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Autoradiographic and confocal laser microscopic observation show lafutidine binds to CGRP-immunoreactive nerves as well as gastric parietal cells

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image of Inflammopharmacology

The present study was undertaken to observe the binding sites of lafutidine, a newly invented H2 receptor antagonist ((+/-)-2-(furfurylsulfinyl)-N-[4-[4-(piperidinomethyl)-2-pyridyl]oxy-(Z)-2 butenyl] acetamide), in the Mongolian gerbil and human gastric mucosa using unfixed cryostat section or incubation with aqueous solution of tritiated lafutidine, followed by in vitro autoradiography or autoradiography of soluble compounds. The localization of calcitonin gene-related peptide immunoreactivity was compared with the lafutidine binding sites. As a result, lafutidine-specific binding sites in the body of the fundic glands were accumulated on the parietal cells, while in the neck and base of the fundic glands, lafutidine was found to bind to the CGRP immunoreactive nerves. In the human fundic mucosa, the lafutidine bindings were also observed on the enteric nerves as well as the parietal cells. In conclusion, autoradiographic studies have shown that lafutidine effector sites coincided with the CGRP-immunoreactive nerves as well as the parietal cells.


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