Devazepide

From Wikipedia, the free encyclopedia
Jump to: navigation, search
Devazepide
Devazepide.png
Systematic (IUPAC) name
N-(1-methyl- 2-oxo- 5-phenyl- 3H-1,4-benzodiazepin-3-yl)- 1H-indole -2-carboxamide
Clinical data
Legal status
?
Identifiers
CAS number 103420-77-5 YesY
ATC code None
PubChem CID 443375
IUPHAR ligand 878
ChemSpider 391607 N
UNII JE6P7QY7NH N
KEGG D02693 YesY
ChEMBL CHEMBL9506 N
Chemical data
Formula C25H20N4O2 
Mol. mass 408.452 g/mol
 N (what is this?)  (verify)

Devazepide[1] (L-364,718, MK-329) is a drug which is structurally derived from the benzodiazepine family, but with quite different actions from most benzodiazepines, lacking affinity for GABAA receptors and instead acting as a cholecystokinin antagonist selective for the CCKA subtype.[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 CCKA receptor.[6][7]

Preparation of Devazepide. doi:10.1021/jm00120a002 EP 1492540 


Actually, maybe final methylation step need to check in doi.

See also[edit]

References[edit]

  1. ^ US Patent 4820834
  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. 1990 Sep 3;526(2):276-83. PMID 2257485
  3. ^ Cooper SJ, Dourish CT. Multiple cholecystokinin (CCK) receptors and CCK-monoamine interactions are instrumental in the control of feeding. Physiology and Behaviour. 1990 Dec;48(6):849-57. PMID 1982361
  4. ^ Cooper SJ, Dourish CT, Clifton PG. CCK antagonists and CCK-monoamine interactions in the control of satiety. American Journal of Clinical Nutrition. 1992 Jan;55(1 Suppl):291S-295S. PMID 1728842
  5. ^ Scarpignato C, Varga G, Corradi C. Effect of CCK and its antagonists on gastric emptying. Journal of Physiology Paris. 1993;87(5):291-300. PMID 8298606
  6. ^ Weller A. The ontogeny of postingestive inhibitory stimuli: examining the role of CCK. Developmental Psychobiology. 2006 Jul;48(5):368-79. PMID 16770766
  7. ^ Savastano DM, Covasa M. Intestinal nutrients elicit satiation through concomitant activation of CCK(1) and 5-HT(3) receptors. Physiology and Behaviour. 2007 Oct 22;92(3):434-42. PMID 17531277