A novel water-soluble selective CRF1 receptor antagonist, NBI 35965, blunts stress-induced visceral hyperalgesia and colonic motor function in rats

Brain Research

Volumn 985, Issue 1, 2003, Pages 32-42

  Million, Mulugeta ^a   Grigoriadis, Dimitri E ^b   Sullivan, Sue ^b   Crowe, Paul D ^b   McRoberts, James A ^a   Zhou, Huping ^a   Saunders, Paul R ^a   Maillot, Celine ^a   Mayer, Emeran A ^a   Taché, Yvette ^a  

^a UNIVERSITY OF CALIFORNIA   (United States)

^b NEUROCRINE BIOSCIENCES INC   (United States)

Author keywords

Colonic transit; Colorectal distention; CRF1 receptor; Non peptide receptor antagonist; Visceral pain

Indexed keywords

CARBACHOL; CORTICOTROPIN RELEASING FACTOR ANTAGONIST; CORTICOTROPIN RELEASING FACTOR DERIVATIVE; CORTICOTROPIN RELEASING FACTOR RECEPTOR; CORTICOTROPIN RELEASING FACTOR[12 DEXTRO PHENYLALANINE]; CYCLIC AMP; NBI 35965; RECEPTOR SUBTYPE; SAUVAGINE; UNCLASSIFIED DRUG; WATER;

ANIMAL BEHAVIOR; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; AUTORADIOGRAPHY; AVOIDANCE BEHAVIOR; BINDING AFFINITY; BINDING KINETICS; BRAIN CORTEX; COLON MOTILITY; CONTROLLED STUDY; DEFECATION; DOSE RESPONSE; DRUG MEGADOSE; DRUG RECEPTOR BINDING; DRUG SPECIFICITY; GENETIC TRANSFECTION; HYPERALGESIA; INTESTINE TRANSIT TIME; MALE; MATERNAL DEPRIVATION; NEWBORN; NONHUMAN; PRIORITY JOURNAL; RAT; RAT STRAIN; SOLUBILITY;

EID: 0142122206     PISSN: 00068993     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0006-8993(03)03027-0     Document Type: Article

References (53)

1. Behan D.P., Grigoriadis D.E., Lovenberg T., Chalmers D., Heinrichs S., Liaw C., De Souza E.B. Neurobiology of corticotropin releasing factor (CRF) receptors and CRF-binding protein: implications for the treatment of CNS disorders. Mol. Psychiatry. 1:1996;265-277.
2. Bonaz B., Taché Y. Water-avoidance stress-induced c-fos expression in the rat brain and stimulation of fecal output: role of corticotropin-releasing factor. Brain Res. 641:1994;21-28.
3. Castagliuolo I., Lamont J.T., Qiu B., Fleming S.M., Bhaskar K.R., Nikulasson S.T., Kornetsky C., Pothoulakis C. Acute stress causes mucin release from rat colon: role of corticotropin releasing factor and mast cells. Am. J. Physiol. 271:1996;G884-G892.
4. Chen C., Dagnino R. Jr., De Souza E.B., Grigoriadis D.E., Huang C.Q., Kim K.I., Liu Z., Moran T., Webb T.R., Whitten J.P., Xie Y.F., McCarthy J.R. Design and synthesis of a series of non-peptide high-affinity human corticotropin-releasing factor-1 receptor antagonists. J. Med. Chem. 39:1996;4358-4360.
5. Coutinho S.V., Plotsky P.M., Sablad M., Miller J.C., Zhou H., Bayati A.I., McRoberts J.A., Mayer E.A. Neonatal maternal separation alters stress-induced responses to viscerosomatic nociceptive stimuli in rat. Am. J. Physiol. Gastrointest. Liver Physiol. 282:2002;G307-G316.
6. Creed F. The relationship between psychosocial parameters and outcome in irritable bowel syndrome. Am. J. Med. 107:1999;74S-80S.
7. Fukudo S., Nomura T., Hongo M. Impact of corticotropin-releasing hormone on gastrointestinal motility and adrenocorticotropic hormone in normal controls and patients with irritable bowel syndrome. Gut. 42:1998;845-849.
8. Funada M., Hara C., Wada K. Involvement of corticotropin-releasing factor receptor subtype 1 in morphine withdrawal regulation of the brain noradrenergic system. Eur. J. Pharmacol. 430:2001;277-281.
9. K.E. Gabry, G.P. Chrousos, K.C. Rice, R.M. Mostafa, E. Sternberg, A.B. Negrao, E.L. Webster, S.M. McCann, P.W. Gold, Marked suppression of gastric ulcerogenesis and intestinal responses to stress by a novel class of drugs, Mol. Psychiatry 7 (2002) 474-483, 433.
10. Gilligan P.J., Robertson D.W., Zaczek R. Corticotropin releasing factor (CRF) receptor modulators: progress and opportunities for new therapeutic agents. J. Med. Chem. 43:2000;1641-1660.
11. Griebel G., Simiand J., Steinberg R., Jung M., Gully D., Roger P., Geslin M., Scatton B., Maffrand J.P., Soubrie P. 4-(2-Chloro-4-methoxy-5-methylphenyl)-N-[(1S) -2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl]5-methyl-N-(2-propynyl)-1, 3-thiazol-2-amine hydrochloride (SSR125543A), a potent and selective corticotrophin-releasing factor(1) receptor antagonist. II. Characterization in rodent models of stress-related disorders. J. Pharmacol. Exp. Ther. 301:2002;333-345.
12. Grigoriadis D.E., Lovenberg T.W., Chalmers D.T., Liaw C., De Souze E.B. Characterization of corticotropin-releasing factor receptor subtypes. Ann. NY Acad. Sci. 780:1996;60-80.
13. Gué M., Del Rio-Lacheze C., Eutamene H., Theodorou V., Fioramonti J., Bueno L. Stress-induced visceral hypersensitivity to rectal distension in rats: role of CRF and mast cells. Neurogastroenterol. Motil. 9:1997;271-279.
14. Gué M., Junien J.L., Buéno L. Conditioned emotional response in rats enhances colonic motility through the central release of corticotropin-releasing factor. Gastroenterology. 100:1991;964-970.
15. Habib K.E., Weld K.P., Rice K.C., Pushkas J., Champoux M., Listwak S., Webster E.L., Atkinson A.J., Schulkin J., Contoreggi C., Chrousos G.P., McCann S.M., Suomi S.J., Higley J.D., Gold P.W. Oral administration of a corticotropin-releasing hormone receptor antagonist significantly attenuates behavioral, neuroendocrine, and autonomic responses to stress in primates. Proc. Natl. Acad. Sci. USA. 97:2000;6079-6084.
16. Heinrichs S.C., De Souza E.B., Schulteis G., Lapsansky J.L., Grigoriadis D.E. Brain penetrance, receptor occupancy and antistress in vivo efficacy of a small molecule corticotropin releasing factor type I receptor selective antagonist. Neuropsychopharmacology. 27:2002;194-202.
17. Heinrichs S.C., Taché Y. Therapeutic potential of CRF receptor antagonists: a gut-brain perspective. Expert. Opin. Invest. Drugs. 10:2001;647-659.
18. Hoare S.R., Sullivan S.K., Ling N., Crowe P.D., Grigoriadis D.E. Mechanism of corticotropin-releasing factor type I receptor regulation by nonpeptide antagonists. Mol. Pharmacol. 63:2003;751-765.
19. Keck M.E., Welt T., Wigger A., Renner U., Engelmann M., Holsboer F., Landgraf R. The anxiolytic effect of the CRH(1) receptor antagonist R121919 depends on innate emotionality in rats. Eur. J. Neurosci. 13:2001;373-380.
20. Koob G.F., Heinrichs S.C. A role for corticotropin releasing factor and urocortin in behavioral responses to stressors. Brain Res. 848:1999;141-152.
21. Kresse A.E., Million M., Saperas E., Taché Y. Colitis induces CRF expression in hypothalamic magnocellular neurons and blunts CRF gene response to stress in rats. Am. J. Physiol. 281:2001;G1203-G1213.
22. Lechner S.M., Curtis A.L., Brons R., Valentino R.J. Locus coeruleus activation by colon distention: role of corticotropin-releasing factor and excitatory amino acids. Brain Res. 756:1997;114-124.
23. Lenz H.J., Burlage M., Raedler A., Greten H. Central nervous system effects of corticotropin-releasing factor on gastrointestinal transit in the rat. Gastroenterology. 94:1988;598-602.
24. Liaw C.W., Lovenberg T.W., Barry G., Oltersdorf T., Grigoriadis D.E., De S.E. Cloning and characterization of the human corticotropin-releasing factor-2 receptor complementary deoxyribonucleic acid. Endocrinology. 137:1996;72-77.
25. Lovenberg T.W., Liaw C.W., Grigoriadis D.E., Clevenger W., Chalmers D.T., De Souza E.B., Oltersdorf T. Cloning and characterization of a functionally distinct corticotropin-releasing factor receptor subtype from rat brain. Proc. Natl. Acad. Sci. USA. 92:1995;836-840.
26. Maciejewski-Lenoir D., Heinrichs S.C., Liu X.J., Ling N., Tucker A., Xie Q., Lappi D.A., Grigoriadis D.E. Selective impairment of corticotropin-releasing factor1 (CRF1) receptor-mediated function using CRF coupled to saporin. Endocrinology. 141:2000;498-504.
27. Maillot C., Million M., Wei J.Y., Gauthier A., Taché Y. Peripheral corticotropin-releasing factor and stress-stimulated colonic motor activity involve type 1 receptor in rats. Gastroenterology. 119:2000;1569-1579.
28. Martinez V., Taché Y. Role of CRF receptor 1 in central CRF-induced stimulation of colonic propulsion in rats. Brain Res. 893:2001;29-35.
29. Martinez V., Wang L., Rivier J.E., Vale W., Taché Y. Differential actions of peripheral corticotropin-releasing factor (CRF), urocortin II, and urocortin III on gastric emptying and colonic transit in mice: role of CRF receptor subtypes 1 and 2. J. Pharmacol. Exp. Ther. 301:2002;611-617.
30. Mayer E.A., Collins S.M. Evolving pathophysiologic models of functional gastrointestinal disorders. Gastroenterology. 122:2002;2032-2048.
31. Mayer E.A., Naliboff B.D., Chang L., Coutinho S.V. Stress and irritable bowel syndrome. Am. J. Physiol. Gastrointest. Liver Physiol. 280:2001;G519-G524.
32. 1 receptor in conscious rats. Am. J. Physiol. 282:2002;G857-G865.
33. 2-mediated action on gastric transit in rats. Am. J. Physiol. 282:2002;G34-G40.
34. Million M., Wang L., Martinez V., Taché Y. Differential Fos expression in the paraventricular nucleus of the hypothalamus, sacral parasympathetic nucleus and colonic motor response to water avoidance stress in Fischer and Lewis rats. Brain Res. 877:2000;345-353.
35. Mönnikes H., Schmidt B.G., Taché Y. Psychological stress-induced accelerated colonic transit in rats involves hypothalamic corticotropin-releasing factor. Gastroenterology. 104:1993;716-723.
36. Mönnikes H., Schmidt B.G., Tebbe J., Bauer C., Taché Y. Microinfusion of corticotropin releasing factor into the locus coeruleus/subcoeruleus nuclei stimulates colonic motor function in rats. Brain Res. 644:1994;101-108.
37. Ness T.J., Gebhart G.F. Colorectal distension as a noxious visceral stimulus: physiologic and pharmacologic characterization of pseudoaffective reflexes in the rat. Brain Res. 450:1988;153-169.
38. Okuyama S., Chaki S., Kawashima N., Suzuki Y., Ogawa S., Nakazato A., Kumagai T., Okubo T., Tomisawa K. Receptor binding, behavioral, and electrophysiological profiles of nonpeptide corticotropin-releasing factor subtype 1 receptor antagonists CRA1000 and CRA1001. J. Pharmacol. Exp. Ther. 289:1999;926-935.
39. Perrin M.H., Sutton S.W., Cervini L.A., Rivier J.E., Vale W.W. Comparison of an agonist, urocortin, and an antagonist, astressin, as radioligands for characterization of CRF receptors. J. Pharmacol. Exp. Ther. 288:1999;729-734.
40. Perrin M.H., Vale W.W. Corticotropin releasing factor receptors and their ligand family. Ann. NY Acad. Sci. 885:1999;312-328.
41. Plotsky P.M., Meaney M.J. Early, postnatal experience alters hypothalamic corticotropin-releasing factor (CRF) mRNA, median eminence CRF content and stress-induced release in adult rats. Brain Res. Mol. Brain Res. 18:1993;195-200.
42. 2 receptors: membrane homogenate and autoradiographic studies. J. Pharmacol. Exp. Ther. 286:1998;459-468.
43. 1 receptor in fecal watery excretion. Eur. J. Pharmacol. 435:2002;231-235.
44. Schulz D.W., Mansbach R.S., Sprouse J., Braselton J.P., Collins J., Corman M., Dunaiskis A., Faraci S., Schmidt A.W., Seeger T., Seymour P., Tingley III F.D., Winston E.N., Chen Y.L., Heym J. CP-154,526: a potent and selective nonpeptide antagonist of corticotropin releasing factor receptors. Proc. Natl. Acad. Sci. USA. 93:1996;10477-10482.
45. Smith G.W., Aubry J.M., Dellu F., Contarino A., Bilezikjian L.M., Gold L.H., Chen R., Marchuk Y., Hauser C., Bentley C.A., Sawchenko P.E., Koob G.F., Vale W., Lee K.F. Corticotropin releasing factor receptor 1-deficient mice display decreased anxiety, impaired stress response, and aberrant neuroendocrine development. Neuron. 20:1998;1093-1102.
46. Taché Y., Martinez V., Million M., Maillot C. Role of corticotropin releasing factor receptor subtype 1 in stress-related functional colonic alterations: implications in irritable bowel syndrome. Eur. J. Surg. 168:(Suppl. 587):2002;16-22.
47. Taché Y., Martinez V., Million M., Wang L. Stress and the gastrointestinal tract III. Stress-related alterations of gut motor function: role of brain corticotropin-releasing factor receptors. Am. J. Physiol. 280:2001;G173-G177.
48. Timpl P., Spanagel R., Sillaber I., Kresse A., Reul J.M., Stalla G.K., Blanquet V., Steckler T., Holsboer F., Wurst W. Impaired stress response and reduced anxiety in mice lacking a functional corticotropin-releasing hormone receptor. Nat. Genet. 19:1998;162-166.
49. Turnbull A.V., Rivier C. Corticotropin-releasing factor (CRF) and endocrine response to stress: CRF receptors, binding protein, and related peptides. Proc. Soc. Exp. Biol. Med. 215:1997;1-10.
50. Valentino R.J., Miselis R.R., Pavcovich L.A. Pontine regulation of pelvic viscera: pharmacological target for pelvic visceral dysfunctions. Trends Pharmacol. Sci. 20:1999;253-260.
51. Van Pett K., Viau V., Bittencourt J.C., Chan R.K., Li H.Y., Arias C., Prins G.S., Perrin M., Vale W., Sawchenko P.E. Distribution of mRNAs encoding CRF receptors in brain and pituitary of rat and mouse. J. Comp. Neurol. 428:2000;191-212.
52. Wang L., Martinez V., Rivier J.E., Taché Y. Peripheral urocortin inhibits gastric emptying and food intake in mice: differential role of CRF receptor 2. Am. J. Physiol. Regul. Integr. Comp. Physiol. 281:2001;R1401-R1410.
53. Zobel A.W., Nickel T., Kunzel H.E., Ackl N., Sonntag A., Ising M., Holsboer F. Effects of the high-affinity corticotropin-releasing hormone receptor 1 antagonist R121919 in major depression: the first 20 patients treated. J. Psychiatr. Res. 34:2000;171-181.