Novel M(1) allosteric ligands: a patent review.

摘要: Introduction: There is substantial evidence from preclinical and early proof-of-concept studies suggesting that selective modulation of the M1 muscarinic receptor efficacious in cognitive models Alzheimer's disease (AD) antipsychotic schizophrenia. For example, a number nonselective agonists have previously shown positive effects on function AD patients, but were limited due to cholinergic adverse events thought be mediated by pan activation M2 M5 subtypes. Thus, there need identify activators evaluate their potential disorders. One strategy confer selectivity for identification allosteric or modulators, which would target an site rather than highly conserved orthosteric acetylcholine binding site. Areas covered: This review discusses its therapeutic value treatment ...