LM22A-4

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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

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