Effects of corticotropin-releasing factor 1 receptor antagonism on the hypothalamic-pituitary-adrenal axis of rodents

Journal of Pharmacology and Experimental Therapeutics

Volumn 341, Issue 3, 2012, Pages 672-680

  Gehlert, Donald R ^a   Cramer, Jeffrey ^a   Morin, S Michelle ^a  

^a ELI LILLY AND COMPANY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3 (4 CHLORO 2 MORPHOLIN 4 YL THIAZOL 5 YL) 8 (1 ETHYLPROPYL) 2,6 DIMETHYL IMIDAZO[1,2 B]PYRIDAZINE; ALCOHOL; CAFFEINE; CORTICOSTERONE; CORTICOTROPIN; CORTICOTROPIN RELEASING FACTOR ANTAGONIST; CORTICOTROPIN RELEASING FACTOR RECEPTOR 1; INSULIN; MTIP; UNCLASSIFIED DRUG; YOHIMBINE;

ALCOHOL CONSUMPTION; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; AREA UNDER THE CURVE; ARTICLE; CONCENTRATION RESPONSE; CONTROLLED STUDY; CORTICOSTERONE BLOOD LEVEL; CORTICOTROPIN BLOOD LEVEL; DRUG BLOOD LEVEL; DRUG EFFICACY; DRUG SCREENING; DRUG SYNTHESIS; ENDOCRINE FUNCTION; ENZYME INHIBITION; HORMONE INHIBITION; HORMONE RELEASE; HYPERINSULINEMIA; HYPOTHALAMUS HYPOPHYSIS ADRENAL SYSTEM; MALE; MAXIMUM PLASMA CONCENTRATION; MOUSE; NONHUMAN; PHARMACOLOGICAL STIMULATION; PRIORITY JOURNAL; PROTEIN FUNCTION; RECEPTOR BLOCKING; SINGLE DRUG DOSE;

ADRENOCORTICOTROPIC HORMONE; AMPHIBIAN PROTEINS; ANIMALS; AREA UNDER CURVE; CORTICOSTERONE; HYPOTHALAMO-HYPOPHYSEAL SYSTEM; INFUSIONS, INTRAVENTRICULAR; MALE; MICE; MICE, INBRED C57BL; PEPTIDE HORMONES; PITUITARY-ADRENAL SYSTEM; PYRIDAZINES; RADIOIMMUNOASSAY; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, CORTICOTROPIN-RELEASING HORMONE; THIAZOLES;

EID: 84861548194     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.111.189753     Document Type: Article

References (38)

1. Anisman H, Hayley S, Kelly O, Borowski T, and Merali Z (2001) Psychogenic, neurogenic, and systemic stressor effects on plasma corticosterone and behavior: mouse strain-dependent outcomes. Behav Neurosci 115:443-454. (Pubitemid 32378173)
2. Bale TL, Contarino A, Smith GW, Chan R, Gold LH, Sawchenko PE, Koob GF, Vale WW, and Lee KF (2000) Mice deficient for corticotropin-releasing hormone receptor-2 display anxiety-like behaviour and are hypersensitive to stress. Nat Genet 24:410-414. (Pubitemid 30187443)
3. Bale TL, Picetti R, Contarino A, Koob GF, Vale WW, and Lee KF (2002) Mice deficient for both corticotropin-releasing factor receptor 1 (CRFR1) and CRFR2 have an impaired stress response and display sexually dichotomous anxiety-like behavior. J Neurosci 22:193-199. (Pubitemid 34033497)
4. Bale TL and ValeWW(2004) CRF and CRF receptors: role in stress responsivity and other behaviors. Annu Rev Pharmacol Toxicol 44:525-557. (Pubitemid 38263852)
5. Binneman B, Feltner D, Kolluri S, Shi Y, Qiu R, and Stiger T (2008) A 6-week randomized, placebo-controlled trial of CP-316,311 (a selective CRH1 antagonist) in the treatment of major depression. Am J Psychiatry 165:617-620. (Pubitemid 351705339)
6. Bohs C, Cregor M, Gunaratna G, and Kissinger C (2000) Culex automated blood sampler. Part II. Managing freely-moving animals and monitoring their activity. Curr Sep 18:147-151.
7. Carballeira A, Fishman LM, and Jacobi JD (1976) Dual sites of inhibition by metyrapone of human adrenal steroidogenesis: correlation of in vivo and in vitro studies. J Clin Endocrinol Metab 42:687-695.
8. Coric V, Feldman HH, Oren DA, Shekhar A, Pultz J, Dockens RC, Wu X, Gentile KA, Huang SP, Emison E, et al. (2010) Multicenter, randomized, double-blind, active comparator and placebo-controlled trial of a corticotropin-releasing factor receptor-1 antagonist in generalized anxiety disorder. Depress Anxiety 27:417-425.
9. 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. (Pubitemid 30187442)
10. Gehlert DR, Cippitelli A, Thorsell A, Lê AD, Hipskind PA, Hamdouchi C, Lu J, Hembre EJ, Cramer J, Song M, et al. (2007) 3-(4-Chloro-2-morpholin-4- yl-thiazol-5-yl)-8-(1-ethylpropyl)-2,6-dimethyl-imidazo[1,2-b]pyridazine: a novel brain-penetrant, orally available corticotropin-releasing factor receptor 1 antagonist with efficacy in animal models of alcoholism. J Neurosci 27:2718-2726. (Pubitemid 46393604)
11. Gehlert DR, Shekhar A, Morin SM, Hipskind PA, Zink C, Gackenheimer SL, Shaw J, Fitz SD, and 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. (Pubitemid 40282587)
12. Goren HJ, Kulkarni RN, and Kahn CR (2004) Glucose homeostasis and tissue transcript content of insulin signaling intermediates in four inbred strains of mice: C57BL/6, C57BLKS/6, DBA/2, and 129X1. Endocrinology 145:3307-3323. (Pubitemid 38830003)
13. Gully D, Geslin M, Serva L, Fontaine E, Roger P, Lair C, Darre V, Marcy C, Rouby PE, Simiand J, et al. (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 factor1 receptor antagonist. I. Biochemical and pharmacological characterization. J Pharmacol Exp Ther 301:322-332. (Pubitemid 34250311)
14. Gutman DA, Owens MJ, Skelton KH, Thrivikraman KV, and 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. (Pubitemid 36152368)
15. Hashimoto K, Nishiyama M, Tanaka Y, Noguchi T, Asaba K, Hossein PN, Nishioka T, and Makino S (2004) Urocortins and corticotropin releasing factor type 2 receptors in the hypothalamus and the cardiovascular system. Peptides 25:1711-1721. (Pubitemid 39346213)
16. Heinrichs SC, De Souza EB, Schulteis G, Lapsansky JL, and Grigoriadis DE (2002) Brain penetrance, receptor occupancy and antistress in vivo efficacy of a small molecule corticotropin releasing factor type I receptor selective antagonist. Neuropsychopharmacology 27:194-202. (Pubitemid 34686971)
17. Held K, Künzel H, Ising M, Schmid DA, Zobel A, Murck H, Holsboer F, and Steiger A (2004) Treatment with the CRH1-receptor-antagonist R121919 improves sleep-EEG in patients with depression. J Psychiatr Res 38:129-136. (Pubitemid 38134453)
18. Holsboer F (2000) The corticosteroid receptor hypothesis of depression. Neuropsychopharmacology 23:477-501.
19. Institute of Laboratory Animal Resources (1996) Guide for the Care and Use of Laboratory Animals, 7th ed, Institute of Laboratory Animal Resources, Commission on Life Sciences, National Research Council, Washington DC.
20. Ising M, Zimmermann US, Künzel HE, Uhr M, Foster AC, Learned-Coughlin SM, Holsboer F, and Grigoriadis DE (2007) High-affinity CRF1 receptor antagonist NBI-34041: preclinical and clinical data suggest safety and efficacy in attenuating elevated stress response. Neuropsychopharmacology 32:1941-1949. (Pubitemid 47258521)
21. Jamieson PM, Li C, Kukura C, Vaughan J, and ValeW(2006) Urocortin 3 modulates the neuroendocrine stress response and is regulated in rat amygdala and hypothalamus by stress and glucocorticoids. Endocrinology 147:4578-4588. (Pubitemid 44402163)
22. Kehne J and De Lombaert S (2002) Non-peptidic CRF1 receptor antagonists for the treatment of anxiety, depression and stress disorders. Curr Drug Targets CNS Neurol Disord 1:467-493.
23. Koob G and Kreek MJ (2007) Stress, dysregulation of drug reward pathways, and the transition to drug dependence. Am J Psychiatry 164:1149-1159. (Pubitemid 47292402)
24. Marinelli PW, Funk D, Juzytsch W, Harding S, Rice KC, Shaham Y, and Lê AD (2007) The CRF1 receptor antagonist antalarmin attenuates yohimbine-induced increases in operant alcohol self-administration and reinstatement of alcohol seeking in rats. Psychopharmacology (Berl) 195:345-355. (Pubitemid 350160269)
25. Müller MB, Zimmermann S, Sillaber I, Hagemeyer TP, Deussing JM, Timpl P, Kormann MS, Droste SK, Kuhn R, Reul JM, et al. (2003) Limbic corticotropin-releasing hormone receptor 1 mediates anxiety-related behavior and hormonal adaptation to stress. Nat Neurosci 6:1100-1107. (Pubitemid 37186203)
26. Muret L, Priou A, Oliver C, and Grino M (1992) Stimulation of adrenocorticotropin secretion by insulin-induced hypoglycemia in the developing rat involves arginine vasopressin but not corticotropin-releasing factor. Endocrinology 130:2725-2732.
27. Nielsen DM (2006) Corticotropin-releasing factor type-1 receptor antagonists: the next class of antidepressants? Life Sci 78:909-919.
28. Peters S, Hampsch J, Cregor M, Starrett C, Gunaratna G, and Kissinger C (2000) Culex ABS. I. Introduction to automated blood sampling. Curr Sep 18:139-145.
29. Pinnock SB and Herbert J (2001) Corticosterone differentially modulates expression of corticotropin releasing factor and arginine vasopressin mRNA in the hypothalamic paraventricular nucleus following either acute or repeated restraint stress. Eur J Neurosci 13:576-584. (Pubitemid 32158791)
30. Preil J, Müller MB, Gesing A, Reul JM, Sillaber I, van Gaalen MM, Landgrebe J, Holsboer F, Stenzel-Poore M, and WurstW(2001) Regulation of the hypothalamic-pituitary-adrenocortical system in mice deficient for CRH receptors 1 and 2. Endocrinology 142:4946-4955. (Pubitemid 33022371)
31. 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. (Pubitemid 28293127)
32. Sommer WH, Rimondini R, Hansson AC, Hipskind PA, Gehlert DR, Barr CS, and Heilig MA (2008) Upregulation of voluntary alcohol intake, behavioral sensitivity to stress, and amygdala crhr1 expression following a history of dependence. Biol Psychiatry 63:139-145. (Pubitemid 350299311)
33. Song C, Earley B, and Leonard BE (1995) Behavioral, neurochemical, and immuno-logical responses to CRF administration. Is CRF a mediator of stress? Ann NY Acad Sci 771:55-72.
34. Spindel E, Griffith L, and Wurtman RJ (1983) Neuroendocrine effects of caffeine. II. Effects on thyrotropin and corticosterone secretion. J Pharmacol Exp Ther 225: 346-350. (Pubitemid 13091222)
35. Timpl P, Spanagel R, Sillaber I, Kresse A, Reul JM, Stalla GK, Blanquet V, Steckler T, Holsboer F, and Wurst W (1998) Impaired stress response and reduced anxiety in mice lacking a functional corticotropin-releasing hormone receptor 1. Nat Genet 19:162-166. (Pubitemid 28248798)
36. Vale W, Spiess J, Rivier C, and Rivier J (1981) Characterization of a 41-residue ovine hypothalamic peptide that stimulates secretion of corticotropin and β-endorphin. Science 213:1394-1397. (Pubitemid 12243637)
37. Zgombick JM and Erwin VG (1988) Ethanol differentially enhances adrenocortical response in LS and SS mice. Alcohol 5:287-294. (Pubitemid 19263832)
38. Zobel AW, Nickel T, Künzel HE, Ackl N, Sonntag A, Ising M, and 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. (Pubitemid 30364916)