Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core.Wood MR, Noetzel MJ, Engers JL, Bollinger KA, Melancon BJ, Tarr JC, Han C, West M, Gregro AR, Lamsal A, Chang S, Ajmera S, Smith E, Chase P, Hodder PS, Bubser M, Jones CK, Hopkins CR, Emmitte KA, Niswender CM, Wood MW, Duggan ME, Conn PJ, Bridges TM, Lindsley CW
(2016)
Bioorg Med Chem Lett 26: 3029-3033
MeSH Terms: Allosteric Regulation, Animals, Brain, Humans, Microsomes, Liver, Piperidines, Pyrimidines, Quinazolines, Rats, Receptor, Muscarinic M4, Structure-Activity Relationship, ThiophenesAdded April 6, 2017