Positive allosteric modulator of muscarinic M1
= 198 nM). Displays no activity at M2
at concentrations up to 30 μ
M. Potentiates NMDA receptor currents in hippocampal neurons; activity reverses cognitive decifits in a rodent model of hippocampal-dependent memory. CNS penetrant.
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Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) Lead. Part II. Development of potent and highly selective M1 PAM.
Bridges et al.
Discovery and characterization of novel subtype-selective allosteric agonists for the investigation of M1 receptor function in the central nervous system.
Lebois et al.
ACS Chem.Neurosci., 2010;1:104
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