Author/Authors :
Nicholas J. Murgolo، نويسنده , , Joseph Kozlowski، نويسنده , , Melissa A. B. Tice، نويسنده , , Frank P. Hollinger، نويسنده , , Joan E. Brown، نويسنده , , Guowei Zhou، نويسنده , , Lisa A. Taylor، نويسنده , , Robert D. McQuade، نويسنده ,
Abstract :
An analog (SCH55112) of pirenzepine was prepared in which the N4 piperazyl nitrogen was replaced with carbon. This structrual change abolished the 55-fold m1/m2 selectivity of pirenzepine due to specific loss of m1 affinity. Mutagenesis mapping and modeling studies suggested this change was due to loss of a hydrogen bond to m1 Thr32 (m2Ala30).
