Author/Authors :
Hiroshi Harada، نويسنده , , Hiroshi Yamazaki، نويسنده , , Yoshihito Toyotomi، نويسنده , , Hirotaka Tateishi، نويسنده , , Yukiko Mine، نويسنده , , Naoyuki Yoshida، نويسنده , , Shiro Kato، نويسنده ,
Abstract :
A series of novel N-[1-(1-substituted 4-piperidinylmethyl)-4-piperidinyl]benzamides was prepared and its compounds were evaluated for their binding to 5-HT4 receptors and effects on gastrointestinal motility in conscious dogs. 4-Amino-N-[1-[1-(4-aminobutyl)-4-piperidinylmethyl]-4-piperidinyl]-5-chloro-2-methoxybenzamide (15) was found to have a potent binding affinity for 5-HT4 receptors (IC50: 6.47 nM) and showed excellent colonic prokinetic activity.