2-METHYL-8-(PHENYLMETHOXY)IMIDAZO[1,2-A]PYRIDINE-3-ACETONITRILE

Description

SCH 28080 is a reversible K⁺-competitive inhibitor of H⁺/K⁺-ATPases that is best known for its ability to block acid secretion through its action against the gastric H⁺/K⁺-ATPase (IC₅₀ = 1.3 μM). It is effective against gastric H⁺/K⁺-ATPases from a variety of species and can inhibit colonic H⁺/K⁺-ATPases, but this activity appears to be species-dependent. SCH 28080 is also used to investigate the role of H⁺/K⁺-ATPases in non-mammalian organisms and to distinguish the actions of H⁺/K⁺-ATPases from other ATP-dependent transporters.

Uses

SCH 28080 is a potent inhibitor of H+,K+-ATPase.

Definition

ChEBI: 2-(2-methyl-8-phenylmethoxy-3-imidazo[1,2-a]pyridinyl)acetonitrile is an imidazopyridine.

Biological Activity

Potent inhibitor of H + ,K + -ATPase (IC 50 = 20 nM); binds to the K + recognition site and is competitive with respect to K + . Inhibits gastric acid secretion in vitro and in vivo .

Biochem/physiol Actions

SCH-28080 is a potent inhibitor of gastric H+ and K+-ATPase. The novel antiulcer agents, SCH-28080 and SCH-32651 were examined for their ability to inhibit the H+K+ ATPase enzyme activity in a preparation of microsomal membranes from rabbit fundic mucosa. SCH- 28080 inhibited the isolated enzyme activity with a potency similar to omeprazole, IC50s of 2.5 and 4.0 μM respectively. SCH 32651 was less potent exhibiting an IC50 of 200.0 μM. Both compounds may therefore exert their antisecretory activity via a direct inhibition of the parietal cell H+K+ ATPase.

storage

Room temperature