Author/Authors :
Craig D. Boyle، نويسنده , , Samuel Chackalamannil، نويسنده , , Lian-Yong Chen، نويسنده , , Sundeep Dugar، نويسنده , , Pradeep Pushpavanam، نويسنده , , William Billard، نويسنده , , Herbert BinchIII، نويسنده , , Gordon Crosby، نويسنده , , Mary Cohen-Williams، نويسنده , , Vicki L. Coffin، نويسنده , , Ruth A. Duffy، نويسنده , , Vilma Ruperto، نويسنده , , Jean E. Lachowicz، نويسنده ,
Abstract :
Benzylidene ketal derivatives were investigated as selective M2 receptor antagonists for the treatment of Alzheimerʹs 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.
