L-365260 hemihydrate is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B) , with K i s of 1.9 nM and 2.0 nM, respectively. L-365260 hemihydrate interacts in a stereoselective and competitive manner
In Vitro:L-365260 hemihydrate exhibits a similar high affinity for brain CCK-B receptors of rats, mice and man, and a lower affinity for gastrin and brain CCK-B (IC 50 =20-40 nM) receptors in dog tissues. L-365260 (1 μM) hemihydrate strongly attenuates the CC
In Vivo:L-365260 hemihydrate (0.1-30mg/kg; p.o.) antagonizes gastrin-stimulated acid secretion in mice (ED 50 =0.03mg/kg), rats (ED 50 =0.9mg/kg) and guinea pigs (ED 50 =5.1mg/kg). L-365260 hemihydrate (0.01-10mg/kg; s.c.) enhances analgesia induced by
Biological Activity:L-365260 hemihydrate is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B) , with K i s of 1.9 nM and 2.0 nM, respectively. L-365260 hemihydrate interacts in a stereoselective and competitive manner