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Benzylidene ketal derivatives as M2 muscarinic receptor antagonists |
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| Authors: | Boyle C D Chackalamannil S Chen L Y Dugar S Pushpavanam P Billard W Binch H Crosby G Cohen-Williams M Coffin V L Duffy R A Ruperto V Lachowicz J E |
| Affiliation: | Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA |
| Abstract: | Benzylidene ketal derivatives were investigated as selective M2 receptor antagonists for the treatment of Alzheimer's disease. Compound 10 was discovered to have subnanomolar M2 receptor affinity and 100-fold selectivity against other muscarinic receptors. Also, 10 demonstrated in vivo efficacy in rodent models of muscarinic activity and cognition. |
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