Devazepide Explained

Devazepide^[1] (L-364,718, MK-329) is benzodiazepine drug, but with quite different actions from most benzodiazepines, lacking affinity for GABA_A receptors and instead acting as an CCK_A receptor antagonist.^[2] It increases appetite and accelerates gastric emptying,^{[3] [4]} and has been suggested as a potential treatment for a variety of gastrointestinal problems including dyspepsia, gastroparesis and gastric reflux.^[5] It is also widely used in scientific research into the CCK_A receptor.^{[6] [7]}

Synthesis

Devazepide is synthesised in a similar manner to other benzodiazepines.^{[8] [9]}

See also

• Benzodiazepine
• Cholecystokinin antagonist

References

1. US . 4820834 . Benzodiazepine analogs. 1989-04-11. Merck & Co. Inc.. Evans. Ben E.. Freidinger. Roger M.. Bock. Mark G..
2. Hill DR, Woodruff GN . Differentiation of central cholecystokinin receptor binding sites using the non-peptide antagonists MK-329 and L-365,260 . Brain Research . 526 . 2 . 276–83 . September 1990 . 2257485 . 10.1016/0006-8993(90)91232-6 . 23851131 .
3. Cooper SJ, Dourish CT . Multiple cholecystokinin (CCK) receptors and CCK-monoamine interactions are instrumental in the control of feeding . Physiology & Behavior . 48 . 6 . 849–57 . December 1990 . 1982361 . 10.1016/0031-9384(90)90239-z . 24850080 .
4. Cooper SJ, Dourish CT, Clifton PG . CCK antagonists and CCK-monoamine interactions in the control of satiety . The American Journal of Clinical Nutrition . 55 . 1 Suppl . 291S–295S . January 1992 . 1728842 . 10.1093/ajcn/55.1.291s . free .
5. Scarpignato C, Varga G, Corradi C . Effect of CCK and its antagonists on gastric emptying . Journal of Physiology, Paris . 87 . 5 . 291–300 . 1993 . 8298606 . 10.1016/0928-4257(93)90035-r . 23725376 .
6. Weller A . The ontogeny of postingestive inhibitory stimuli: examining the role of CCK . Developmental Psychobiology . 48 . 5 . 368–79 . July 2006 . 16770766 . 10.1002/dev.20148 .
7. Savastano DM, Covasa M . Intestinal nutrients elicit satiation through concomitant activation of CCK(1) and 5-HT(3) receptors . Physiology & Behavior . 92 . 3 . 434–42 . October 2007 . 17531277 . 10.1016/j.physbeh.2007.04.017 . 5566756 .
8. Evans BE, Rittle KE, Bock MG, DiPardo RM, Freidinger RM, Whitter WL, Lundell GF, Veber DF, Anderson PS, Chang RS . 6 . Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists . Journal of Medicinal Chemistry . 31 . 12 . 2235–46 . December 1988 . 2848124 . 10.1021/jm00120a002 .
9. EP. 1492540. The use of devazepide as analgesic agent. 2005-01-05. ML Laboratories plc. Jackson. Karen.