期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 56, 期 20, 页码 8196-8200出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm401032k
关键词
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资金
- National Health and Medical Research Council (NHMRC) of Australia [519461]
- Australian Postgraduate Award (APA)
The M, mAChR is implicated in several CNS disorders and possesses an allosteric binding site for which ligands modulating the affinity and/or efficacy of ACh may be exploited for selective receptor targeting. We report the synthesis of a focused library of putative M-4 PAMs derived from VU0152100 and VU10005. These compounds investigate the pharmacological effects of previously identified methoxy and fluoro substituents, providing useful estimates of affinity (K-B), cooperativity (alpha beta), and direct agonist properties (tau(B)).
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