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VU-0238429 is a drug which acts as a selective positive allosteric modulator for the muscarinic acetylcholine receptor M. It was the first selective ligand developed for the M 5 5 subtype, and is structurally derived from older M  1-selective positive allosteric modulators such as VU-0119498.  Replacing the  O-methyl- by a phenylgroup further improves the receptor subtype selectivity ( VU-0400265).
References [ edit ]
^ Bridges TM, Marlo JE, Niswender CM, et al. (June 2009). "Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins". Journal of Medicinal Chemistry. 52 (11): 3445–8. doi: 10.1021/jm900286j. PMID 19438238.
^ Conn PJ, Jones CK, Lindsley CW (March 2009). "Subtype-selective allosteric modulators of muscarinic receptors for the treatment of CNS disorders". Trends in Pharmacological Sciences. 30 (3): 148–55. doi: 10.1016/j.tips.2008.12.002. PMC . 2907736 PMID 19201489.
^ Bridges, T. M.; Kennedy, J. P.; Hopkins, C. R.; Conn, P. J.; Lindsley, C. W. (2010). "Heterobiaryl and heterobiaryl ether derived M5 positive allosteric modulators". Bioorganic & Medicinal Chemistry Letters. 20 (19): 5617. doi: 10.1016/j.bmcl.2010.08.042. PMC . 3179183 PMID 20801651.