13996-06-0Relevant articles and documents
A structure-activity relationship study of the positive allosteric modulator LY2033298 at the M4 muscarinic acetylcholine receptor
Szabo, Monika,Huynh, Tracey,Valant, Celine,Lane, J. Robert,Sexton, Patrick M.,Christopoulos, Arthur,Capuano, Ben
supporting information, p. 1998 - 2003 (2015/11/17)
Positive allosteric modulators (PAMs) targeting the M4 muscarinic acetylcholine receptor (mAChR) offer greater sub-type selectivity and unique potential as central nervous system agents through their novel mode of action to traditional orthosteric ligands. In an attempt to elucidate the molecular determinants of allostery mediated by the exemplar thienopyridine M4 mAChR PAM, LY2033298, we report herein a systematic structure-activity relationship (SAR) study investigating different linkage points, halogen replacements to examine size and electronic effects, and different substitution combinations on the thienopyridine scaffold. We applied an operational model of allosterism to determine values of functional affinity (KB), cooperativity (αβ) and intrinsic agonism (τB) for all compounds.
SUBSTITUTED CARBOXAMIDES METHOD FOR PRODUCTION AND USE THEREOF AS TNF-ALPHA RELEASE INHIBITORS
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Page/Page column 42, (2010/11/24)
The invention relates to novel agents of formula (I), where R1 = aryl, optionally substituted with C1 to C5 alkyl, C2 to C5 alkenyl, C1 to C5 O-alkyl, aryloxy (O-aryl), C1/
