Ability of mosapride, a gastrokinetic agent, to bind to 5-HT4 receptor was
examined in the stomach of human and guinea pig by in vitro receptor autora
diography. [(125)]SB207710 binding sites were detected in the muscle layer
including the myenteric plexus of the stomach from both humans and guinea p
igs, although the binding was observed more clearly and densely in the stom
ach of guinea pigs than humans. Mosapride as well as SB204070 inhibited the
binding of [I-125]SB207710. Thus. mosapride possesses the ability to bind
to 5-HT4 receptors of human stomach and may modulate the motility, as in th
e case of guinea pig stomach.