Devazepide

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Devazepide
Devazepide.svg
Clinical data
ATC code
  • none
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
KEGG
ChEMBL
ECHA InfoCard 100.208.547
Chemical and physical data
Formula C25H20N4O2
Molar mass 408.452 g/mol
3D model (JSmol)
 NYesY (what is this?)  (verify)

Devazepide[1] (L-364,718, MK-329) is benzodiazepine drug, but with quite different actions from most benzodiazepines, lacking affinity for GABAA receptors and instead acting as an CCKA 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 CCKA receptor.[6][7]

Synthesis[edit]

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

See also[edit]

References[edit]

  1. ^ US Patent 4820834
  2. ^ Hill, DR; Woodruff, GN (Sep 1990). "Differentiation of central cholecystokinin receptor binding sites using the non-peptide antagonists MK-329 and L-365,260". Brain Research. 526 (2): 276–83. PMID 2257485. doi:10.1016/0006-8993(90)91232-6. 
  3. ^ Cooper, SJ; Dourish, CT (Dec 1990). "Multiple cholecystokinin (CCK) receptors and CCK-monoamine interactions are instrumental in the control of feeding". Physiology and Behaviour. 48 (6): 849–57. PMID 1982361. doi:10.1016/0031-9384(90)90239-z. 
  4. ^ Cooper, SJ; Dourish, CT; Clifton, PG (January 1992). "CCK antagonists and CCK-monoamine interactions in the control of satiety". Am. J. Clin. Nutr. 55: 291S–295S. PMID 1728842. 
  5. ^ Scarpignato, C; Varga, G; Corradi, C (1993). "Effect of CCK and its antagonists on gastric emptying". Journal of Physiology Paris. 87 (5): 291–300. PMID 8298606. doi:10.1016/0928-4257(93)90035-r. 
  6. ^ Weller, A (Jul 2006). "The ontogeny of postingestive inhibitory stimuli: examining the role of CCK". Developmental Psychobiology. 48 (5): 368–79. PMID 16770766. doi:10.1002/dev.20148. 
  7. ^ Savastano, DM; Covasa, M (Oct 2007). "Intestinal nutrients elicit satiation through concomitant activation of CCK(1) and 5-HT(3) receptors". Physiology and Behaviour. 92 (3): 434–42. PMID 17531277. doi:10.1016/j.physbeh.2007.04.017. 
  8. ^ "Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists". Journal of Medicinal Chemistry. 31: 2235–2246. doi:10.1021/jm00120a002. 
  9. ^ EP 1492540