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Chemical Compound Review

MK-329     N-(2-methyl-3-oxo-6-phenyl- 2,5...

Synonyms: Devazepida, Devazepidum, Rac-Devazepide, CHEMBL39263, AGN-PC-000PLW, ...
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Disease relevance of DEVAZEPIDE


Psychiatry related information on DEVAZEPIDE


High impact information on DEVAZEPIDE


Chemical compound and disease context of DEVAZEPIDE

  • Pretreatment with devazepide receptor (1 microgram/kg) antagonized the inhibitory effects of buspirone and 8-OH-DPAT injected i.p. on emotional stress-induced colonic hyperkinesia but did not alter the effects of clonazepam (1 mg/kg).(ABSTRACT TRUNCATED AT 250 WORDS)[16]
  • Half of the rats (DEV group) were pretreated with devazepide (300 microg/kg body weight) and the other half (CON group) with vehicle, 30 min prior to CS training sessions and choice tests [17].
  • In experiment 1, 15 min of sucrose intake in adult, male Sprague-Dawley rats after 6 h of food deprivation was increased by devazepide (20 micrograms/kg) administered into the SPD artery whether given alone or in conjunction with cholecystokinin octapeptide (CCK-8, 2 micrograms/kg ip) [18].

Biological context of DEVAZEPIDE


Anatomical context of DEVAZEPIDE


Associations of DEVAZEPIDE with other chemical compounds

  • The response to CCK was inhibited in a competitive manner by the addition of the benzodiazepine analog, MK-329 [27].
  • We conclude that CCK receptor blockade with 10 mg MK-329 does not alter plasma insulin, glucagon, or glucose responses to a mixed meal [28].
  • 1. Three recently described non-peptide cholecystokinin (CCK) antagonists (devazepide, lorglumide, loxiglumide) have been studied for their antagonism of the contraction to cholecystokinin-octapeptide (CCK-OP) in human alimentary muscle and guinea-pig intestine [29].
  • The effect of oleate was abolished by the CCK-A receptor antagonist Devazepide (0.5 mg/kg), whereas the effect of butyrate persisted despite pretreatment with either Devazepide or a combination of the calcium channel inhibitors nifedipine (1 mg/kg) and the omega-conotoxins GVIA and SVIB (each 25 microg/kg) [30].
  • 4. Previous i.c.v. injection of devazepide, a CCKA receptor antagonist, (10 micrograms kg-1) antagonized the inhibitory effects of both CCK-8s and igmesine injected i.c.v. on dopamine-induced colonic hyperkinesia.(ABSTRACT TRUNCATED AT 250 WORDS)[31]

Gene context of DEVAZEPIDE

  • This paper reviews experiments in which devazepide (a selective CCK-A receptor antagonist) and L-365,260 (a selective CCK-B-gastrin receptor antagonist) have been used [32].
  • Thus, devazepide, a selective CCK-A receptor antagonist, produced a dose-related inhibition of the CCK-8-stimulated rise in circulating beta-endorphin concentrations [33].
  • Injected i.c.v., devazepide (L 364,718), a CCKA receptor antagonist, at 0.1 and 1 microgram/kg, abolished the effect of both JO 1784 and NPY; by contrast L365,260, a CCKB antagonist, required a dose of 10 micrograms/kg to block the antagonistic effect of NPY and JO 1784.(ABSTRACT TRUNCATED AT 250 WORDS)[34]
  • MK-329, a CCK-A receptor selective antagonist, at a dose of 20 nmol/kg fully inhibited the action of 20 nmol/kg CCK8, while 100 nmol/kg of (R)L-365,260, a CCK-B selective antagonist, had no effect on the CCK8 response [35].
  • In Experiments 1 and 2, pups received the selective CCK1 receptor antagonist devazepide (600 microg/kg), the selective CCK2 receptor antagonist L365,260 (600 microg/kg), or vehicle [36].

Analytical, diagnostic and therapeutic context of DEVAZEPIDE

  • In a double-blind, four-period crossover study eight subjects received single doses of 0.5, 2, or 10 mg MK-329, or placebo, followed by an intravenous infusion of CCK-8 (30 pmol/kg.h) [12].
  • In a double-blind, two-period, randomized crossover design, the subjects received either 10 mg MK-329 or placebo orally 3 hours 15 minutes before the meal, which contained 51CrCl3 as food marker [15].
  • Treatment with MK-329 enhances morphine analgesia and chronic treatment with MK-329 prevents the development of tolerance to morphine analgesia [37].
  • 3. The response to 100 pmol CCK was completely abolished by devazepide (0.5 mg kg-1) and by chronic subdiaphragmatic vagotomy performed 10-14 days prior to experimentation, indicating that CCK sensitivity was via CCKA receptors and exclusively mediated via vagal afferents rather than splanchnic or enteric afferents [38].
  • The suppression of food intake by beta-conglycinin peptone was abolished by an intravenous injection of devazepide, a selective peripheral CCK receptor antagonist [39].


  1. The cholecystokinin receptor antagonist devazepide enhances morphine-induced analgesia but not morphine-induced respiratory depression in the squirrel monkey. Dourish, C.T., O'Neill, M.F., Schaffer, L.W., Siegl, P.K., Iversen, S.D. J. Pharmacol. Exp. Ther. (1990) [Pubmed]
  2. Characterization of the receptors and mechanisms involved in the cardiovascular actions of sCCK-8 in the pithed rat. Gaw, A.J., Hills, D.M., Spraggs, C.F. Br. J. Pharmacol. (1995) [Pubmed]
  3. Involvement of spinal cholecystokininB receptors in mediating neurotensin hyperalgesia from the medullary nucleus raphe magnus in the rat. Urban, M.O., Smith, D.J., Gebhart, G.F. J. Pharmacol. Exp. Ther. (1996) [Pubmed]
  4. Enhancement of the cytotoxicity of cisplatin by the cholecystokinin antagonist MK-329 in a human pancreatic cancer cell line. Jamshidipour, R., Pinho, E.B., Hom, D.K., Howell, S.B. Cancer Chemother. Pharmacol. (1994) [Pubmed]
  5. Devazepide reverses the anorexic effect of simmondsin in the rat. Cokelaere, M.M., Busselen, P., Flo, G., Daenens, P., Decuypere, E., Kühn, E., Van Boven, M. J. Endocrinol. (1995) [Pubmed]
  6. Evidence for potentiation by CCK antagonists of the effect of cholecystokinin octapeptide in the elevated plus-maze. Vasar, E., Lang, A., Harro, J., Bourin, M., Bradwejn, J. Neuropharmacology (1994) [Pubmed]
  7. Reciprocal interaction of 5-hydroxytryptamine and cholecystokinin in the control of feeding patterns in rats. Grignaschi, G., Mantelli, B., Fracasso, C., Anelli, M., Caccia, S., Samanin, R. Br. J. Pharmacol. (1993) [Pubmed]
  8. Effect of intracerebroventricular and systemic injections of caerulein, a CCK analogue, on electrical self-stimulation and its interaction with the CCKA receptor antagonist, L-364,718 (MK-329). Hamilton, M.H., Rose, I.C., Herberg, L.J., de Belleroche, J.S. Psychopharmacology (Berl.) (1990) [Pubmed]
  9. Cholecystokinin-B receptor antagonists attenuate morphine dependence and withdrawal in rats. Lu, L., Huang, M., Liu, Z., Ma, L. Neuroreport (2000) [Pubmed]
  10. 'Anxiolytic' effect of CCK-antagonists on plus-maze behavior in mice. Rataud, J., Darche, F., Piot, O., Stutzmann, J.M., Böhme, G.A., Blanchard, J.C. Brain Res. (1991) [Pubmed]
  11. Endogenous cholecystokinin reduces feeding in young rats. Weller, A., Smith, G.P., Gibbs, J. Science (1990) [Pubmed]
  12. Effects of a novel cholecystokinin (CCK) receptor antagonist, MK-329, on gallbladder contraction and gastric emptying in humans. Implications for the physiology of CCK. Liddle, R.A., Gertz, B.J., Kanayama, S., Beccaria, L., Coker, L.D., Turnbull, T.A., Morita, E.T. J. Clin. Invest. (1989) [Pubmed]
  13. Cholecystokinin-B receptor ligands of the dipeptoid series act as agonists on rat stomach histidine decarboxylase. Ding, X.Q., Chen, D., Håkanson, R. Gastroenterology (1995) [Pubmed]
  14. Regulation of somatostatin-14 and -28 secretion by gastric acid in dogs: differential role of cholecystokinin. Greenberg, G.R., Fung, L., Pokol-Daniel, S. Gastroenterology (1993) [Pubmed]
  15. The effect of the cholecystokinin receptor antagonist MK-329 on meal-stimulated pancreaticobiliary output in humans. Cantor, P., Mortensen, P.E., Myhre, J., Gjorup, I., Worning, H., Stahl, E., Survill, T.T. Gastroenterology (1992) [Pubmed]
  16. Comparative involvement of 5-HT1, 5-HT2 and 5-HT3 receptors in stress-induced colonic motor alterations in rats. Gué, M., Alary, C., Rio-Lacheze, C.D., Junien, J.L., Buéno, L. Eur. J. Pharmacol. (1993) [Pubmed]
  17. Devazepide, a CCK(A) antagonist, attenuates the satiating but not the preference conditioning effects of intestinal carbohydrate infusions in rats. Pérez, C., Lucas, F., Sclafani, A. Pharmacol. Biochem. Behav. (1998) [Pubmed]
  18. Cholecystokinin satiety involves CCKA receptors perfused by the superior pancreaticoduodenal artery. Cox, J.E. Am. J. Physiol. (1998) [Pubmed]
  19. Synergistic interaction between leptin and cholecystokinin to reduce short-term food intake in lean mice. Barrachina, M.D., Martínez, V., Wang, L., Wei, J.Y., Taché, Y. Proc. Natl. Acad. Sci. U.S.A. (1997) [Pubmed]
  20. Autocrine growth stimulation of human renal Wilms' tumour G401 cells by a gastrin-like peptide. Blackmore, M., Doherty, E., Manning, J.E., Hirst, B.H. Int. J. Cancer (1994) [Pubmed]
  21. Selective CCK-A but not CCK-B receptor antagonists inhibit HT-29 cell proliferation: synergism with pharmacological levels of melatonin. González-Puga, C., García-Navarro, A., Escames, G., León, J., López-Cantarero, M., Ros, E., Acuña-Castroviejo, D. J. Pineal Res. (2005) [Pubmed]
  22. Pharmacological analysis of CCK2 receptor antagonists using isolated rat stomach ECL cells. Lindström, E., Björkqvist, M., Håkanson, R. Br. J. Pharmacol. (1999) [Pubmed]
  23. Roles for CCK1 and 5-HT3 receptors in the effects of CCK on presympathetic vasomotor neuronal discharge in the rat. Saita, M., Verberne, A.J. Br. J. Pharmacol. (2003) [Pubmed]
  24. MK-329 has no direct effect on the pancreas. Berlin, R.G. Gastroenterology (1989) [Pubmed]
  25. Cholecystokinin receptor antagonist MK-329 blocks intestinal fat-induced inhibition of meal-stimulated gastric acid secretion. Lloyd, K.C., Maxwell, V., Kovacs, T.O., Miller, J., Walsh, J.H. Gastroenterology (1992) [Pubmed]
  26. Distribution of cholecystokinin receptors in the bovine brain: a quantitative autoradiographic study. Morency, M.A., Quirion, R., Mishra, R.K. Neuroscience (1994) [Pubmed]
  27. Effect of cholecystokinin and secretin on somatostatin release from cultured antral cells. Buchan, A.M., Meloche, R.M., Kwok, Y.N., Kofod, H. Gastroenterology (1993) [Pubmed]
  28. Regulation of pancreatic endocrine function by cholecystokinin: studies with MK-329, a nonpeptide cholecystokinin receptor antagonist. Liddle, R.A., Gertz, B.J., Kanayama, S., Beccaria, L., Gettys, T.W., Taylor, I.L., Rushakoff, R.J., Williams, V.C., Coker, L.D. J. Clin. Endocrinol. Metab. (1990) [Pubmed]
  29. Studies of three non-peptide cholecystokinin antagonists (devazepide, lorglumide and loxiglumide) in human isolated alimentary muscle and guinea-pig ileum. D'Amato, M., Stamford, I.F., Bennett, A. Br. J. Pharmacol. (1991) [Pubmed]
  30. Vagal afferent responses to fatty acids of different chain length in the rat. Lal, S., Kirkup, A.J., Brunsden, A.M., Thompson, D.G., Grundy, D. Am. J. Physiol. Gastrointest. Liver Physiol. (2001) [Pubmed]
  31. Reversal of CRF- and dopamine-induced stimulation of colonic motility by CCK and igmesine (JO 1784) in the rat. Gué, M., Gleïzes-Escala, C., Del Rio-Lacheze, C., Junien, J.L., Buéno, L. Br. J. Pharmacol. (1994) [Pubmed]
  32. CCK antagonists and CCK-monoamine interactions in the control of satiety. Cooper, S.J., Dourish, C.T., Clifton, P.G. Am. J. Clin. Nutr. (1992) [Pubmed]
  33. Cholecystokinin type A and type B receptor antagonists produce opposing effects on cholecystokinin-stimulated beta-endorphin secretion from the rat pituitary. Millington, W.R., Mueller, G.P., Lavigne, G.J. J. Pharmacol. Exp. Ther. (1992) [Pubmed]
  34. Neuropeptide Y and sigma ligand (JO 1784) suppress stress-induced colonic motor disturbances in rats through sigma and cholecystokinin receptors. Gue, M., Junien, J.L., Del Rio, C., Bueno, L. J. Pharmacol. Exp. Ther. (1992) [Pubmed]
  35. Peripheral cholecystokinin type A receptors mediate oxytocin secretion in vivo. Miller, T.R., Bianchi, B.R., Witte, D.G., Lin, C.W. Regul. Pept. (1993) [Pubmed]
  36. Examining the role of cholecystokinin in appetitive learning in the infant rat. Weller, A., Tsitolovskya, L., Gispan, I.H., Rabinovitz, S. Peptides (2001) [Pubmed]
  37. The role of CCK caerulein, and CCK antagonists in nociception. Baber, N.S., Dourish, C.T., Hill, D.R. Pain (1989) [Pubmed]
  38. Sensitivity of vagal mucosal afferents to cholecystokinin and its role in afferent signal transduction in the rat. Richards, W., Hillsley, K., Eastwood, C., Grundy, D. J. Physiol. (Lond.) (1996) [Pubmed]
  39. Soybean beta-conglycinin peptone suppresses food intake and gastric emptying by increasing plasma cholecystokinin levels in rats. Nishi, T., Hara, H., Tomita, F. J. Nutr. (2003) [Pubmed]
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