouse Models of Neurobehavioral Disorders. Cambridge University Press. pp. 139–. ISBN 978-1-316-06140-4.

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