Autoradiographic localization of ylonium bromide binding sites in the rat gastrointestinal tract.

The anatomical localization of the binding sites of the spasmolytic drug octylonium bromide (OB) in the rat gastrointestinal tract was analyzed by use of light microscope autoradiography. The drug was visualized after in vitro incubation of frozen sections of the gastrointestinal tract with a 10 nM concentration of 14C-OB and after in vivo injection into the ascending, transverse, descending and sigmoidal portions of the colon. In vitro experiments demonstrated the specific accumulation of 14C-OB within the colonic and rectal smooth muscle. In contrast, no specific binding of the radiolabeled drug was noticeable in the stomach or in the small intestine. In vivo intracolonic injection of 14C-OB showed a significant accumulation of the drug in the colonic musculature 2 min after administration. The predominant localization of 14C-OB in the colonic and rectal musculature could explain its effectiveness in suppressing the amplitude and frequency of colonic contractions and in controlling the irritable bowel syndrome.