Ebrotidine--a new H2-receptor antagonist with mucosal strengthening activity.
The mechanism of gastric mucosal protection by ebrotidine against ethanol-induced mucosal injury was investigated in rats treated intragastrically either with the drug or vehicle. Results of macroscopic assessment revealed that ebrotidine at doses of 50mg and higher/kg body weight effectively prevented mucosal injury, and that the maximal protective effect was achieved by 1h. Physicochemical analysis established that ebrotidine evoked 30% increase in mucus gel dimension, and showed 20% increase in phospholipids, and the content of sulfo- (18%) and sialomucins (21%). This was accompanied by 1.4-fold increase in mucus gel viscosity, 16% increase in H+ retardation capacity, and 65% increase in hydrophobicity. Our data show that ebrotidine is a unique H2-antagonist capable of enhancement of the physicochemical characteristics of gastric mucus.
Piotrowski
J
J
Research Center, New Jersey Dental School, University of Medicine and Dentistry of New Jersey, Newark 07103-2400.
Yamaki
K
K
Morita
M
M
Slomiany
A
A
Slomiany
B L
BL
D000818:Animals; D001557:Benzenesulfonates / Q000008:administration & dosage / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D000431:Ethanol / Q000037:antagonists & inhibitors / Q000633:toxicity; D005753:Gastric Mucosa / Q000187:drug effects* / Q000293:injuries / Q000473:pathology; D005782:Gels; D006023:Glycoproteins / Q000378:metabolism; D006635:Histamine H2 Antagonists / Q000008:administration & dosage / Q000494:pharmacology*; D009093:Mucus / Q000737:chemistry / Q000187:drug effects; D010743:Phospholipids / Q000378:metabolism; D051381:Rats; D013844:Thiazoles / Q000008:administration & dosage / Q000494:pharmacology*; D014783:Viscosity
D001557:Benzenesulfonates; D005782:Gels; D006023:Glycoproteins; D006635:Histamine H2 Antagonists; D010743:Phospholipids; D013844:Thiazoles; D000431:Ethanol; C075156:ebrotidine