[HTML][HTML] Mechanistic insights into allosteric structure-function relationships at the M1 muscarinic acetylcholine receptor
Benzylquinolone carboxylic acid (BQCA) is the first highly selective positive allosteric
modulator (PAM) for the M 1 muscarinic acetylcholine receptor (mAChR), but it possesses
low affinity for the allosteric site on the receptor. More recent drug discovery efforts identified
3-((1S, 2S)-2-hydroxycyclohexyl)-6-((6-(1-methyl-1H-pyrazol-4-yl) pyridin-3-yl) methyl)
benzo [h] quinazolin-4 (3H)-one (referred to herein as benzoquinazolinone 12) as a more
potent M 1 mAChR PAM with a structural ancestry originating from BQCA and related …
modulator (PAM) for the M 1 muscarinic acetylcholine receptor (mAChR), but it possesses
low affinity for the allosteric site on the receptor. More recent drug discovery efforts identified
3-((1S, 2S)-2-hydroxycyclohexyl)-6-((6-(1-methyl-1H-pyrazol-4-yl) pyridin-3-yl) methyl)
benzo [h] quinazolin-4 (3H)-one (referred to herein as benzoquinazolinone 12) as a more
potent M 1 mAChR PAM with a structural ancestry originating from BQCA and related …