Ce. Pendley et al., RP-73870, A GASTRIN CHOLECYSTOKININ-B RECEPTOR ANTAGONIST WITH POTENTANTIULCER ACTIVITY IN THE RAT/, The Journal of pharmacology and experimental therapeutics, 273(3), 1995, pp. 1015-1022
RP 73870, the racemic potassium salt of -methyl]-3-ureido}-3-phenyl}-2
-ethylsulfonate-(RS) is a potent, reversible antagonist of both gastri
n and cholecystokinin-B receptors in guinea pig and rat tissues. This
compound is a potent inhibitor of pentagastrin-stimulated gastric acid
secretion in the perfused rat stomach. RP 73870 also inhibits basal g
astric acid secretion in the rat, although at doses higher than that r
equired for inhibition of pentagastrin-stimulated gastric acid secreti
on. RP 73870 is a potent inhibitor of aspirin-induced gastric damage i
n the rat. In the prevention of aspirin-induced gastric damage, RP 738
70, given p.o., was 10-fold less potent than when given i.v. RP 73870
was as potent as a H-2 receptor antagonist or proton pump inhibitor in
the prevention of cysteamine-induced duodenal ulcers in the rat. Rela
tive to other gastrin/cholecystokinin-B antagonists, RP 73870 demonstr
ates greater affinity to gastrin binding sites, and possesses a unique
spectrum of in vivo biological activities appropriate for an anti-ulc
er indication.