Ability of mosapride to bind to 5-HT4 receptor in the human stomach.
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 autoradiography. [125I]SB207710 binding sites were detected in the muscle layer including the myenteric plexus of the stomach from both humans and guinea pigs, although the binding was observed more clearly and densely in the stomach of guinea pigs than humans. Mosapride as well as SB204070 inhibited the binding of [125I]SB207710. Thus, mosapride possesses the ability to bind to 5-HT4 receptors of human stomach and may modulate the motility, as in the case of guinea pig stomach.
Sakurai-Yamashita
Y
Y
Department of Pharmacology, Nagasaki University School of Medicine, Japan.
Takada
K
K
Takemura
K
K
Yamashita
K
K
Enjoji
A
A
Kanematsu
T
T
Taniyama
K
K
D000368:Aged; D000818:Animals; D001549:Benzamides / Q000378:metabolism* / Q000494:pharmacology; D001665:Binding Sites; D001667:Binding, Competitive; D004146:Dioxanes / Q000378:metabolism / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D005260:Female; D005753:Gastric Mucosa / Q000378:metabolism*; D005765:Gastrointestinal Agents / Q000378:metabolism* / Q000494:pharmacology; D006168:Guinea Pigs; D006801:Humans; D007457:Iodine Radioisotopes; D008297:Male; D008875:Middle Aged; D009025:Morpholines / Q000378:metabolism* / Q000494:pharmacology; D010880:Piperidines / Q000378:metabolism / Q000494:pharmacology; D011869:Radioligand Assay; D011985:Receptors, Serotonin / Q000378:metabolism*; D044422:Receptors, Serotonin, 5-HT4; D012702:Serotonin Antagonists / Q000378:metabolism / Q000494:pharmacology; D013270:Stomach / Q000187:drug effects
D001549:Benzamides; D004146:Dioxanes; D005765:Gastrointestinal Agents; D007457:Iodine Radioisotopes; D009025:Morpholines; D010880:Piperidines; D011985:Receptors, Serotonin; C088873:SB 207710; D012702:Serotonin Antagonists; C084858:SB 204070A; D044422:Receptors, Serotonin, 5-HT4; C062720:mosapride