Devazepide

Devazepide
Systematic (IUPAC) name
N-(1-methyl- 2-oxo- 5-phenyl- 3H-1,4-benzodiazepin-3-yl)- 1H-indole -2-carboxamide
Clinical data
Pregnancy cat.  ?
Legal status  ?
Identifiers
CAS number 103420-77-5 Y
ATC code None
PubChem CID 59751
IUPHAR ligand 878
UNII JE6P7QY7NH N
KEGG D02693 Y
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]

Evans, B. E.; Rittle, K. E.; DiPardo, R. M.; Freidinger, R. M.; Whitter,W. L.; People,W. T.; Lendell, G. F.; Veber, D. F.; Anderson, P. S.; Chang, R. S. L.; Lotti, V. J.; Cerino, D. J.; Chen, T. B.; Kling, P. J.; Kunkel, K. A.; Springer, J. P.; Hirschfield, J.; J. Med. Chem. 1988, 31, 2235.

http://dx.doi.org/10.1021/jm00120a002

EP 1492540 

See also

References

  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
Benzodiazepine derivatives
1,4-Benzodiazepines
1,5-Benzodiazepines
2,3-Benzodiazepines *
Triazolobenzodiazepines
Imidazobenzodiazepines
Oxazolobenzodiazepines
Thienodiazepines
Pyridodiazepines
Pyrazolodiazepines
Pyrrolodiazepines
Tetrahydroisoquinobenzodiazepines
Benzodiazepine prodrugs
* atypical activity profile (not GABAA receptor ligands)