Devazepide_product_DataBase

Bioactivity	Devazepide (L-364,718) is a potent, competitive, selective and orally active nonpeptide antagonist of cholecystokinin (CCK) receptor, with IC50s of 81 pM, 45 pM and 245 nM for rat pancreatic, bovine gallbladder and guinea pig brain CCK receptors, respectively. Devazepide (L-364,718) is effective for gastrointestinal disorders[1].
Target	IC50: 45 pM (Rat pancreatic CCK receptor), 81 pM (Bovine gallbladder CCK receptor), 245 nM (Guinea pig brain CCK receptor)
In Vivo	Devazepide (oral gavage; 4 mg/kg; twice per day) significantly accelerates cholesterol crystallization and crystal growth to microlithiasis, and the formation of gallstones in mice[2].Devazepide (intraperitoneal injection; 0.1-1 mg/kg) has opposite effects on spontaneous locomotor activity, and on caerulein- and apomorphine-induced hypomotility in the mouse[3]. Animal Model:
Name	Devazepide
CAS	103420-77-5
Formula	C25H20N4O2
Molar Mass	408.45
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	-20°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Reference	[1]. Chang RS, et al. Biochemical and pharmacological characterization of an extremely potent and selective nonpeptide cholecystokinin antagonist. Proc Natl Acad Sci U S A. 1986 Jul;83(13):4923-6. [2]. Helen H Wang, et al. The cholecystokinin-1 receptor antagonist devazepide increases cholesterol cholelithogenesis in mice. Eur J Clin Invest [3]. E Vasar, et al. Differential involvement of CCK-A and CCK-B receptors in the regulation of locomotor activity in the mouse. Psychopharmacology (Berl). 1991;105(3):393-9

PeptideDB

Devazepide

CAS: 103420-77-5 F: C25H20N4O2 W: 408.45