Synthesis and pharmacological evaluation of analogues of benzyl quinolone carboxylic acid (BQCA) designed to bind irreversibly to an allosteric site of the M1 …

…, PM Sexton, B Capuano, A Christopoulos…

Index: Huynh, Tracey; Valant, Celine; Crosby, Ian T.; Sexton, Patrick M.; Christopoulos, Arthur; Capuano, Ben Journal of Medicinal Chemistry, 2013 , vol. 56, # 20 p. 8196 - 8200

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Citation Number: 10

Abstract

Activation of the M1 muscarinic acetylcholine receptor (mAChR) is a prospective treatment for alleviating cognitive decline experienced in central nervous system (CNS) disorders. Current therapeutics indiscriminately enhance the activity of the endogenous neurotransmitter ACh, leading to side effects. BQCA is a positive allosteric modulator and allosteric agonist at the M1 mAChR that has high subtype selectivity and is a promising ...