Corticotropin-Releasing Factor: Physiology, Pharmacology and Role in Central Nervous System and Immune Disorders

Errol B. De Souza and Dimitri E. Grigoriadis
Neurocrine Biosciences, Inc.
3050 Science Park Rd.
San Diego, CA 92121

Tel: (619)-685-7660
Fax: (619)-658-7601


REFERENCES

1. Abou-Samra A-B, Harwood JP, Catt KJ, Aguilera G. Mechanisms of action of CRF and other regulators of ACTH release in pituitary corticotrophs. Ann N Y Acad Sci 1987;67-84.

2. Aguilera G, Millan MA, Hauger RL, Catt KJ. Corticotropin-releasing factor receptors: Distribution in brain, pituitary and peripheral tissues. Ann N Y Acad Sci 1987;48-66.

3. Aldrich PE, Arvanitis AG, Cheeseman RS, et al. 1N-Alkyl-N-arylpyrimidinamines and derivatives thereof. World Patent Application: WO 95/10506, April 20, 1995.

4. Anderson SM, Kant GJ, De Souza EB. Effects of chronic stress on anterior pituitary and brain corticotropin-releasing factor receptors. Pharmacol Biochem Behav 1993;44:755-761.

5. Battaglia G, Webster EL, De Souza EB. Characterization of corticotropin-releasing factor receptor-mediated adenylate cyclase activity in the rat central nervous system. Synapse 1987;1:572-581.

6. Behan DP, Heinrichs SC, Troncoso JC, et al. Displacement of corticotropin releasing factor from its binding protein as a treatment for Alzheimer's disease. Nature 1995;378:284-287.

7. Behan DP, Linton EA, Lowry PJ. Isolation of the human plasma corticotrophin-releasing factor-binding protein. J Endocrinol 1989;122:23-31.

8. Bissette G, Reynolds GP, Kilts CD, Widerlov W, Nemeroff CB. Corticotropin-releasing factor-like immunoreactivity in senile dementia of the Alzheimer type. JAMA 1985;254:3067-3069.

9. Blalock JE. A molecular basis for bidirectional communication between the immune and neuroendocrine systems. Physiol Rev 1989;69:1-32.

10. Bright GM. Amino-substituted pyrazoles having CRF antagonist activity. World Patent Application: WO 94/13644, June 23, 1994.

11. Bright GM, Welch WMJ. Substituted pyrazoles as CRF antagonists. World Patent Application: WO 94/13661, June 23, 1994.

12. Brown MR, Fisher LA. Regulation of the autonomic nervous system by corticotropin-releasing factor. In: De Souza EB, Nemeroff CB, eds. Corticotropin-releasing factor: Basic and clinical studies of a neuropeptide. Boca Raton, FL: CRC Press, Inc., 1990;291-298.

13. Calogero AE, Sternberg EM, Bagdy G, et al. Neurotransmitter-induced hypothalamic-pituitary-adrenal axis responsiveness in inflammatory disease-susceptible Lewis rats: In vivo and in vitro studies suggesting a global defect in CRH secretion. Neuroendocrinology 1992;55:600-608.

14. Chadwick DJ, Marsh J, Ackrill K, eds. Corticotropin-releasing factor. Chichester, West Sussex, England: John Wiley & Sons Ltd., 1993.

15. Chalmers DT, Lovenberg TW, De Souza EB. Localization of novel corticotropin-releasing factor receptor (CRF2) mRNA to specific sub-cortical nuclei in rat brain: Comparison with CRF1 receptor mRNA expression. J Neurosci 1995;15:6340-6350.

16. Chang CP, Pearse RI, O'Connell S, Rosenfeld MG. Identification of a seven transmembrane helix receptor for corticotropin-releasing factor and sauvagine in mammalian brain. Neuron 1993;11:1187-1195.

17. Chen C, Dagnino Jr. R, De Souza EB, et al. Design and synthesis of a series of non-peptide high-affinity human corticotropin-releasing factor1 (CRF1) receptor antagonists. J Med Chem 1996;39:4358-4360.

18. Chen R, Lewis KA, Perrin MH, Vale WW. Expression cloning of a human corticotropin-releasing-factor receptor. Proc Natl Acad Sci USA 1993;90:8967-8971.

19. Chen YL. Pyrazolopyrimidines as CRF antagonists. World Patent Application: WO 94/13677, June 23, 1994.

20. Chen YL. Pyrrolopyrimidines as CRF antagonists. World Patent Application: WO 94/13676, June 23, 1994.

21. Chen YL. Corticotropin releasing factor antagonists. World Patent Application: WO 95/33750, December 14, 1995, 1995.

22. Chikanza IC, Petrou P, Chrousos G, Kingsley G, Panayi GS. Excessive and dysregulated secretion of prolactin in rheumatoid arthritis: immunopathogenetic and therapeutic implications. Br J Rheumatol 1993;32:445-448..

23. Conte-Devolx B, Grino M, Nieoullon A, et al. Corticoliberin, somatocrinin and amine contents in normal and parkinsonian human hypothalamus. Neurosci Lett 1985;56:217-222.

24. Courtemanche G, Gautier C, Gully D, Roger P, Valette G, Wermuth CG. Dérivés alkylamino ramifiés du thiazole, leurs procédés de préparation et les compositions pharmaceutiques qui les contiennent. European Patent Application: EP 0 576 350 A1, December 29, 1993.

25. Crofford LJ, Sano H, Karalis K, et al. Corticotropin-releasing hormone in synovial fluids and tissues of patients with rheumatoid arthritis and osteoarthritis. J Immunology 1993;151:1587-1596.

26. Crofford LJ, Sano H, Karalis K, et al. Local secretion of corticotropin-releasing hormone in the joints of Lewis rats with inflammatory arthritis. J Clin Invest 1992;90:2555-2564.

27. De France JF. The septal nuclei. New York: Plenum, 1976.

28. De Souza EB. Corticotropin-releasing factor receptors in the rat central nervous system: Characterization and regional distribution. J Neurosci 1987;7:88-100.

29. De Souza EB. CRH defects in Alzheimer's and other neurologic diseases. Hosp Practice 1988;23:59-71.

30. De Souza EB. Role of corticotropin-releasing factor in neuropsychiatric disorders and neurodegenerative diseases. In: Seamon KB, ed. Annual reports in medicinal chemistry. San Diego: Academic Press, Inc., 1990;215-224.

31. De Souza EB. Corticotropin-releasing hormone receptors. In: Bjorklund A, Hokfelt T, Kuhar MJ, eds. Handbook of chemical neuroanatomy—Neuropeptide receptors in the CNS, Part III. Amsterdam: Elsevier, 1992;145-185.

32. De Souza EB, Nemeroff CB, eds. Corticotropin-releasing factor: Basic and clinical studies of a neuropeptide. Boca Raton, Florida: CRC Press, Inc., 1990.

33. De Souza EB, Whitehouse PJ, Kuhar MJ, Price DL, Vale WW. Reciprocal changes in corticotropin-releasing factor (CRF)-like immunoreactivity and CRF receptors in cerebral cortex of Alzheimer's disease. Nature 1986;319:593-595.

34. De Souza EB, Whitehouse PJ, Price DL, Vale WW. Abnormalities in corticotropin-releasing hormone (CRH) in Alzheimer's disease and other human disorders. Ann NY Acad Sci 1987;512:237-247.

35. Donaldson CJ, Sutton SW, Perrin MH, et al. Cloning and characterization of human urocortin. Endocrinology 1996;137:2167-2170.

36. Dunn AJ, Berridge CW. Physiological and behavioral responses to corticotropin-releasing factor administration: is CRF a mediator of anxiety of stress responses? Brain Res Brain Res Rev 1990;15:71-100.

37. Ehlers CL. CRF effects on EEG activity: implications for the modulation of normal and abnormal brain states. In: De Souza EB, Nemeroff CB, eds. Corticotropin-releasing factor: Basic and clinical studies of a neuropeptide. Boca Raton, FL: CRC Press, Inc., 1990;233-252.

38. Faraci WS, Welch WM. Pyrazoles and pyrazolopyrimidines having CRF antagonist activity. WO 94/13643, June 23, 1994.

39. Fisher LA. Corticotropin-releasing factor: endocrine and autonomic integration of responses to stress. Trends Pharmacol Sci 1989;10:189-193.

40. Gold PW, Loriaux DL, Roy A, et al. Responses to corticotropin-releasing hormone in the hypercortisolism of depression and Cushing's disease. N Engl J Med 1986;314:1329-1334.

41. Grigoriadis DE, De Souza EB. Heterogeneity between brain and pituitary corticotropin-releasing factor receptors is due to differential glycosylation. Endocrinology 1989;125:1877-1888.

42. Grigoriadis DE, Heroux JA, De Souza EB. Characterization and regulation of corticotropin-releasing factor receptors in the central nervous, endocrine and immune systems. In: Chadwick DJ, Marsh J, Ackrill K, eds. Corticotropin-releasing factor. Chichester, West Sussex: John Wiley and Sons Ltd., 1993;85-101.

43. Grigoriadis DE, Liu XJ, Vaughn J, et al. 125I-Tyr0-Sauvagine: A novel high affinity radioligand for the pharmacological and biochemical study of human corticotropin-releasing factor2a receptors. Mol Pharmacol 1996;50:679-686.

44. Grigoriadis DE, Struble RG, Price DL, De Souza EB. Normal pattern of labeling of cerebral cortical corticotropin-releasing factor (CRF) receptors in Alzheimer's disease: Evidence from chemical cross-linking studies. Neuropharmacology 1989;28:761-764.

45. Heisler S, Hook VYH, Axelrod J. Corticotropin-releasing factor stimulation of protein carboxylmethylation in mouse pituitary tumor cells. Biochem Pharmacol 1983;32:1295-1299.

46. Heroux JA, Grigoriadis DE, De Souza EB. Age-related decreases in corticotropin-releasing factor (CRF) receptors in rat brain and anterior pituitary gland. Brain Res 1991;542:155-158.

47. Karalis K, Sano H, Redwine J, Listwak S, Wilder RL, Chrousos GP. Autocrine or paracrine inflammatory actions of corticotropin-releasing hormone in vivo. Science 1991;254:421-423.

48. Kishimoto T, Pearse II RV, Lin CR, Rosenfeld MG. A sauvagine/corticotropin-releasing factor receptor expressed in heart and skeletal muscle. Proc Natl Acad Sci USA 1995;92:1108-1112.

49. Koob GF, Britton KT. Behavioral effects of corticotropin-releasing factor. In: De Souza EB, Nemeroff CB eds. Corticotropin-releasing factor: Basic and clinical studies of a neuropeptide. Boca Raton, FL: CRC Press Inc., 1990; 253-265.

50. Kostich W, Chen A, Sperle K, Horlick RA, Patterson J, Largent BL. Molecular cloning and expression analysis of human CRH receptor type 2 a and b isoforms. Soc Neurosci Abstr 1996;22:1545.

51. Laatikainen T, Virtanen T, Raisanen I, Salminen K. Immunoreactive corticotropin-releasing factor and corticotropin in plasma during pregnancy, labour and puerperium. Neuropeptides 1987;10:343-353.

52. Letter A, McMaster B, Moore G, Schlefinger D. Complete amino acid sequence of urotensin I, a hypotensive and corticotropin releasing neuropeptide from Catostomus. Science 1982;218:162-164.

53. Liaw C, Grigoriadis DE, De Souza EB, Oltersdorf T. Colorimetric assay for rapid screening of corticotropin-releasing factor receptor ligands. J Mol Neurosci 1994;5:83-92.

54. Liaw CW, Lovenberg TW, Barry G, Oltersdorf T, Grigoriadis DE, De Souza EB. Cloning and characterization of the human CRF2 receptor gene and cDNA. Endocrinology 1996;137:72-77.

55. Linton EA, Wolfe CDA, Behan DP, Lowry PJ. A specific carrier substance for human corticotropin-releasing factor in late gestational maternal plasma which could mask the ACTH-releasing activity. Clin Endocrinol 1988;28:315-324.

56. Lovenberg TW, Chalmers DT, Liu C, De Souza EB. CRF2a and CRF2b receptor mRNAs are differentially distributed between the rat central nervous system and peripheral tissues. Endocrinology 1995;136:4139-4142.

57. Lovenberg TW, Liaw CW, Grigoriadis DE, et al. Cloning and characterization of a functionally distinct corticotropin-releasing factor receptor subtype from rat brain. Proc Natl Acad Sci USA 1995;92:836-840.

58. Majzoub JA, Emanuel R, Adler G, Martinez C, Robinson B, Wittert G. Second messenger regulation of mRNA for corticotropin-releasing factor. In: Chadwick DJ, Marsh J, Ackrill K, eds. Corticotropin releasing factor. Chichester, West Sussex, England: John Wiley & Sons Ltd., 1993;30-43.

59. May C, Rapoport SI, Tomai TP, Chrousos GP, Gold PW. Cerebral spinal fluid concentrations of corticotropin-releasing hormone (CRH) and corticotropin (ACTH) are reduced in Alzheimer's disease. Neurology 1987;37:535-538.

60. Montecucchi PC, Henschen A. Amino acid composition and sequence analysis of sauvagine, a new active peptide from the skin of Phyllomedusa sauvagei. Int J Pept Protein Res 1981;18:113-120.

61. Mouradian MM, Farah JM, Jr., Mohr E, Fabbrini G, O'Donohue TL, Chase TN. Spinal fluid CRF reduction in Alzheimer's disease. Neuropeptides 1986;8:393-400.

62. Nemeroff CB, Bissette G, Akil H, Fink M. Neuropeptide concentrations in the cerebrospinal fluid of depressed patients treated with electroconvulsive therapy: corticotropin-releasing factor, b-endorphin and somatostatin. Br J Psychiatry 1991;158:59-63.

63. Nemeroff CB, Owens MJ, Bissett G, Andorn AC, Stanley M. Reduced corticotropin-releasing factor receptor binding sites in the frontal cortex of suicide victims. Arch Gen Psychiatry 1988;45:577-579.

64. Nemeroff CB, Widerlov E, Bissett G, et al. Elevated concentration of CSF corticotropin-releasing factor-like immunoreactivity in depressed patients. Science 1984;226:1342-1344.

65. Okawara Y, Morley SD, Burzio LO, Zwiers H, Lederis K, Richter D. Cloning and sequence analysis of cDNA for corticotropin-releasing factor precursor from the teleost fish Catostomus commersoni. Proc Natl Acad Sci USA 1988;85:8439-43.

66. Owens MJ, Nemeroff CB. Preclinical and clinical studies with corticotropin-releasing factor: implications for affective disorders. Psychopharmacol Bull 1988;24:335-339.

67. Owens MJ, Nemeroff CB. Neurotransmitter regulation of the CRF secretion in vitro. In: De Souza EB, Nemeroff CB, eds. Corticotropin-releasing factor: Basic and clinical studies of a neuropeptide. Boca Raton, FL: CRC Press, Inc., 1990;107-114.

68. Owens MJ, Nemeroff CB. Physiology and pharmacology of corticotropin-releasing factor. Pharmacol Rev 1991;43:425-473.

69. Perrin M, Donaldson C, Chen R, et al. Identification of a second corticotropin-releasing factor receptor gene and characterization of a cDNA expressed in heart. Proc Natl Acad Sci USA 1995;92:2969-2973.

70. Petrusz P, Merchenthaler I. The corticotropin-releasing factor system. In: Nemeroff CB, eds. Neuroendocrinology. Boca Raton, FL: CRC Press, Inc., 1992;129-184.

71. Plotsky PM, Cunningham ETJ, Widmaier EP. Catecholaminergic modulation of corticotropin-releasing factor and adrenocorticotropin secretion. Endocrinol Rev 1989;10:437-458.

72. Pomara N, Singh RR, Deptula D, et al. CSF corticotropin-releasing factor (CRF) in Alzheimer's disease: Its relationship to severity of dementia and monoamine metabolites. Biol Psychiatry 1989;26:500-504.

73. Potter E, Behan DP, Fischer WH, Linton EA, Lowry PJ, Vale WW. Cloning and characterization of the cDNAs for human and rat corticotropin-releasing factor-binding proteins. Nature 1991;349:423-426.

74. Potter E, Behan DP, Linton EA, Lowry PJ, Sawchenko PE, Vale WW. The central distribution of a corticotropin-releasing factor (CRF)-binding protein predicts multiple sites and modes of interaction with CRF. Proc Natl Acad Sci USA 1992;89:4192-4196.

75. Powers RE, Walker LC, De Souza EB, et al. Immunohistochemical study of neurons containing corticotropin-releasing factor in Alzheimer's disease. Synapse 1987;1:405-410.

76. Rivier J, Rivier C, Vale W. Synthetic competitive antagonist of corticotropin-releasing factor: effect on ACTH secretion in the rat. Science 1984;224:889-891.

77. Romier C, Bernassau J-M, Cambillau C, Darbon H. Solution structure of human corticotropin releasing factor by 1H NMR and distance geometry with restrained molecular dynamics. Protein Eng 1993;6:149-156.

78. Roy A, Pickar D, Paul S, Doran A, Chrousos GP, Gold PW. CSF corticotropin-releasing hormone in depressed patients and normal control subjects. Am J Psychiatry 1987;143:896-899.

79. Roy-Byrne PP, Uhde T, Post R, Gallucci W, Chrousos GP, Gold PW. The corticotropin-releasing hormone stimulation test in patients with panic disorder. Am J Psychiatry 1986;143:896-899.

80. Sawchenko PE, Swanson LW. Organization of CRF immunoreactive cells and fibers in the rat brain: immunohistochemical studies. In: De Souza EB, Nemeroff CB, eds. Corticotropin-releasing factor: Basic and clinical studies of a neuropeptide. Boca Raton, FL: CRC Press, Inc., 1990;29-52.

81. Shibasaki T, Odagiri E, Shizume K, Ling N. Corticotropin-releasing factor like activity in human placental extract. J Clin Endocrinol Metab 1982;55:384-386.

82. Siggins GR. Electrophysiology of corticotropin-releasing factor in nervous tissue. In: De Souza EB, Nemeroff CB, eds. Corticotropin-releasing factor: Basic and clinical studies of a neuropeptide. Boca Raton, FL: CRC Press, Inc., 1990;205-216.

83. Stenzel-Poore MP, Heldwein KA, Stenzel P, Lee S, Vale WW. Characterization of the genomic corticotropin-releasing factor (CRF) gene from Xenopus laevis: two members of the CRF family exist in amphibians. Mol Endocrinol 1992;6:1716-24.

84. Sternberg EM, Young WS, III, Bernardini R, et al. A central nervous system defect in biosynthesis of corticotropin-releasing hormone is associated with susceptibility to streptococcal cell wall-induced arthritis in Lewis rats. Proc Natl Acad Sci USA 1989;86:4771-4775.

85. Suda T, Iwashita M, Tozawa F, et al. Characterization of CRH binding protein in human plasma by chemical cross-linking and its binding during pregnancy. J Clin Endocrinol Metab 1988;67:1278-1283.

86. Suda T, Sumitomo T, Tozawa F, Ushiyama T, Demura H. Corticotropin-releasing factor-binding protein is a glycoprotein. Biochem Biophys Res Comm 1989;165:703-707.

87. Swanson LW, Sawchenko PE, Rivier J, Vale WW. The organization of ovine corticotropin-releasing factor immunoreactive cells and fibers in the rat brain: An immunohistochemical study. Neuroendocrinology 1983;36:165-186.

88. Tache Y, Gunion MM, Stephens R. CRF: Central nervous system action to influence gastrointestinal function and role in the gastrointestinal response to stress. In: De Souza EB, Nemeroff CB, eds. Corticotropin-releasing factor: Basic and clinical studies of a neuropeptide. Boca Raton, FL: CRC Press, Inc., 1990;299-308.

89. Thompson RC, Seasholtz AF, Douglass JO, Herbert E. Cloning and distribution of expression of the rat corticotropin-releasing factor (CRF) gene. In: De Souza EB, Nemeroff CB, eds. Corticotropin releasing factor: Basic and clinical studies of a neuropeptide. Boca Raton, FL: CRC Press, Inc., 1990;1-12.

90. Vale W, Rivier C, Brown MR, et al. Chemical and biological characterization of corticotropin-releasing factor. Recent Prog Horm Res 1983;39:245-270.

91. Vale W, Spiess J, Rivier C, Rivier J. Characterization of a 41-residue ovine hypothalamic peptide that stimulates secretion of corticotropin and b-endorphin. Science 1981;213:1394-1397.

92. Valentino RJ. Effects of CRF on spontaneous and sensory-evoked activity of locus coeruleus neurons. In: De Souza EB, Nemeroff CB, eds. Corticotropin-releasing factor: Basic and clinical studies of a neuropeptide. Boca Raton, FL: CRC Press, Inc., 1990;217-232.

93. Vaughan J, Donaldson C, Bittencourt J, et al. Characterization of a novel neuropeptide in rat brain related to CRF. 25th Annual Meeting of the Society for Neuroscience, San Diego, 1995.

94. Vaughan J, Donaldson C, Bittencourt J, et al. Urocortin, a mammalian neuropeptide related to fish urotensin I and to corticotropin-releasing factor. Nature 1995;378:287-291.

95. Vita N, Laurent P, Lefort S, et al. Primary structure and functional expression of mouse pituitary and human brain corticotrophin releasing factor receptors. FEBS Lett 1993;335:1-5.

96. Webster EL, Grigoriadis DE, De Souza EB. Corticotropin-releasing factor receptors in the brain-pituitary-immune axis. In: McCubbin JA, Kaufmann PG, Nemeroff CB, eds. Stress, neuropeptides, and systemic disease. San Diego: Academic Press, 1991;233-260.

97. Whitehouse PJ, Vale WW, Zweig RM, et al. Reduction in corticotropin-releasing factor-like immunoreactivity in cerebral cortex in Alzheimer's disease, Parkinson’s disease, and progressive supranuclear palsy. Neurology 1987;37:905-909.

98. Whitten JP, Xie YF, Erickson PE, et al. Rapid microscale synthesis, a new method for lead optimization using robotics and solution phase chemistry: Application to the synthesis and optimization of corticotropin-releasing factor (CRF) receptor antagonists. J Med Chem 1996;39:4354-4357.

Back to Chapter

published 2000