464
Views
47
CrossRef citations to date
0
Altmetric
Reviews

Corticotropin releasing factor receptor antagonists for major depressive disorder

, &
Pages 519-535 | Published online: 14 Mar 2011

Bibliography

  • WHO Media centre, Mental and neurological disorders, Fact sheet N°265, 2001
  • Jacobi F, Wittchen HU, Holting C, Prevalence, co-morbidity and correlates of mental disorders in the general population: results from the German Health Interview and Examination Survey (GHS). Psychol Med 2004;34:597-611
  • Kessler RC. Epidemiology of women and depression. J Affect Disord 2003;74:5-13
  • Murray C, Lopez A. Summary: the global burden of disease: a comprehensive assessment of mortality and disability from diseases, injuries, and risk factors in 1990 and projected to 2020. Harvard School of Public Health on behalf of the World Health Organization and the World Bank. Harvard University Press, Cambridge; 1996
  • Trivedi MH, Rush AJ, Wisniewski SR, Evaluation of outcomes with citalopram for depression using measurement-based care in STAR*D: implications for clinical practice. Am J Psychiatry 2006;163:28-40
  • Kroenke K, West SL, Swindle R, Similar effectiveness of paroxetine, fluoxetine, and sertraline in primary care: a randomized trial. JAMA 2001;286:2947-55
  • Luo L, Rodriguez E, Jerbi K, Ten years of Nature Reviews Neuroscience: insights from the highly cited. Nat Rev Neurosci 2010;11:718-26
  • Uhr M, Tontsch A, Namendorf C, Polymorphisms in the drug transporter gene ABCB1 predict antidepressant treatment response in depression. Neuron 2008;57:203-9
  • van Rossum EF, Binder EB, Mayer M, Polymorphisms of the glucocorticoid receptor gene and major depression. Biol Psychiatry 2006;59:681-8
  • Binder EB, Salyakina D, Lichtner P, Polymorphisms in FKBP5 are associated with increased recurrence of depressive episodes and rapid response to antidepressant treatment. Nat Genet 2004;36:1319-25
  • Francis DD, Caldji C, Champagne F, The role of corticotropin-releasing factor – norepinephrine systems in mediating the effects of early experience on the development of behavioral and endocrine responses to stress. Biol Psychiatry 1999;46:1153-66
  • Heim C, Newport DJ, Mletzko T, The link between childhood trauma and depression: insights from HPA axis studies in humans. Psychoneuroendocrinology 2008;33:693-710
  • Holsboer F. The corticosteroid receptor hypothesis of depression. Neuropsychopharmacology 2000;23:477-501
  • Pacher P, Kohegyi E, Kecskemeti V, Current trends in the development of new antidepressants. Curr Med Chem 2001;8:89-100
  • Shelton RC. The dual-action hypothesis: does pharmacology matter? J Clin Psychiatry 2004;65:5-10
  • Holsboer F. The rationale for corticotropin-releasing hormone receptor (CRH-R) antagonists to treat depression and anxiety. J Psychiatr Res 1999;33:181-214
  • Schmidt MV, Trumbach D, Weber P, Individual stress vulnerability is predicted by short-term memory and AMPA receptor subunit ratio in the hippocampus. J Neurosci 2010;30:16949-58
  • Rivier J, Spiess J, Vale W. Characterization of rat hypothalamic corticotropin-releasing factor. Proc Natl Acad Sci USA 1983;80:4851-5
  • Gray TS. Amygdaloid CRF pathways. Role in autonomic, neuroendocrine, and behavioral responses to stress. Ann N Y Acad Sci 1993;697:53-60
  • Lehnert H, Schulz C, Dieterich K. Physiological and neurochemical aspects of corticotropin-releasing factor actions in the brain: the role of the locus coeruleus. Neurochem Res 1998;23:1039-52
  • Arborelius L, Owens MJ, Plotsky PM, The role of corticotropin-releasing factor in depression and anxiety disorders. J Endocrinol 1999;160:1-12
  • Smith SM, Vale WW. The role of the hypothalamic-pituitary-adrenal axis in neuroendocrine responses to stress. Dialogues Clin Neurosci 2006;8:383-95
  • Bale TL, Vale WW. CRF and CRF receptors: role in stress responsivity and other behaviors. Annu Rev Pharmacol Toxicol 2004;44:525-57
  • Heinrichs SC, Koob GF. Corticotropin-releasing factor in brain: a role in activation, arousal, and affect regulation. J Pharmacol Exp Ther 2004;311:427-40
  • Steckler T, Holsboer F. Corticotropin-releasing hormone receptor subtypes and emotion. Biol Psychiatry 1999;46:1480-508
  • Ising M, Kunzel HE, Binder EB, The combined dexamethasone/CRH test as a potential surrogate marker in depression. Prog Neuropsychopharmacol Biol Psychiatry 2005;29:1085-93
  • Pariante CM, Miller AH. Glucocorticoid receptors in major depression: relevance to pathophysiology and treatment. Biol Psychiatry 2001;49:391-404
  • Raison CL, Miller AH. When not enough is too much: the role of insufficient glucocorticoid signaling in the pathophysiology of stress-related disorders. Am J Psychiatry 2003;160:1554-65
  • Holsboer F, Muller OA, Doerr HG, ACTH and multisteroid responses to corticotropin-releasing factor in depressive illness: relationship to multisteroid responses after ACTH stimulation and dexamethasone suppression. Psychoneuroendocrinology 1984;9:147-60
  • Gold PW, Chrousos G, Kellner C, Psychiatric implications of basic and clinical studies with corticotropin-releasing factor. Am J Psychiatry 1984;141:619-27
  • Nemeroff CB, Widerlov E, Bissette G, Elevated concentrations of CSF corticotropin-releasing factor-like immunoreactivity in depressed patients. Science 1984;226:1342-4
  • Nemeroff CB, Owens MJ, Bissette G, Reduced corticotropin releasing factor binding sites in the frontal cortex of suicide victims. Arch Gen Psychiatry 1988;45:577-9
  • Hartline KM, Owens MJ, Nemeroff CB. Postmortem and cerebrospinal fluid studies of corticotropin-releasing factor in humans. Ann N Y Acad Sci 1996;780:96-105
  • Heuser I, Bissette G, Dettling M, Cerebrospinal fluid concentrations of corticotropin-releasing hormone, vasopressin, and somatostatin in depressed patients and healthy controls: response to amitriptyline treatment. Depress Anxiety 1998;8:71-9
  • Merali Z, Du L, Hrdina P, Dysregulation in the suicide brain: mRNA expression of corticotropin-releasing hormone receptors and GABA(A) receptor subunits in frontal cortical brain region. J Neurosci 2004;24:1478-85
  • Raadsheer FC, Hoogendijk WJ, Stam FC, Increased numbers of corticotropin-releasing hormone expressing neurons in the hypothalamic paraventricular nucleus of depressed patients. Neuroendocrinology 1994;60(4):436-44
  • Holsboer F, Ising M. Stress hormone regulation: biological role and translation into therapy. Annu Rev Psychol 2010;61:81-109
  • Holsboer F. Stress, hypercortisolism and corticosteroid receptors in depression: implications for therapy. J Affect Disord 2001;62:77-91
  • Nemeroff CB, Bissette G, Akil H, Neuropeptide concentrations in the cerebrospinal fluid of depressed patients treated with electroconvulsive therapy. Corticotrophin-releasing factor, beta-endorphin and somatostatin. Br J Psychiatry 1991;158:59-63
  • Holsboer F, Liebl R, Hofschuster E. Repeated dexamethasone suppression test during depressive illness. Normalisation of test result compared with clinical improvement. J Affect Disord 1982;4:93-101
  • Ising M, Horstmann S, Kloiber S, Combined dexamethasone/corticotropin releasing hormone test predicts treatment response in major depression – a potential biomarker? Biol Psychiatry 2007;62:47-54
  • Reul JM, Stec I, Soder M, Chronic treatment of rats with the antidepressant amitriptyline attenuates the activity of the hypothalamic-pituitary-adrenocortical system. Endocrinology 1993;133:312-20
  • de Kloet ER, Sibug RM, Helmerhorst FM, Stress, genes and the mechanism of programming the brain for later life. Neurosci Biobehav Rev 2005;29:271-81
  • Lewis K, Li C, Perrin MH, 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 2001;98:7570-5
  • Reyes TM, Lewis K, Perrin MH, 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 2001;98:2843-8
  • Hsu SY, Hsueh AJ. Human stresscopin and stresscopin-related peptide are selective ligands for the type 2 corticotropin-releasing hormone receptor. Nat Med 2001;7:605-11
  • Perrin MH, Vale WW. Corticotropin releasing factor receptors and their ligand family. Ann N Y Acad Sci 1999;885:312-28
  • Skelton KH, Owens MJ, Nemeroff CB. The neurobiology of urocortin. Regul Pept 2000;93:85-92
  • Vale W, Spiess J, Rivier C, Characterization of a 41-residue ovine hypothalamic peptide that stimulates secretion of corticotropin and beta-endorphin. Science 1981;213:1394-7
  • Perrin MH, Donaldson CJ, Chen R, Cloning and functional expression of a rat brain corticotropin releasing factor (CRF) receptor. Endocrinology 1993;133:3058-61
  • Chen R, Lewis KA, Perrin MH, Expression cloning of a human corticotropin-releasing-factor receptor. Proc Natl Acad Sci USA 1993;90:8967-71
  • Vamvakopoulos NC, Sioutopoulou TO. Human corticotropin-releasing hormone receptor gene (CRHR) is located on the long arm of chromosome 17 (17q12-qter). Chromosome Res 1994;2:471-3
  • Polymeropoulos MH, Torres R, Yanovski JA, The human corticotropin-releasing factor receptor (CRHR) gene maps to chromosome 17q12-q22. Genomics 1995;28:123-4
  • Chang CP, Pearse 2nd RV, O'Connell S, Identification of a seven transmembrane helix receptor for corticotropin-releasing factor and sauvagine in mammalian brain. Neuron 1993;11:1187-95
  • Vita N, Laurent P, Lefort S, Primary structure and functional expression of mouse pituitary and human brain corticotrophin releasing factor receptors. FEBS Lett 1993;335:1-5
  • Yu J, Xie LY, Abou-Samra AB. Molecular cloning of a type A chicken corticotropin-releasing factor receptor with high affinity for urotensin I. Endocrinology 1996;137:192-7
  • Dautzenberg FM, Dietrich K, Palchaudhuri MR, Identification of two corticotropin-releasing factor receptors from Xenopus laevis with high ligand selectivity: unusual pharmacology of the type 1 receptor. J Neurochem 1997;69:1640-9
  • Myers DA, Trinh JV, Myers TR. Structure and function of the ovine type 1 corticotropin releasing factor receptor (CRF1) and a carboxyl-terminal variant. Mol Cell Endocrinol 1998;144:21-35
  • McCarthy JR, Heinrichs SC, Grigoriadis DE. Recent advances with the CRF1 receptor: design of small molecule inhibitors, receptor subtypes and clinical indications. Curr Pharm Des 1999;5:289-315
  • Ross PC, Kostas CM, Ramabhadran TV. A variant of the human corticotropin-releasing factor (CRF) receptor: cloning, expression and pharmacology. Biochem Biophys Res Commun 1994;205:1836-42
  • Grammatopoulos DK, Dai Y, Randeva HS, 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 1999;13:2189-202
  • Hoare SR, Sullivan SK, Pahuja A, Conformational states of the corticotropin releasing factor 1 (CRF1) receptor: detection, and pharmacological evaluation by peptide ligands. Peptides 2003;24:1881-97
  • Hoare SR. Mechanisms of peptide and nonpeptide ligand binding to Class B G-protein-coupled receptors. Drug Discov Today 2005;10:417-27
  • Grigoriadis DE, Hoare SR, Lechner SM, Drugability of extracellular targets: discovery of small molecule drugs targeting allosteric, functional, and subunit-selective sites on GPCRs and ion channels. Neuropsychopharmacology 2009;34:106-25
  • Lederis K, Letter A, McMaster D, Complete amino acid sequence of urotensin I, a hypotensive and corticotropin-releasing neuropeptide from Catostomus. Science 1982;218:162-5
  • Montecucchi PC, Anastasi A, de Castiglione R, 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 1980;16:191-9
  • De Souza EB, Perrin MH, Rivier J, Corticotropin-releasing factor receptors in rat pituitary gland: autoradiographic localization. Brain Res 1984;296:202-7
  • Potter E, Sutton S, Donaldson C, Distribution of corticotropin-releasing factor receptor mRNA expression in the rat brain and pituitary. Proc Natl Acad Sci USA 1994;91:8777-81
  • Chalmers DT, Lovenberg TW, De Souza EB. 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 1995;15:6340-50
  • De Souza EB, Insel TR, Perrin MH, Corticotropin-releasing factor receptors are widely distributed within the rat central nervous system: an autoradiographic study. J Neurosci 1985;5:3189-203
  • Reul JM, Holsboer F. Corticotropin-releasing factor receptors 1 and 2 in anxiety and depression. Curr Opin Pharmacol 2002;2:23-33
  • Gehlert DR, Shekhar A, Morin SM, Stress and central Urocortin increase anxiety-like behavior in the social interaction test via the CRF1 receptor. Eur J Pharmacol 2005;509:145-53
  • Zambrowicz BP, Sands AT. Knockouts model the 100 best-selling drugs – will they model the next 100? Nat Rev Drug Discov 2003;2:38-51
  • Coste SC, Murray SE, Stenzel-Poore MP. Animal models of CRH excess and CRH receptor deficiency display altered adaptations to stress. Peptides 2001;22:733-41
  • Smith GW, Aubry JM, Dellu F, Corticotropin releasing factor receptor 1-deficient mice display decreased anxiety, impaired stress response, and aberrant neuroendocrine development. Neuron 1998;20:1093-102
  • Timpl P, Spanagel R, Sillaber I, Impaired stress response and reduced anxiety in mice lacking a functional corticotropin-releasing hormone receptor 1. Nat Genet 1998;19:162-6
  • Muller MB, Zimmermann S, Sillaber I, Limbic corticotropin-releasing hormone receptor 1 mediates anxiety-related behavior and hormonal adaptation to stress. Nat Neurosci 2003;6:1100-7
  • Coric V, Feldman HH, Oren DA, Multicenter, randomized, double-blind, active comparator and placebo-controlled trial of a corticotropin-releasing factor receptor-1 antagonist in generalized anxiety disorder. Depress Anxiety 2010;27:417-25
  • Sweetser S, Camilleri M, Linker Nord SJ, Do corticotropin releasing factor-1 receptors influence colonic transit and bowel function in women with irritable bowel syndrome? Am J Physiol Gastrointest Liver Physiol 2009;296:G1299-306
  • Tojo K, Abou-Samra AB. Corticotropin-releasing factor (CRF) stimulates 45Ca2+ uptake in the mouse corticotroph cell line AtT-20. Life Sci 1993;52:621-30
  • Kovalovsky D, Refojo D, Liberman AC, Activation and induction of NUR77/NURR1 in corticotrophs by CRH/cAMP: involvement of calcium, protein kinase A, and MAPK pathways. Mol Endocrinol 2002;16:1638-51
  • Hoare SR, Sullivan SK, Schwarz DA, Ligand affinity for amino-terminal and juxtamembrane domains of the corticotropin releasing factor type I receptor: regulation by G-protein and nonpeptide antagonists. Biochemistry 2004;43:3996-4011
  • Hoare SR, Brown BT, Santos MA, Single amino acid residue determinants of non-peptide antagonist binding to the corticotropin-releasing factor1 (CRF1) receptor. Biochem Pharmacol 2006;72:244-55
  • Liaw CW, Grigoriadis DE, Lovenberg TW, Localization of ligand-binding domains of human corticotropin-releasing factor receptor: a chimeric receptor approach. Mol Endocrinol 1997;11:980-5
  • Liaw CW, Grigoriadis DE, Lorang MT, Localization of agonist- and antagonist-binding domains of human corticotropin-releasing factor receptors. Mol Endocrinol 1997;11:2048-53
  • Hoare SR, Fleck BA, Gross RS, Allosteric ligands for the corticotropin releasing factor type 1 receptor modulate conformational states involved in receptor activation. Mol Pharmacol 2008;73:1371-80
  • Gross RS, Guo Z, Dyck B, Design and synthesis of tricyclic corticotropin-releasing factor-1 antagonists. J Med Chem 2005;48:5780-93
  • Saunders J, Williams J. Antagonists of the corticotropin releasing factor receptor. Prog Med Chem 2003;41:195-247
  • Steckler T, Dautzenberg FM. Corticotropin-releasing factor receptor antagonists in affective disorders and drug dependence – an update. CNS Neurol Disord Drug Targets 2006;5:147-65
  • Valdez GR. Development of CRF1 receptor antagonists as antidepressants and anxiolytics: progress to date. CNS Drugs 2006;20:887-96
  • Zorrilla EP, Koob GF. The therapeutic potential of CRF1 antagonists for anxiety. Expert Opin Investig Drugs 2004;13:799-828
  • Lanier M, Williams JP. Small molecule corticotropin-releasing factor antagonists. Expert Opin Ther Patents 2002;12:1619-30
  • Kehne JH, Cain CK. Therapeutic utility of non-peptidic CRF1 receptor antagonists in anxiety, depression, and stress-related disorders: evidence from animal models. Pharmacol Ther 2010;128:460-87
  • Grigoriadis DE. The corticotropin-releasing factor receptor: a novel target for the treatment of depression and anxiety-related disorders. Expert Opin Ther Targets 2005;9:651-84
  • Tellew JE, Luo Z. Small molecule antagonists of the corticotropin releasing factor (CRF) receptor: recent medicinal chemistry developments. Curr Top Med Chem 2008;8:506-20
  • Hemley CF, McCluskey A, Keller PA. Corticotropin releasing hormone – a GPCR drug target. Curr Drug Targets 2007;8:105-15
  • Zorrilla EP, Koob GF. Progress in corticotropin-releasing factor-1 antagonist development. Drug Discov Today 2010;15:371-83
  • Chen C, Wilcoxen KM, Huang CQ, Design of 2,5-dimethyl-3-(6-dimethyl-4-methylpyridin-3-yl)-7-dipropylaminopyrazolo[1,5-a]pyrimidine (NBI 30775/R121919) and structure–activity relationships of a series of potent and orally active corticotropin-releasing factor receptor antagonists. J Med Chem 2004;47:4787-98
  • Heinrichs SC, De Souza EB, Schulteis G, Brain penetrance, receptor occupancy and antistress in vivo efficacy of a small molecule corticotropin releasing factor type I receptor selective antagonist. Neuropsychopharmacology 2002;27:194-202
  • Held K, Kunzel H, Ising M, Treatment with the CRH1-receptor-antagonist R121919 improves sleep-EEG in patients with depression. J Psychiatr Res 2004;38:129-36
  • Kunzel HE, Zobel AW, Nickel T, Treatment of depression with the CRH-1-receptor antagonist R121919: endocrine changes and side effects. J Psychiatr Res 2003;37:525-33
  • Kunzel HE, Ising M, Zobel AW, Treatment with a CRH-1-receptor antagonist (R121919) does not affect weight or plasma leptin concentration in patients with major depression. J Psychiatr Res 2005;39:173-7
  • Zobel AW, Nickel T, Kunzel HE, Effects of the high-affinity corticotropin-releasing hormone receptor antagonist R121919 in major depression: the first 20 patients treated. J Psychiatr Res 2000;34:171-81
  • Hamilton M. Rating depressive patients. J Clin Psychiatry 1980;41:21-4
  • Kimura M, Muller-Preuss P, Lu A, Conditional corticotropin-releasing hormone overexpression in the mouse forebrain enhances rapid eye movement sleep. Mol Psychiatry 2010;15:154-65
  • Holsboer F, von Bardeleben U, Steiger A. Effects of intravenous corticotropin-releasing hormone upon sleep-related growth hormone surge and sleep EEG in man. Neuroendocrinology 1988;48:32-8
  • Chen YL, Braselton J, Forman J, Synthesis and SAR of 2-aryloxy-4-alkoxy-pyridines as potent orally active corticotropin-releasing factor 1 receptor antagonists. J Med Chem 2008;51:1377-84
  • Binneman B, Feltner D, Kolluri S, A 6-week randomized, placebo-controlled trial of CP-316,311 (a selective CRH1 antagonist) in the treatment of major depression. Am J Psychiatry 2008;165:617-20
  • Gilligan PJ, He L, Clarke T, 8-(4-Methoxyphenyl)pyrazolo[1,5-a]-1,3,5-triazines: selective and centrally active corticotropin-releasing factor receptor-1 (CRF1) antagonists. J Med Chem 2009;52:3073-83
  • Di Fabio R, St-Denis Y, Sabbatini FM, Synthesis and pharmacological characterization of novel druglike corticotropin-releasing factor 1 antagonists. J Med Chem 2008;51:7370-9
  • Tellew JE, Lanier M, Moorjani M, Discovery of NBI-77860/GSK561679, a potent corticotropin-releasing factor (CRF1) receptor antagonist with improved pharmacokinetic properties. Bioorg Med Chem Lett 2010;20:7259-64
  • Ising M, Zimmermann US, Kunzel HE, High-affinity CRF1 receptor antagonist NBI-34041: preclinical and clinical data suggest safety and efficacy in attenuating elevated stress response. Neuropsychopharmacology 2007;32:1941-9
  • Schmidt ME, Andrews RD, van der Ark P, Dose-dependent effects of the CRF(1) receptor antagonist R317573 on regional brain activity in healthy male subjects. Psychopharmacology (Berl) 2010;208:109-19
  • Gully D, Geslin M, Serva L, 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. I. Biochemical and pharmacological characterization. J Pharmacol Exp Ther 2002;301:322-32
  • Kehne J, De Lombaert S. Non-peptidic CRF1 receptor antagonists for the treatment of anxiety, depression and stress disorders. Curr Drug Targets CNS Neurol Disord 2002;1:467-93
  • Lu A, Steiner MA, Whittle N, Conditional mouse mutants highlight mechanisms of corticotropin-releasing hormone effects on stress-coping behavior. Mol Psychiatry 2008;13:1028-42
  • Licinio J, O'Kirwan F, Irizarry K, Association of a corticotropin-releasing hormone receptor 1 haplotype and antidepressant treatment response in Mexican-Americans. Mol Psychiatry 2004;9:1075-82
  • Lekman M, Laje G, Charney D, The FKBP5-gene in depression and treatment response – an association study in the Sequenced Treatment Alternatives to Relieve Depression (STAR*D) Cohort. Biol Psychiatry 2008;63:1103-10
  • Kirchheiner J, Lorch R, Lebedeva E, Genetic variants in FKBP5 affecting response to antidepressant drug treatment. Pharmacogenomics 2008;9:841-6
  • Horstmann S, Lucae S, Menke A, Polymorphisms in GRIK4, HTR2A, and FKBP5 show interactive effects in predicting remission to antidepressant treatment. Neuropsychopharmacology 2010;35:727-40
  • Scammell JG, Denny WB, Valentine DL, Overexpression of the FK506-binding immunophilin FKBP51 is the common cause of glucocorticoid resistance in three New World primates. Gen Comp Endocrinol 2001;124:152-65
  • Vermeer H, Hendriks-Stegeman BI, van der Burg B, Glucocorticoid-induced increase in lymphocytic FKBP51 messenger ribonucleic acid expresion: a potential marker for glucocorticoid sensitivity, potency, and bioavailability. J Clin Endocrinol Metab 2003;88:277-84
  • Patent application: WO/2010/015655; 2010
  • Patent application: WO/2008/022716; 2008
  • Kobilka B, Schertler GF. New G-protein-coupled receptor crystal structures: insights and limitations. Trends Pharmacol Sci 2008;29:79-83
  • Liu Z, Zhu F, Wang G, Association study of corticotropin-releasing hormone receptor1 gene polymorphisms and antidepressant response in major depressive disorders. Neurosci Lett 2007;414:155-8
  • Keck ME, Welt T, Wigger A, The anxiolytic effect of the CRH(1) receptor antagonist R121919 depends on innate emotionality in rats. Eur J Neurosci 2001;13:373-80
  • Li YW, Hill G, Wong H, Receptor occupancy of nonpeptide corticotropin-releasing factor 1 antagonist DMP696: correlation with drug exposure and anxiolytic efficacy. J Pharmacol Exp Ther 2003;305:86-96
  • Gutman DA, Owens MJ, Skelton KH, The corticotropin-releasing factor1 receptor antagonist R121919 attenuates the behavioral and endocrine responses to stress. J Pharmacol Exp Ther 2003;304:874-80
  • Gutman DA, Owens MJ, Thrivikraman KV, Persistent anxiolytic affects after chronic administration of the CRF(1) receptor antagonist R121919 in rats. Neuropharmacology 2010; In press
  • Chaki S, Nakazato A, Kennis L, Anxiolytic- and antidepressant-like profile of a new CRF1 receptor antagonist, R278995/CRA0450. Eur J Pharmacol 2004;485:145-58
  • Lelas S, Wong H, Li YW, 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 2004;309:293-302
  • Gehlert DR, Shekhar A, Morin SM, Stress and central Urocortin increase anxiety-like behavior in the social interaction test via the CRF1 receptor. Eur J Pharmacol 2005;509:145-53
  • Gehlert DR, Cippitelli A, Thorsell A, 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 2007;27:2718-26
  • Hsin LW, Webster EL, Chrousos GP, Synthesis and biological activity of fluoro-substituted pyrrolo[2,3-d]pyrimidines: the development of potential positron emission tomography imaging agents for the corticotropin-releasing hormone type 1 receptor. Bioorg Med Chem Lett 2000;10:707-10
  • Hsin LW, Tian X, Webster EL, CRHR1 receptor binding and lipophilicity of pyrrolopyrimidines, potential nonpeptide corticotropin-releasing hormone type 1 receptor antagonists. Bioorg Med Chem 2002;10:175-83
  • Martarello L, Kilts CD, Ely T, Synthesis and characterization of fluorinated and iodinated pyrrolopyrimidines as PET/SPECT ligands for the CRF1 receptor. Nucl Med Biol 2001;28:187-95
  • Kumar JS, Majo VJ, Prabhakaran J, Synthesis of [N-methyl-11C]-3-[(6-dimethylamino)pyridin-3-yl]-2,5-dimethyl-N, N-dipropylpyrazolo[1,5-a]pyrimidine-7-amine: a potential PET ligand for in vivo imaging of CRF1 receptors. J Label Compd Radiopharm 2003;46(11):1055-65
  • Kumar JS, Majo VJ, Simpson NR, Synthesis of [O-methyl-11C]-4-(1,3-dimethoxy-2-propylamino)-2,7-dimethyl-8-(2,4-dichlorophenyl)[1,5-a]pyrazolo-1,3,5-triazine ([11C]DMP696): a potential PET ligand for CRF1 receptors. J Label Compd Radiopharm 2004;47(13):971-6
  • Kumar JS, Majo VJ, Sullivan GM, Synthesis and in vivo evaluation of [11C]SN003 as a PET ligand for CRF1 receptors. Bioorg Med Chem 2006;14:4029-34
  • Sullivan GM, Parsey RV, Kumar JS, PET Imaging of CRF1 with [11C]R121920 and [11C]DMP696: is the target of sufficient density? Nucl Med Biol 2007;34:353-61

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.