Effect of ebrotidine on gastric mucosal EGF and PDGF receptor expression.
The effect of ebrotidine, a new H2-blocker with gastroprotective properties, on the expression of gastric mucosal epidermal growth factor (EGF) and platelet-derived growth factor (PDGF) receptors, was investigated. Mucosal cell membranes were isolated from rats receiving twice daily for 5 days a dose of 100mg/kg ebrotidine or 100mg/kg ranitidine or vehicle only. Assays for EGF and PDGF revealed the presence of both types of receptors, activation of which led to enhanced tyrosine kinase activity. The receptor binding values in the control group were 2.4 fmol for EGF and 1.45 fmol/mg protein for PDGF, whereas the values in the ebrotidine group increased for EGF by 65.7% and 38.6% for PDGF, but no such effect was observed with ranitidine. The results suggest that the gastroprotective properties of ebrotidine stem from its ability to stimulate the epithelial proliferative activities through the enhancement of EGF and PDGF receptors expression.
Piotrowski
J
J
Research Center, University of Medicine and Dentistry of New Jersey, Newark 07103-2400.
Czajkowski
A
A
Yotsumoto
F
F
Slomiany
A
A
Slomiany
B L
BL
D000818:Animals; D001557:Benzenesulfonates / Q000494:pharmacology*; D002462:Cell Membrane / Q000187:drug effects / Q000378:metabolism; D004815:Epidermal Growth Factor / Q000378:metabolism; D066246:ErbB Receptors / Q000096:biosynthesis* / Q000378:metabolism; D005753:Gastric Mucosa / Q000187:drug effects* / Q000378:metabolism; D006635:Histamine H2 Antagonists / Q000494:pharmacology*; D010766:Phosphorylation; D010982:Platelet-Derived Growth Factor / Q000378:metabolism; D011899:Ranitidine / Q000494:pharmacology; D051381:Rats; D017479:Receptors, Platelet-Derived Growth Factor / Q000096:biosynthesis* / Q000378:metabolism; D013844:Thiazoles / Q000494:pharmacology*; D014443:Tyrosine / Q000378:metabolism
D001557:Benzenesulfonates; D006635:Histamine H2 Antagonists; D010982:Platelet-Derived Growth Factor; D013844:Thiazoles; D014443:Tyrosine; D004815:Epidermal Growth Factor; D011899:Ranitidine; D066246:ErbB Receptors; D017479:Receptors, Platelet-Derived Growth Factor; C075156:ebrotidine