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Part of the book series: Endocrine Updates ((ENDO,volume 21))

Abstract

It has long been postulated that the pituitary gland plays a central role in mediating the stress response (11). Later, it was hypothesized that higher brain centers are involved in the regulation of pituitary ACTH release and that the pituitary gland is under control of hypothalamic factors which would reach the adenohypophysis via hypothalamic-hypophyseal blood vessels (2). Further evidence for the existence of this hypothetical hypothalamic corticotropin releasing factor (CRF) was provided by demonstrating that hypothalamic organ extracts stimulated pituitary ACTH release (3 4).

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References

  1. Selye H 1937 Studies on adaptation. Endocrinology 21:169–188

    Article  Google Scholar 

  2. Harris GW 1948 Neural control of the pituitary gland. Phys Rev 28:139–179

    CAS  Google Scholar 

  3. Saffran M, Schally AV, Benfey BG 1955 Stimulation of the release of corticotrophin from the adenohypophysis by a neurohypophysial factor. Endocrinology 57:439–444

    Article  PubMed  CAS  Google Scholar 

  4. Guillemin R, Rosenberg B 1955 Humoral hypothalamic control of anterior pituitary: a study with combined tissue cultures. Endocrinology 57:599–607

    Article  PubMed  CAS  Google Scholar 

  5. Vale W, Spiess J, Rivier C, Rivier J 1981 Characterization of a 41-residue ovine hypothalamic peptide that stimulates secretion of corticotropin and 0-endorphin. Science 213:1394–1397

    Article  PubMed  CAS  Google Scholar 

  6. Shibahara S, Morimoto Y, Furutani Y, Notake M, Takahashi H, Shimizu S, Horikawa S, Numa S 1983 Isolation and sequence analysis of human corticotropinreleasing factor precursor gene. EMBO J 5:775–779

    Google Scholar 

  7. Rivier J, Spiess J, Vale W 1983 Chemical and biological characterization of rat hypothalamic corticotropin-releasing factor. Proc Natl Acad Sci USA 80:4851–4855

    Article  PubMed  CAS  Google Scholar 

  8. Lederis K, Letter A, McMaster D, Moore G, Schlesinger D 1982 Complete amino acid sequence of urotensin I, a hypotensive and corticotropin-releasing neuropeptide from Catostomus. Science 218:162–165

    Article  PubMed  CAS  Google Scholar 

  9. Montecucchi PC, Anastasi A, De Castiglione R, Erspamer V 1980 Isolation and amino acid composition of sauvagine. An active polypeptide from methanol extracts of the skin of the South American frog Phyllomedusa sauvagei. Int J Pept Protein Res 18:113–120

    Article  Google Scholar 

  10. Vaughan J, Donaldson C, Bittencourt J, Perrin MH, Lewis K, Sutton S, Chan R, Turnbull AV, Lovejoy D, Rivier C, Rivier J, Sawchenko PE, Vale W 1995 Urocortin, a mammalian neuropeptide related to fish urotensin I and to corticotropin releasing factor. Nature 378:287–292

    Article  PubMed  CAS  Google Scholar 

  11. Reyes TM, Lewis K, Perrin MH, Kunitake KS, Vaughan J, Arias CA, Hogenesch JB, Gulyas J, Rivier J, VaIe WW, Sawchenko PE 2001 Urocortin II: a member of the corticotropin-releasing factor (CRF) neuropeptide family that is selectively bound by type 2 CRF receptors. Proc Natl Acad Sci USA 98:2843–2848

    Article  PubMed  CAS  Google Scholar 

  12. Lewis K, Li C, Perrin MH, Blount A, Kunitake K, Donaldson C, Vaughan J, Reyes TM, Gulyas J, Fischer W, Bilezikjian L, Rivier J, Sawchenko PE, Vale WW 2001 Identification of urocortin III, an additional member of the corticotropin-releasing factor (CRF) family with high affinity for the CRF2 receptor. Proc Natl Acad Sci USA 98:7570–7575

    Article  PubMed  CAS  Google Scholar 

  13. Hsu SY, Hsueh AJW 2001 Human stresscopin and stresscopin-related peptide are selective ligands for the type 2 corticotropin-releasing hormone receptor. Nat Med 7:605–611

    Article  PubMed  CAS  Google Scholar 

  14. Orth DN, Jackson RV, DeCherney S, DeBold CR, Alexander AN, Island DP, Rivier J, Rivier C, Spiess J, Vale W 1983 Effect of synthetic ovine corticotropin-releasing factor. Dose response of plasma adrenocorticotropin and cortisol. J Clin Invest 71:587–595

    Article  PubMed  CAS  Google Scholar 

  15. Asaba K, Makino S, Hashimoto K 1998 Effect of urocortin on ACTH secretion from rat anterior pituitary in vitro and in vivo: comparison with corticotropin-releasing hormone. Brain Res 806:95–103

    Article  PubMed  CAS  Google Scholar 

  16. Chrousos GP, Luger A, Avgerinos PC, Kling MA, Oldfield EH, Nieman LK, Schiirmeyer T, Loriaux DL, Gold PW 1987 Corticotropin releasing hormone: relevance to human physiology and pathophysiology. In: D’Agata R, Chrousos GP, eds. Recent advances in adrenal regulation and function. New York: Raven Press; 121–135

    Google Scholar 

  17. Skelton KH, Owens MJ, Nemeroff CB 2000 The neurobiology of urocortin. Regulatory Peptides 93:85–92

    Article  PubMed  CAS  Google Scholar 

  18. Brown MR, Fisher LA, Spiess J, Rivier C, Rivier J, Vale W 1982 Corticotropinreleasing factor: actions on the autonomic nervous system and metabolism. Endocrinology 111:928–931

    Article  PubMed  CAS  Google Scholar 

  19. Britton DR, Koob GF, Rivier J, Vale W 1982 Intraventricular corticotropin-releasing factor enhances behavioral effects of novelty. Life Sci 31:363–367

    Article  PubMed  CAS  Google Scholar 

  20. Gold PW, Loriaux DL, Roy A, Kling MA, Calabrese JR, Kellner CH, Nieman LK, Post RM, Pickar D, Galluci WT, et al. 1986 Responses to corticotropin-releasing hormone in the hypercortisolism of depression and Cushing’s disease. Pathophysiologic and diagnostic implications. N Engl J Med 314:1329–1335

    Article  PubMed  CAS  Google Scholar 

  21. Gold PW, Gwirtsman H, Avgerinos PC, Nieman LK, Gallucci WT, Kaye W, Jimerson D, Ebert M, Rittmaster R, Loriaux DL et al. 1986 Abnormal hypothalamicpituitary-adrenal function in anorexia nervosa. Pathophysiologic mechanisms in underweight and weight corrected patients. N Engl J Med 314:1335–1342

    Article  PubMed  CAS  Google Scholar 

  22. Arborelius L, Owens MJ, Plotsky PM, Nemeroff CB 1999 The role of corticotropinreleasing factor in depression and anxiety disorders. J Endocrinol 160:1–12

    Article  PubMed  CAS  Google Scholar 

  23. Luger A, Deuster PA, Kyle SB, Gallucci WT, Montgomery LC, Gold PW, Loriaux DL, Chrousos GP 1987 Acute hypothalamic-pituitary-adrenal responses to the stress of treadmill exercise. Physiologic adaptations to physical training. N Engl J Med 316:1309–1315

    Article  PubMed  CAS  Google Scholar 

  24. Nemeroff CB, Bissette G, Akil H, Fink M 1991 Neuropeptide concentrations in the cerebrospinal fluid of depressed patients treated with electroconvulsive therapy: corticotropin-releasing factor, 13-endorphin and somatostatin. Brit J Psych 158:59–63

    Article  CAS  Google Scholar 

  25. Arato M, Banki CM, Bissette G, Nemeroff CB 1989 Elevated CSF CRF in suicide victims. Biol Psychiatry 25:355–359

    Article  PubMed  CAS  Google Scholar 

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

    Article  PubMed  CAS  Google Scholar 

  27. Baigent SM 2001 Peripheral corticotropin-releasing hormone and urocortin in the control of the immune response. Peptides 22:809–820

    Article  PubMed  CAS  Google Scholar 

  28. Gisslinger H, Svoboda T, Clodi M, Gilly B, Ludwig H, Havelec L, Luger A 1993 Interferon-a stimulates the hypothalamic-pituitary-adrenal axis in vivo and in vitro. Neuroendocrinol 57:489–495

    Article  CAS  Google Scholar 

  29. Gaillard RC 1998 Cytokines in the neuroendocrine system. Int Rev Immunol 17:181–216

    Article  PubMed  CAS  Google Scholar 

  30. Benoit SC, Thiele TE, Heinrichs SC, Rushing PA, Blake KA, Steeley RJ 2000 Comparison of central administration of corticotropin-releasing hormone and urocortin on food intake, conditioned taste aversion, and c-Fos expression. Peptides 21:345–351

    Article  PubMed  CAS  Google Scholar 

  31. Wang L, Martinez V, Rivier JE, Tache Y 2001 Peripheral urocortin inhibits gastric emptying and food intake in mice: differential role of CRF receptor 2. Am J Physiol regulatory Integrative Comp Physiol 281:R1401–R1410

    CAS  Google Scholar 

  32. Maillot C, Million M, Wei JY, Gauthier A, Tache Y 2000 Peripheral Corticotropinreleasing factor and stress-stimulated colonic motor activity involve type 1 receptor in rats. Gastroenterology 119:1569–1579

    Article  PubMed  CAS  Google Scholar 

  33. Parkes DG, Weisinger RS, May CN 2001 Cardiovascular actions of CRH and urocortin: an update. Peptides 22:821–827

    Article  PubMed  CAS  Google Scholar 

  34. Nishikimi T, Miyata A, Horio T, Yoshihara F, Nagaya N, Taldshita S, Yutani C, Matsuo H, Matsuoka H, Kangawa K 2000 Urocortin, a member of the corticotropinreleasing factor family, in normal and diseased heart. Am J Physiol Heart Circ Physiol 279:H3031–H3039

    PubMed  CAS  Google Scholar 

  35. Slominski A, Wortsman J, Pisarchik A, Zbytek B, Linton EA, Mazurkiewicz JE, Wei ET 2001 Cutaneous expression of corticotropin-releasing hormone (CRH), urocortin, and CRH receptors. Faseb J 15:1678–1693

    Article  PubMed  CAS  Google Scholar 

  36. Sasaki A, Shinkawa 0, Margioris A, Liotta AS, Sato S, Murakami 0, Go M, Shimizu Y, Hanew K, Yoshinaga K 1987 Immunoreactive corticotropin-releasing hormone in human plasma during pregnancy, labor, and delivery. J Clin Endocrinol Metab 64:224–229

    Article  PubMed  CAS  Google Scholar 

  37. Makrigiannakis A, Zoumakis E, Kalantaridou S, Coutifaris C, Margioris AN, Coukos G, Rice KC, Gravanis A, Chrousos GP 2001 Corticotropin-releasing hormone promotes blastocyst implantation and early maternal tolerance. Nat Immunol 2:1018–1024

    Article  PubMed  CAS  Google Scholar 

  38. Udelsman R, Harwood JP, Milan MA, Chrousos GP, Goldstein DS, Zimlichman R, Catt KJ, Aguilera G 1986 Functional corticotropin releasing factor receptors in the primate peripheral sympathetic nervous system. Nature 319:147–150

    Article  PubMed  CAS  Google Scholar 

  39. Smith R, Mesiano S, Chan EC, Brown S, Jaffe RB 1998 Corticotropin-releasing hormone directly and preferentially stimulates dehydroepiandrosterone sulfate secretion by human fetal adrenal cortical cells. J Clin Endocrinol Metab 83:2916–2920

    Article  PubMed  CAS  Google Scholar 

  40. Heinrich N, Meyer MR, Furkert J, Sasse A, Beyermann M, Bönigk W, Berger H 1998 Corticotropin-releasing factor (CRF) agonist stimulate testosterone production in mouse Leydig cells through CRF-receptor-1. Endocrinology 139:651–658

    Article  PubMed  CAS  Google Scholar 

  41. Suda T, Tomori N, Tozawa F, Mouri T, Demura H, Shizume K 1984 Distribution and characterization of immunoreactive corticotropin-releasing factor in human tissues. J Endocrinol Metab 59:861–866

    Article  CAS  Google Scholar 

  42. Orth DN 1992 Corticotropin-releasing hormone in humans. Endocrine Rev 13:164–191

    CAS  Google Scholar 

  43. Bittencourt JC, Vaughan J, Arias C, Rissman RA, Vale WW, Sawchenko PE 1999 Urocortin expression in rat brain. Evidence against a pervasive relationship of urocortincontaining projections with targets bearing type 2 receptors. J Comp Neurol 415:285–312

    Article  PubMed  CAS  Google Scholar 

  44. Aguilera G, Harwood JP, Wilson JX, Morell J, Brown JH, Katt KJ 1983 Mechanism of action of corticotropin releasing factor and other regulators of corticotropin release in rat pituitary cells. J Biol Chem 258:8039–8045

    PubMed  CAS  Google Scholar 

  45. Sakai K, Yamada M, Horiba N, Wakui M, Demura H, Suda T 1998 The genomic organisation of the human corticotropin-releasing factor type-1 receptor. Gene 219:125–130

    Article  PubMed  CAS  Google Scholar 

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

    Article  PubMed  CAS  Google Scholar 

  47. Vita N, Laurent P, Lefort S 1993 Primary structure and functional expression of a mouse pituitary and human brain corticotrophin releasing factor receptors. FEBS Lett 335:1–5

    Article  PubMed  CAS  Google Scholar 

  48. Perrin MH, Donaldson CJ, Cheng R, Lewis KA, Vale WW 1993 Cloning and functional expression of a rat brain corticotropin releasing factor (CRF) receptor. Endocrinology 133:3058–3061

    Article  PubMed  CAS  Google Scholar 

  49. Grammatopoulos DK, Dai Y, Randeva HS, Levine MA, Karteris E, Easton AJ, Hillhouse EW 1999 A novel spliced variant of the type 1 corticotropin-releasing hormone receptor with a deletion in the seventh transmembrane domain present in the human pregnant term myometrium and fetal membranes. Mol Endocrinol 13:2189–2202

    Article  PubMed  CAS  Google Scholar 

  50. Pisarchik A, Slominski AT 2001 Alternative splicing of CRH-R1 receptors in human and mouse skin: identification of new variants and their differential expression. Faseb J 15:2754–2756

    PubMed  CAS  Google Scholar 

  51. Liaw CW, Lovenberg TW, Barry G, Oltersdorf T, Grigoriadis DE, De Souza EB 1996 Cloning and characterization of the human corticotropin-releasing factor-2 receptor complementary deoxyribonucleic acid. Endocrinology 137:72–77

    Article  PubMed  CAS  Google Scholar 

  52. Valdenaire O, Giller T, Breu V, Gottowik J, Kilpatrick G 1997 A new functional isoform of the human CRF2 receptor for corticotropin-releasing factor. Biochim Biophys Acta 1352:129–132

    Article  PubMed  CAS  Google Scholar 

  53. Kostich WA, Chen A, Sperle K, Largent BL 1998 Molecular identification and analysis of a novel human corticotropin-releasing factor (CRF) receptor: the CRF2y receptor. Mol Endocrinol 12:1077–1085

    Article  PubMed  CAS  Google Scholar 

  54. Arai M, Assil IQ, Abou-Samra AB 2001 Chracterization of three corticotropin-releasing factor receptors in catfish: a novel third receptor is predominantly expressed in pituitary and urophysis. Endocrinology 142:446–454

    Article  PubMed  CAS  Google Scholar 

  55. Milian MA, Jacobowitz DM, Hauger RL, Catt KJ, Aguilera G 1986 Distribution of corticotropin-releasing factor receptors in primate brain. Proc Natl Acad Sci USA 83:1921–1925

    Article  Google Scholar 

  56. Mar Sanchez M, Young LJ, Plotsky PM, Insel TR 1999 Autoradiographic and in situ hybridization localization of corticotropin-releasing factor 1 and 2 receptors in nonhuman primate brain. J Comp Neurol 409:365–377

    Google Scholar 

  57. Perry MH, Vale WW 1999 Corticotropin releasing factor receptors and their ligand family. Ann N Y Acad Sci 885:312–328

    Google Scholar 

  58. Dieterich KD, Lehnert H, De Souza EB 1997 Corticotropin-releasing factor receptors: an overview. Exp Clin Endocrinol Diab 105:65–82

    CAS  Google Scholar 

  59. Aguilera G, Rabadan-Diehl C, Nikodemova M 2001 Regulation of pituitary corticotropin releasing hormone receptors. Peptides 22:769–774

    Article  PubMed  CAS  Google Scholar 

  60. Lovenberg TW, Liaw CW, Grigoriadis DE, Clevenger W, Chalmers DT, De Souza EB, Oltersdorf T 1995 Cloning and characterization of a functionally distinct corticotropin-releasing factor receptor subtype from rat brain. Proc Natl Acad Sci USA 92:836–840

    Article  PubMed  CAS  Google Scholar 

  61. Rominger DH, Rominger CM, Fitzgerald LW, Grzanna R, Largent BL, Zaczek 1998 Characterization of [125I]sauvagine binding to CRH2 receptors: membrane homogenate and autoradiographic studies. J Pharmacol Exp Ther 286:459–468

    PubMed  CAS  Google Scholar 

  62. Smith GW, Aubry JM, Dellu F, Contarino A, Bilezikjian LM, Gold LH, Chen R, Marchuk Y, Hauser C, Bentley CA, Sawchenko PE, Koob GF, Vale W, Lee KF 1998 Corticotropin releasing factor receptor 1-deficient mice display decreased anxiety, impaired stress response, and aberrant neuroendocrine development. Neuron 20: 1093–1102

    Article  PubMed  CAS  Google Scholar 

  63. Muller MB, Landgraf R, Preil J, Sillaber I, Kresse AE, Keck ME, Zimmermann S, Holsboer F, Wurst W 2000 Selective activation of the hypothalamic vassopressinergic system in mice deficient for the corticotropin-releasing hormone receptor 1 is dependent on glucocorticoids. Endocrinology 141:4262–4269

    Article  PubMed  CAS  Google Scholar 

  64. Muglia LJ, Jacobson L, Weninger SC, Karalis KP, Jeong KH, Majzoub 2001 The physiology of corticotropin-releasing hormone deficiency in mice. Peptides 22:725–731

    Article  PubMed  CAS  Google Scholar 

  65. Timpl P, Spanagel R, Sillaber I, Kresse A, Reul JMHM, Stalla GK, Blanquet V, Steckler T, Holsboer F, Wurst W 1998 Impaired stress response and reduced anxiety in mice lacking a functional corticotropin-releasing hormone receptor 1. Nature Genet 19:162–166

    Article  PubMed  CAS  Google Scholar 

  66. Coste SC, Kesterson RA, Heldwein KA, Stevens SL, Heard AD, Hollis JH, Murray SE, Hill JK, Pantely GA, Hohimer AR, Hatton DC, Phillips TJ, Finn DA, Low MJ, Rittenberg MB, Stenzel P, Stenzel-Poore MP 2000 Abnormal adaptations to stress and impaired cardiovascular function in mice lacking corticotropin-releasing hormone receptor-2. Nature Genet 24:403–409

    Article  PubMed  CAS  Google Scholar 

  67. Bale TL, Contarino A, Smith GW, Chan R, Gold LH, Sawchenko PE, Koob GF, Vale WW, Lee KF 2000 Mice deficient for corticotropin-releasing hormone receptor-2 display anxiety-like behaviour and are hypersensitive to stress. Nature Genet 24:410–414

    Article  PubMed  CAS  Google Scholar 

  68. Kishimoto T, Radulovic J, Radulovic M, Lin CR, Schrick C, Hooshmand F, Hermanson O, Rosenfeld MG, Spiess J 2000 Deletion of Crhr2 reveals an anxiolytic role for corticotropin-releasing hormone receptor-2. Nature Genet 24:415–419

    Article  PubMed  CAS  Google Scholar 

  69. Behan DP, Linton EA, Lowry PJ 1989 Isolation of the human plasma corticotropinreleasing factor protein. J Endocrinol 122:23–31

    Article  PubMed  CAS  Google Scholar 

  70. Behan DP, Grigoriadis DE, Lovenberg T, Chalmers D, Heinrichs S, Liaw C, De Souza EB 1996 Neurobiology of corticotropin releasing factor (CRF) receptors and CRFbinding protein: implications for the treatment of CNS disorders. Mol Psych 1:265–277

    CAS  Google Scholar 

  71. Chatzaki E, Margioris AN, Gravanis A 2002 Expression and regulation of corticotropin-releasing hormone protein (CRH-BP) in rat adrenals. J Neurochem 80:81–90

    Article  PubMed  CAS  Google Scholar 

  72. Burrows HL, Nakajima M, Lesh JS, Goosens KA, Samuelson LC, Inui A, Camper SA, Seasholtz AF 1998 Excess corticotropin-releasing hormone binding protein in the hypothalamic-pituitary-adrenal axis in transgenic mice. J Clin Invest 101:1–9

    Article  Google Scholar 

  73. Seasholtz AF, Burrows HL, Karolyi IJ, Camper SA 2001 Mouse models of altered CRH-binding protein expression. Peptides 22:743–751

    Article  PubMed  CAS  Google Scholar 

  74. Behan DP, Heinrichs SC, Troncoso JC, Liu XJ, Kawas CH, Ling N, De Souza EB 1995 Displacement of corticotropin releasing factor from its binding protein as a possible treatment for Alzheimer’s disease. Nature 378: 284–287

    Article  PubMed  CAS  Google Scholar 

  75. Gilligan PJ, Robertson DW, Zaczek R 2000 Corticotropin releasing factor (CRF) receptor modulators: progress and opportunities for new therapeutic agents. J Med Chem 43:1641–1660

    Article  PubMed  CAS  Google Scholar 

  76. Grigoriadis DE, Haddach M, Ling N, Saunders J 2001 The CRF receptor: structure, function and potential for therapeutic intervention. Curr Med Chem CNSA 1(1)

    Google Scholar 

  77. Eckart K, Jahn O, Radulovic J, Tezval H, van Werven L, Spiess J 2001 A single amino acid serves as an affinity switch between the receptor and the binding protein of corticotropin-releasing factor: implications for the design of agonists and antagonists. Proc. Natl Acad Sci USA 98:11142–11147

    Article  CAS  Google Scholar 

  78. Rivier J, Rivier C, Vale W 1984 Synthetic competitive antagonists of corticotropinreleasing factor: effect on ACTH secretion in the rat. Science 224:889–891

    Article  PubMed  CAS  Google Scholar 

  79. Kornreich WD, Galyean R, Hernandez JF, Craig AG, Donaldson CJ, Yamamoto G, Rivier C, Vale W, Rivier J 1992 Alanine series of ovine corticotropin releasing factor (oCRF): structure-activity relationship study. J Med Chem 35:1870–1876

    Article  PubMed  CAS  Google Scholar 

  80. Lau SH, Rivier J, Vale W, Kaiser ET, Kezdy FJ 1983 Surface properties of an amphiphilic peptide hormone and of its analog: corticotropin-releasing factor and sauvagine. Proc Natl Acad Sci USA 80:7070–7074

    Article  PubMed  CAS  Google Scholar 

  81. Britton KT, Lee G, Vale W, Rivier J, Koob GF 1986 Corticotropin releasing factor (CRF) receptor antagonist blocks activating and anxiogenic actions of CRF in the rat. Brain Res 369:303–306

    Article  PubMed  CAS  Google Scholar 

  82. Gulyas J, Rivier C, Perrin M, Koerber SC, Sutton S, Corrigan A, Lahrichi SL, Craig AG, Vale W, Rivier J 1995 Potent, structurally constrained agonists and competitive antagonists of corticotropin-releasing factor. Proc Natl Acad Sci USA 92:10575–10579

    Article  PubMed  CAS  Google Scholar 

  83. Riihmann A, Bonk I, Lin CR, Rosenfeld MG, Spiess J 1998 Structural requirements for peptidic antagonists of the corticotropin-releasing factor receptor (CRFR): Development of CRFR2I3-selective antisauvagine-30. Proc Natl Acad Sci USA 95:15264–15269

    Article  Google Scholar 

  84. Radulovic J, Ruhmann A, Liepold T, Spiess J 1999 Modulation of learning and anxiety by corticotropin-releasing factor (CRF) and stress: Differential roles of CRF receptors 1 and 2. J Neuroscience 19:5016–5025

    CAS  Google Scholar 

  85. Liaw CW, Grigoriadis DE, Lorang MT, De Souza EB, Maid RA 1997 Localization of agonist-and antagonist-binding domains of human corticotropin-releasing factor receptors. Mol Endocrinol 11:2048–2053

    Article  PubMed  CAS  Google Scholar 

  86. Chen YL, Mansbach RS, Winter SM, Brooks E, Collins J, Corman ML, Dunaiskis AR, Faraci WS, Gallaschun RJ, Schmidt A, Schulz DW 1997 Synthesis and oral efficacy of a 4-(butylethylamino)pyrrolo[2,3-d]pyrimidine: a centrally active corticotropin-releasing factor 1 receptor antagonist. J Med Chem 40:1749–1754

    Article  PubMed  CAS  Google Scholar 

  87. Arborelius L, Skelton KH, Thrivikraman KV, Plotsky PM, Schulz DW, Owens MJ 2000 Chronic administration of the selective corticotropin-releasing Factor 1 receptor antagonist CP-154,526: behavioral, endocrine and neurochemical effects in the rat. J Pharm Exp Ther 294(2): 588–597

    CAS  Google Scholar 

  88. Webster EL, Lewis DB, Torpy DJ, Zachman EK, Rice KC, Chrousos GP 1996 In vivo and in vitro characterization of antalarmin, a nonpeptide corticotropin-releasing hormone (CRH) receptor antagonist: suppression of pituitary ACTH release and peripheral inflammation. Endocrinology 137:5747–5750

    Article  PubMed  CAS  Google Scholar 

  89. Bornstein SR, Webster EL, Torpy DJ, Richman SJ, Mitsiades N, Igel M, Lewis DB, Rice KC, Joost HG, Tsokos M, Chrousos GP 1998 Chronic effects of a nonpeptide corticotropin-releasing hormone type 1 receptor antagonist on pituitary-adrenal function, body weight, and metabolic regulation. Endocrinology 139:1546–1555

    Article  PubMed  CAS  Google Scholar 

  90. Habib KE, Weld KP, Rice KC, Pushkas J, Champoux M, Listwack S, Webster EL, Atkinson AJ, Schulkin J, Contoreggi C, Chrousos GP, McCann SM, Suomi SJ, Higley JD, Gold PW 2000 Oral administration of a corticotropin-releasing hormone receptor antagonist significantly attenuates behavioral, neuroendocrine, and auotomic responses to stress in primates. Proc Natl Acad Sci USA 97:6079–6084

    Article  PubMed  CAS  Google Scholar 

  91. Hsin LW, Tian X, Webster EL, Coop A, Caldwell TM, Jacobson AE, Chrousos GP, Gold PW, Habib KE, Ayala A, Eckelman WC, Contoreggi C, Rice KC 2002 CRHR1 receptor binding and lipophilicity of pyrrolopyrimidines, potential nonpeptide corticotropin-releasing hormone type 1 receptor antagonists. Biorg Med Chem 10:175–183

    Article  CAS  Google Scholar 

  92. Nakazato A, Kumagai T, Okubo T, Tanaka H, Chaki S, Okuyama S, Tomisawa K 2000 Design, synthesis and structure-affinity relationships of 4-methylidenepiperidine and 4-aryl-1,2,3,6-tetrahydropyridine derivatives as corticotropin-releasing factor 1 receptor antagonists. Biorg Med Chem 8:1183–1193

    Article  CAS  Google Scholar 

  93. Zobel AW, Nickel T, Kiinzel HE, Acid N, Sonntag A, Ising M, Holsboer F 2000 Effects of the high-affinity corticotropin-releasing hormone receptor 1 antagonist R121919 in major depression: the first 20 patients treated. J Psych Res 34:171–181

    Article  CAS  Google Scholar 

  94. Mackay KB, Bozigian H, Grigoriadis DE, Loddick SA, Verge G, Foster AC 2001 Neuroprotective effects of the CRF1 antagonist R121920 after permanent focal ischemia in the Rat. J Cereb Blood Flow Metab 21:1208–1214

    Article  PubMed  CAS  Google Scholar 

  95. Strijbos PJ, Relton JK, Rothwell NJ 1994 Corticotrophin-releasing factor antagonist inhibits neuronal damage induced by focal cerebral ischaemia or activation od NMDA receptors in the brain. Brain Res 656:405–408

    Article  PubMed  CAS  Google Scholar 

  96. Roe SY, McGowan EM, Rothwell NJ 1998 Evidence for the involvement of corticotrophin-releasing hormone in the pathogenesis of taumatic brain injury. Eur J Neurosci 10:553–559

    Article  PubMed  CAS  Google Scholar 

  97. Morrison J 1967. The End. The Doors (Electra/Asylum Rec.)

    Google Scholar 

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Maier, C., Kotzmann, H., Luger, A. (2003). CRH-Receptors and their Ligands. In: Gaillard, R.C. (eds) The Acth Axis: Pathogenesis, Diagnosis and Treatment. Endocrine Updates, vol 21. Springer, Boston, MA. https://doi.org/10.1007/978-1-4615-0501-3_4

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