Cortagine: Behavioral and autonomic function of the selective CRF receptor subtype 1 agonist

CNS Drug Reviews

Volumn 13, Issue 4, 2007, Pages 423-443

  Farrokhi, Catherine Borna ^a   Tovote, Philip ^c   Blanchard, Robert J ^a   Blanchard, D Caroline ^b   Litvin, Yoav ^a   Spiess, Joachim ^c  

^a UNIVERSITY OF HAWAII   (United States)

^b UNIVERSITY OF HAWAII   (United States)

^c UNIVERSITY OF HAWAII   (United States)

Author keywords

Anxiety; Behavior; Cortagine; Corticotrophin; CRF1 agonist; CRH; Defense; Depression

Indexed keywords

3 (6 DIMETHYLAMINO 4 METHYL 3 PYRIDINYL) 7 DIPROPYLAMINO 2,5 DIMETHYLPYRAZOLO[1,5 A]PYRIMIDINE; 4 (2 CHLORO 4 METHOXY 5 METHYLPHENYL) N [2 CYCLOPROPYL 1 (3 FLUORO 4 METHYLPHENYL)ETHYL] 5 METHYL N (2 PROPYNYL) 2 THIAZOLAMINE; ANTALARMIN; BUTYL[2,5 DIMETHYL 7 (2,4,6 TRIMETHYLPHENYL) 7H PYRROLO[2,3 D]PYRIMIDIN 4 YL]ETHYLAMINE; CORTAGINE; CORTICOTROPIN RELEASING FACTOR ANTAGONIST; CORTICOTROPIN RELEASING FACTOR RECEPTOR 1; CORTICOTROPIN RELEASING FACTOR RECEPTOR 2; PEPTIDE DERIVATIVE; SAUVAGINE; UNCLASSIFIED DRUG;

AMINO ACID SEQUENCE; ANIMAL BEHAVIOR; CHIMERA; CLINICAL TRIAL; DEPRESSION; DRUG MECHANISM; DRUG MEGADOSE; EXERCISE TEST; HEART RATE VARIABILITY; HUMAN; IC 50; LOW DRUG DOSE; MAZE TEST; NONHUMAN; RECEPTOR AFFINITY; RECEPTOR BINDING; REVIEW; TRANSGENIC RAT;

ANIMALS; AUTONOMIC NERVOUS SYSTEM; BEHAVIOR, ANIMAL; CORTICOTROPIN-RELEASING HORMONE; HUMANS; RECEPTORS, CORTICOTROPIN-RELEASING HORMONE; RECOMBINANT FUSION PROTEINS;

EID: 36849012583     PISSN: 1080563X     EISSN: None     Source Type: Journal    
DOI: 10.1111/j.1527-3458.2007.00027.x     Document Type: Review

References (92)

1. Antoni FA (1986) Hypothalamic control of adrenocorticotropin secretion: Advances since the discovery of 41-residue corticotropin-releasing factor. Endocr Rev 7 : 351 378.
2. Arborelius L, Owens MJ, Plotsky PM, Nemeroff CB (1999) The role of corticotropin-releasing factor in depression and anxiety disorders. J Endocrinol 160 : 1 12.
3. 1A receptor antagonist WAY-100635. Int J Neuropsychopharmacol 4 : 399 408.
4. Bale TL, Vale WW (2003) Increased depression-like behaviors in corticotropin-releasing factor receptor-2-deficient mice: Sexually dichotomous responses. J Neurosci 23 : 5295 5301.
5. Bale TL, Vale WW (2004) CRF and CRF receptors: Role in stress responsivity and other behaviors. Annu Rev Pharmacol Toxicol 44 : 525 557.
6. Basso AM, Spina M, Rivier J, Vale W, Koob GF (1999) Corticotropin- releasing factor antagonist attenuates the "anxiogenic-like" effect in the defensive burying paradigm but not in the elevated plus-maze following chronic cocaine in rats. Psychopharmacology (Berl) 145 : 21 30.
7. Behbehani MM (1995) Functional characteristics of the midbrain periaqueductal gray. Prog Neurobiol 46 : 575 605.
8. Blanchard DC, Blanchard RJ (1990) An ethoexperimental analysis of defense, fear, and anxiety. Published in Anxiety, University of Otago Press, Dunedin.
9. Blanchard DC, Blanchard RJ, Griebel G (2005) Defensive responses to predator threat in the rat and mouse. Curr Protocols Neurosci 8.19.1-8.19.20. John Wiley & Sons.
10. Blanchard RJ, Griebel G, Hendrie JA, Blanchard DC (1997) Differentiation of anxiolytic and panicolytic drugs by effects on rat and mouse defense test batteries. Neurosci Biobehav Rev 21 : 783 789.
11. Blanchard DC, Hynd AL, Minke KA, Minemoto T, Blanchard RJ (2001) Human defensive behaviors to threat scenarios show parallels to fear- and anxiety-related defense patterns of non-human mammals. Neurosci Biobehav Rev 25 : 761 770.
12. Blanchard RJ, Shepherd JK, Rodgers RJ, Magee L, Blanchard DC (1993a) Attenuation of antipredator defensive behavior in rats following chronic treatment with imipramine. Psychopharmacology (Berl) 110 : 245 253.
13. Blanchard RJ, Yudko EB, Rodgers RJ, Blanchard DC (1993b) Defense system psychopharmacology: An ethological approach to the pharmacology of fear and anxiety. Behav Brain Res 58 : 155 165.
14. Bowers LK, Swisher CB, Behbehani MM (2003) Membrane and synaptic effects of corticotropin-releasing factor on periaqueductal gray neurons of the rat. Brain Res 981 : 52 57.
15. Bremner JD, Southwick SM, Darnell A, Charney DS (1996) Chronic PTSD in Vietnam combat veterans: Course of illness and substance abuse. Am J Psychiatry 153 : 369 375.
16. Buwalda B, de Boer SF, Van Kalkeren AA, Koolhaas JM (1997) Physiological and behavioral effects of chronic intracerebroventricular infusion of corticotropin-releasing factor in the rat. Psychoneuroendocrinology 22 : 297 309.
17. Canteras NS, Goto M (1999) Fos-like immunoreactivity in the periaqueductal gray of rats exposed to a natural predator. Neuroreport 10 : 413 418.
18. Carvalho-Netto EF, Litvin Y, Nunes-de-Souza RL, Blanchard DC, Blanchard RJ (2007) Effects of intra-PAG infusion of ovine CRF on defensive behaviors in Swiss-Webster mice. Behav Brain Res 176 : 222 229.
19. Cavalcante JC, Sita LV, Mascaro MB, Bittencourt JC, Elias CF (2006) Distribution of urocortin 3 neurons innervating the ventral premammillary nucleus in the rat brain. Brain Res 1089 : 116 125.
20. Chalmers DT, Lovenberg TW, De Souza EB (1995). Localization of novel corticotropin-releasing factor receptor (CRF2) mRNA expression to specific subcortical nuclei in rat brain: comparison with CRF1 receptor mRNA expression. J Neurosci 15 : 6340 6350.
21. Chen CY, Doong ML, Rivier JE, Taché Y (2003) Intravenous urocortin II decreases blood pressure through CRF2 receptor in rats. Regul Pept 113 : 125 130.
22. Contarino A, Dellu F, Koob GF, Smith GW, Lee KF, Vale W, Gold LH (1999). Reduced anxiety-like and cognitive performance in mice lacking the corticotropin-releasing factor receptor 1. Brain Res 835 : 1 9.
23. Coste SC, Kesterson RA, Heldwein KA, Stevens SL, Heard AD, Hollis JH, Murray SE, Hill JK, Pantely GA, Hohimer AR, et al. (2000) Abnormal adaptations to stress and impaired cardiovascular function in mice lacking corticotropin-releasing hormone receptor-2. Nat Genet 24 : 403 409.
24. Dautzenberg FM, Hauger RL (2002) The CRF peptide family and their receptors: Yet more partners discovered. Trends Pharmacol Sci 23 : 71 77.
25. De Boer SF, Koolhaas JM (2003) Defensive burying in rodents: Ethology, neurobiology and psychopharmacology. Eur J Pharmacol 463 : 145 161.
26. De Souza EB, Nemeroff CB (1990) Corticotropin-releasing factor: Basic and clinical studies of a neuropeptide. CRC Press.
27. Dielenberg RA, Hunt GE, McGregor IS (2001) "When a rat smells a cat": The distribution of Fos immunoreactivity in rat brain following exposure to a predatory odor. Neuroscience 104 : 1085 1097.
28. Farrokhi C, Blanchard DC, Griebel G, Yang M, Gonzales C, Markham C, Blanchard RJ (2004) Effects of the CRF1 antagonist SSR125543A on aggressive behaviors in hamsters. Pharmacol Biochem Behav 77 : 465 469.
29. French JA, Fite JE, Jensen H, Oparowski K, Rukstalis MR, Fix H, Jones B, Maxwell H, Pacer M, Power ML, et al. (2007) Treatment with CRH-1 antagonist antalarmin reduces behavioral and endocrine responses to social stressors in marmosets (Callithrix kuhlii). Am J Primatol (In press).
30. Funk CK, Zorrilla EP, Lee MJ, Rice KC, Koob GF (2007) Corticotropin-releasing factor 1 antagonists selectively reduce ethanol self-administration in ethanol-dependent rats. Biol Psychiatry 61 : 78 86.
31. Gammie SC, Stevenson SA (2006) Intermale aggression in corticotropin-releasing factor receptor 1 deficient mice. Behav Brain Res 171 : 63 69.
32. Gehlert DR, Shekhar A, Morin SM, Hipskind PA, Zink C, Gackenheimer SL, Shaw J, Fitz SD, Sajdyk TJ (2005) Stress and central urocortin increase anxiety-like behavior in the social interaction test via the CRF1 receptor. Eur J Pharmacol 509 : 145 153.
33. Gray TS (1990) The organization and possible function of amygdyloid corticotropin-releasing factor pathways. In : De Souza EB and Nemeroff CB, eds. Corticotropin releasing factor: Basic and clinical studies of a neuropeptide. Florida : CRC Press, 53 68.
34. Gray JA, McNaughton N (2000) The neuropsychology of anxiety: An enquiry into the function of the septo-hippocampal system, Vol. XVI. Oxford, NY : Oxford University Press.
35. Griebel G, Blanchard DC, Agnes RS, Blanchard RJ (1995) Differential modulation of antipredator defensive behavior in Swiss-Webster mice following acute or chronic administration of imipramine and fluoxetine. Psychopharmacology (Berl) 120 : 57 66.
36. Griebel G, Blanchard DC, Blanchard RJ (1996) Predator-elicited flight responses in Swiss-Webster mice: An experimental model of panic attacks. Prog Neuropsychopharmacol Biol Psychiatry 20 : 185 205.
37. Griebel G, Blanchard DC, Jung A, Lee JC, Masuda CK, Blanchard RJ (1995a) Further evidence that the mouse defense test battery is useful for screening anxiolytic and panicolytic drugs: Effects of acute and chronic treatment with alprazolam. Neuropharmacology 34 : 1625 1633.
38. 1A agonists modulate mouse antipredator defensive behavior differently from the 5-HT2A antagonist pirenperone. Pharmacol Biochem Behav 51 : 235 244.
39. Griebel G, Simiand J, Steinberg R, Jung M, Gully D, Roger P, Geslin M, Scatton B, Maffrand JP, Soubrie P (2002) 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 : 333 345.
40. Gutman DA, Owens MJ, Skelton KH, Thrivikraman KV, Nemeroff CB (2003) The corticotropin-releasing factor1 receptor antagonist R121919 attenuates the behavioral and endocrine responses to stress. J Pharmacol Exp Ther 304 : 874 880.
41. Harro J, Tonissaar M, Eller M (2001) The effects of CRA 1000, a non-peptide antagonist of corticotropin-releasing factor receptor type 1, on adaptive behaviour in the rat. Neuropeptides 35 : 100 109.
42. Heim C, Owens MJ, Plotsky PM, Nemeroff CB (1997) Persistent changes in corticotropin-releasing factor systems due to early life stress: Relationship to the pathophysiology of major depression and post-traumatic stress disorder. Psychopharmacol Bull 33 : 185 192.
43. Held K, Kunzel H, Ising M, Schmid DA, Zobel A, Murck H, Holsboer F, Steiger A (2004) Treatment with the CRH1-receptor-antagonist R121919 improves sleep-EEG in patients with depression. J Psychiatr Res 38 : 129 136.
44. Herman JP, Ostrander MM, Mueller NK, Figueiredo H (2005) Limbic system mechanisms of stress regulation: Hypothalamo-pituitary-adrenocortical axis. Prog Neuropsychopharmacol Biol Psychiatry 29 : 1201 1213.
45. Hodgson RA, Higgins GA, Guthrie DH, Lu SX, Pond AJ, Mullins DE, Guzzi MF, Parker EM, Varty GB (2007) Comparison of the V1b antagonist, SSR149415, and the CRF1 antagonist, CP-154,526, in rodent models of anxiety and depression. Pharmacol Biochem Behav 86 : 431 440.
46. Hsu SY, Hsueh AJ (2001) Human stresscopin and stresscopin-related peptide are selective ligands for the type 2 corticotropin-releasing hormone receptor. Nat Med 7 : 605 611.
47. Jones DN, Kortekaas R, Slade PD, Middlemiss DN, Hagan JJ (1998) The behavioural effects of corticotropin-releasing factor-related peptides in rats. Psychopharmacology (Berl) 138 : 124 132.
48. Kalin NH, Shelton SE, Kraemer GW, McKinney WT (1983) Corticotropin- releasing factor administered intraventricularly to rhesus monkeys. Peptides 4 : 217 220.
49. Kostich WA, Grzanna R, Lu NZ, Largent BL (2004) Immunohistochemical visualization of corticotropin-releasing factor type 1 (CRF1) receptors in monkey brain. J Comp Neurol 478 : 111 125.
50. Kunzel HE, Zobel AW, Nickel T, Ackl N, Uhr M, Sonntag A, Ising M, Holsboer F (2003) Treatment of depression with the CRH-1-receptor antagonist R121919: Endocrine changes and side effects. J Psychiatr Res 37 : 525 533.
51. Lancel M, Muller-Preuss P, Wigger A, Landgraf R, Holsboer F (2002) The CRH1 receptor antagonist R121919 attenuates stress-elicited sleep disturbances in rats, particularly in those with high innate anxiety. J Psychiatr Res 36 : 197 208.
52. Lelas S, Wong H, Li YW, Heman KL, Ward KA, Zeller KL, Sieracki KK, Polino JL, Godonis HE, Ren SX, et al. (2004) Anxiolytic-like effects of the corticotropin-releasing factor1 (CRF1) antagonist DMP904 [4-(3-pentylamino)-2,7- dimethyl-8-(2-methyl-4-methoxyphenyl)-pyrazolo-[1,5-a]-pyrimidine] administered acutely or chronically at doses occupying central CRF1 receptors in rats. J Pharmacol Exp Ther 309 : 293 302.
53. Li C, Vaughan J, Sawchenko PE, Vale WW (2002) Urocortin III-immunoreactive projections in rat brain: Partial overlap with sites of type 2 corticotropin-releasing factor receptor expression. J Neurosci 22 : 991 1001.
54. Li YW, Fitzgerald L, Wong H, Lelas S, Zhang G, Lindner MD, Wallace T, McElroy J, Lodge NJ, Gilligan P, et al. (2005) The pharmacology of DMP696 and DMP904, non-peptidergic CRF1 receptor antagonists. CNS Drug Rev 11 : 21 52.
55. Lim MM, Tsivkovskaia NO, Bai Y, Young LJ, Ryabinin AE (2006) Distribution of corticotropin-releasing factor and urocortin 1 in the vole brain. Brain Behav Evol 68 : 229 240.
56. Litvin Y, Pentkowski N, Blanchard DC, Blanchard RJ (2007) CRF type 1 receptors in the dorsal periaqueductal gray modulate anxiety-induced defensive behaviors. Horm Behav 52 : 244 251.
57. Lovenberg TW, Chalmers DT, Liu C, De Souza EB (1995) CRF2 alpha and CRF2 beta receptor mRNAs are differentially distributed between the rat central nervous system and peripheral tissues. Endocrinology 136 : 4139 4142.
58. Lowry CA, Moore FL (2006) Regulation of behavioral responses by corticotropin-releasing factor. Gen Comp Endocrinol 146 : 19 27.
59. Maier SF, Seligman SEP (1976) Learned helplessness: Theory and evidence. J Exp Psychol Gen 105 : 3 46.
60. Menzaghi F, Howard RL, Heinrichs SC, Vale W, Rivier J, Koob GF (1994) Characterization of a novel and potent corticotropin-releasing factor antagonist in rats. J Pharmacol Exp Ther 269 : 564 572.
61. Nemeroff CB, Widerlov E, Bissette G, Walleus H, Karlsson I, Eklund K, Kilts CD, Loosen PT, Vale W (1984) Elevated concentrations of CSF corticotropin-releasing factor-like immunoreactivity in depressed patients. Science 226 : 1342 1344.
62. Nerozzi D, Bersani G, Melia E, Magnani A, Antonozzi I, Frajese G (1988) Corticotropin-releasing factor and adrenal function in major depression. J Endocrinol Invest 11 : 697 701.
63. Overstreet DH, Griebel G (2004) Antidepressant-like effects of CRF1 receptor antagonist SSR125543 in an animal model of depression. Eur J Pharmacol 497 : 49 53.
64. Overton J, Fisher L (1991) Differentiated hemodynamic responses to central versus peripheral administration of corticotropin-releasing factor in conscious rats. J Autonom Nerv Syst 35 : 43 52.
65. Parkes DG, Weisinger RS, May CN (2001) Cardiovascular actions of CRH and urocortin: An update. Peptides 22 : 821 827.
66. Pelleymounter MA, Joppa M, Ling N, Foster AC (2002) Pharmacological evidence supporting a role for central corticotropin-releasing factor(2) receptors in behavioral, but not endocrine, response to environmental stress. J Pharmacol Exp Ther 302 : 145 152.
67. Petit-Demouliere B, Chenu F, Bourin M (2005) Forced swimming test in mice: A review of antidepressant activity. Psychopharmacology (Berl) 177 : 245 255.
68. Porsolt RD (1979) Animal model of depression. Biomedicine 30 : 139 140.
69. Porsolt RD, Le Pichon M, Jalfre M (1977) Depression: A new animal model sensitive to antidepressant treatments. Nature 266 : 730 732.
70. Richter R, Mulvany M (1995) Comparison of hCRF and oCRF effects on cardiovascular responses after central, peripheral, and in vitro application. Peptides 16 : 843 849.
71. Rivier J, Gulyas J, Kunitake K, DiGruccio M, Cantle JP, Perrin MH, Donaldson C, Vaughan J, Million M, Gourcerol G, et al. (2007) Stressin1-A, a potent corticotropin releasing factor receptor 1 (CRF1)-selective peptide agonist. J Med Chem 50 : 1668 1674.
72. Sanchez MM, 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 408 : 365 377.
73. Sautter FJ, Bissette G, Wiley J, Manguno-Mire G, Schoenbachler B, Myers L, Johnson JE, Cerbone A, Malaspina D (2003) Corticotropin-releasing factor in posttraumatic stress disorder (PTSD) with secondary psychotic symptoms, nonpsychotic PTSD, and healthy control subjects. Biol Psychiatry 54 : 1382 1388.
74. Sheehan TP, Chambers RA, Russell DS (2004) Regulation of affect by the lateral septum: Implications for neuropsychiatry. Brain Res Brain Res Rev 46 : 71 117.
75. Skelton KH, Gutman DA, Thrivikraman KV, Nemeroff CB, Owens MJ (2007) The CRF(1) receptor antagonist R121919 attenuates the neuroendocrine and behavioral effects of precipitated lorazepam withdrawal. Psychopharmacology (Berl) (In press).
76. Smith GW, Aubry JM, Dellu F, Contarino A, Bilezikjian LM, Gold LH, Chen R, Marchuk Y, Hauser C, Bentley CA, et al. (1998) Corticotropin releasing factor receptor 1-deficient mice display decreased anxiety, impaired stress response, and aberrant neuroendocrine development. Neuron 20 : 1093 1102.
77. Spiess J, Rivier J, Rivier C, Vale WW (1981) Primary structure of corticotropin-releasing factor from ovine hypothalamus. Proc Natl Acad Sci U S A 78 : 6517 6521.
78. Steru L, Chermat R, Thierry B, Mico JA, Lenegre A, Steru M, Simon P, Porsolt RD (1987) The automated tail suspension test: A computerized device which differentiates psychotropic drugs. Prog Neuropsychopharmacol Biol Psychiatry 11 : 659 671.
79. Stiedl O, Meyer M, Jahn O, Ogren SO, Spiess J (2005) Corticotropin- releasing factor receptor 1 and central heart rate regulation in mice during expression of conditioned fear. J Pharmacol Exp Ther 312 : 905 916.
80. Stiedl O, Meyer M, Kishimoto T, Rosenfeld MG, Spiess J (2003) Stress-mediated heart rate dynamics after deletion of the gene encoding corticotropin-releasing factor receptor 2. Eur J Neurosci 17 : 2231 2235.
81. Takahashi LK (2001) Role of CRF(1) and CRF(2) receptors in fear and anxiety. Neurosci Biobehav Rev 25 : 627 636.
82. Tezval H, Jahn O, Todorovic C, Sasse A, Eckart K, Spiess J (2004) Cortagine, a specific agonist of corticotropin-releasing factor receptor subtype 1, is anxiogenic and antidepressive in the mouse model. Proc Natl Acad Sci U S A 101 : 9468 9473.
83. Timpl P, Spanagel R, Sillaber I, Kresse A, Reul JM, 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. Nat Genet 19 : 162 166.
84. Todorovic C, Jahn O, Tezval H, Hippel C, Spiess J (2005) The role of CRF receptors in anxiety and depression: Implications of the novel CRF1 agonist cortagine. Neurosci Biobehav Rev 29 : 1323 1333.
85. Valdez GR (2006) Development of CRF1 receptor antagonists as antidepressants and anxiolytics: Progress to date. CNS Drugs 20 : 887 896.
86. Valdez GR, Inoue K, Koob GF, Rivier J, Vale W, Zorrilla EP (2002) Human urocortin II: Mild locomotor suppressive and delayed anxiolytic-like effects of a novel corticotropin-releasing factor related peptide. Brain Res 943 : 142 150.
87. Vale WW, Spiess J, Rivier C, Rivier J (1981) Characterization of a 41-residue ovine hypothalamic peptide that stimulates secretion of corticotropin and beta-endorphin. Science 213 : 1394 1397.
88. Van Pett K, Viau V, Bittencourt JC, Chan RK, Li HY, Arias C, Prins GS, Perrin M, Vale W, Sawchenko PE (2000) Distribution of mRNAs encoding CRF receptors in brain and pituitary of rat and mouse. J Comp Neurol 428 : 191 212.
89. Whitnall MH (1993) Regulation of the hypothalamic corticotropin-releasing hormone neurosecretory system. Prog Neurobiol 40 : 573 629.
90. Widerlov E, Bissette G, Nemeroff CB (1988) Monoamine metabolites, corticotropin releasing factor and somatostatin as CSF markers in depressed patients. J Affect Disord 14 : 99 107.
91. Yang M, Augustsson H, Markham CM, Hubbard DT, Webster D, Wall PM, Blanchard RJ, Blanchard DC (2004) The rat exposure test: A model mouse defensive behaviors. Physiol Behav 81 : 465 473.
92. Zobel AW, Nickel T, Kunzel HE, Ackl 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 Psychiatr Res 34 : 171 181.