Devazepide

Devazepide is a nonpeptide antagonist of the cholecystokinin 1 (CCK₁) receptor (K_i = 0.3 nM).¹ It is selective for CCK₁ over the CCK₂ receptor (K_i = 342 nM). Devazepide inhibits CCK-8-induced amylase release in isolated dispersed rat pancreatic acini (IC₅₀ = 25.4 nM). It reduces CCK-8-induced decreases in gastric emptying and food intake in rats (ED₅₀s = 140 and 321 µg/kg, respectively), as well as CCK-8-induced contractions of colon and gall bladder in rabbits and cats, respectively (ED₅₀s = 34 and 210 µg/kg, respectively).² Devazepide (1 mg/kg) enhances morphine-induced increases in tail-flick latency and prevents the development of morphine tolerance, but does not affect morphine dependence, in rats.³ It also induces apoptosis and cell cycle arrest at the G₁/G₀ phase in, and inhibits the migration of, 5637 bladder cancer cells when used at a concentration of 25 µM.⁴

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1. Martín-Martínez, M., Bartolomé-Nebreda, J.M., Gómez-Monterrey, I., et al. Synthesis and stereochemical structure-activity relationships of 1,3-dioxoperhydropyrido[1,2-c]pyrimidine derivatives: Potent and selective cholecystokinin-A receptor antagonists. J. Med. Chem. 40(21), 3402-3407 (1997).

2. Lotti, V.J., Pendleton, R.G., Gould, R.J., et al. In vivo pharmacology of L-364,718, a new potent nonpeptide peripheral cholecystokinin antagonist. J. Pharmacol. Exp. Ther. 241(1), 103-109 (1987).

3. Dourish, C.T., Hawley, D., and Iversen, S.D. Enhancement of morphine analgesia and prevention of morphine tolerance in the rat by the cholecystokinin antagonist L-364,718. Eur. J. Pharmacol. 147(3), 469-472 (1988).

4. Zhang, H., Bao, X., Zhang, J., et al. Devazepide suppresses cell proliferation and migration, and induces apoptosis in bladder carcinoma. Transl. Androl. Urol. 10(5), 2113-2121 (2021).