CRF<sub>1</sub> receptor | Corticotropin-releasing factor receptors | IUPHAR/BPS Guide to PHARMACOLOGY

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CRF1 receptor

Target not currently curated in GtoImmuPdb

Target id: 212

Nomenclature: CRF1 receptor

Family: Corticotropin-releasing factor receptors

Annotation status:  image of a green circle Annotated and expert reviewed. Please contact us if you can help with updates.  » Email us

Gene and Protein Information
class B G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 415 17q21.31 CRHR1 corticotropin releasing hormone receptor 1 6,49
Mouse 7 415 11 E1 Crhr1 corticotropin releasing hormone receptor 1 49
Rat 7 415 10q32.1 Crhr1 corticotropin releasing hormone receptor 1 4,32
Previous and Unofficial Names
CRFR1 | CRF-R | CRHR | CRH-R1 | CRF-R1alpha | CRF 1 receptor | CRF-RA
Database Links
Specialist databases
GPCRDB crfr1_human (Hs), crfr1_mouse (Mm), crfr1_rat (Rn)
Other databases
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Extracellular domain of CRFR1in complex with CRF its natural ligand
PDB Id:  3EHU
Ligand:  corticotrophin-releasing hormone   This ligand is endogenous
Resolution:  1.96Å
Species:  Human
References:  34
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of human corticotropin-releasing factor receptor 1 (CRF1R) in complex with the antagonist CP-376395
PDB Id:  4K5Y
Ligand:  CP 376,395
Resolution:  2.98Å
Species:  Human
References:  22
Natural/Endogenous Ligands
corticotrophin-releasing hormone {Sp: Human, Mouse, Rat}
urocortin 2 {Sp: Human}
urocortin 1 {Sp: Human} , urocortin 1 {Sp: Mouse, Rat}

Download all structure-activity data for this target as a CSV file

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[125I]urocortin 1 (mouse, rat) Hs Full agonist 10.0 pKd 33
pKd 10.0 [33]
[125I]sauvagine (frog) Hs Full agonist 9.8 – 10.0 pKd 10,13
pKd 9.8 – 10.0 [10,13]
[125I]CRF (ovine) Hs Full agonist 9.5 pKd 6,9
pKd 9.5 [6,9]
[125I]Tyr0-CRF (human, rat, mouse) Hs Full agonist 9.3 pKd 13
pKd 9.3 [13]
urocortin 1 {Sp: Human} Hs Full agonist 8.6 – 9.5 pKd 10,13-14
pKd 8.6 – 9.5 [10,13-14]
urocortin 1 {Sp: Mouse, Rat} Hs Full agonist 8.3 – 9.8 pKd 13-14,24,33,48
pKd 8.3 – 9.8 [13-14,24,33,48]
urotensin 1 (fish) Hs Full agonist 7.8 – 9.4 pKd 13,48
pKd 7.8 – 9.4 [13,48]
corticotrophin-releasing hormone {Sp: Human, Mouse, Rat} Hs Full agonist 7.1 – 9.0 pKd 6,9,13-14,31,48
pKd 7.1 – 9.0 [6,9,13-14,31,48]
corticotropin-releasing factor {Sp: Sheep} Hs Full agonist 7.2 – 8.9 pKd 9-10,13,31
pKd 7.2 – 8.9 [9-10,13,31]
sauvagine Hs Full agonist 6.7 – 9.2 pKd 9-10,13-14,33,48
pKd 6.7 – 9.2 [9-10,13-14,33,48]
urocortin 2 {Sp: Human} Hs Full agonist 5.3 – 5.4 pKd 10
pKd 5.3 – 5.4 [10]
Agonist Comments
See Table 1 in the 'introduction' for sequences similarities of the common endogenous ligands.

Ovine CRF is more selective than human/rat CRF.
For urocortin 1 no species differences have been identified thus far.

Agonist potencies:
CRF (ovine) (9.0-9.5); CRF (human) (9.0-9.5); urocortin 1 (human) (9.2-10); sauvagine (frog) (9.2-10)(units: pEC50).
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[125I]astressin Hs Antagonist 9.2 – 9.3 pKd 10,13
pKd 9.2 – 9.3 [10,13]
astressin Hs Antagonist 7.7 – 8.8 pKd 13,31,33
pKd 7.7 – 8.8 [13,31,33]
α-helical CRF Hs Antagonist 7.3 – 7.8 pKd 33
pKd 7.3 – 7.8 [33]
astressin Hs Antagonist 8.7 pKi 38
pKi 8.7 (Ki 2x10-9 M) [38]
SSR125543A Hs Antagonist 8.7 pKi 15
pKi 8.7 [15]
antalarmin Hs Antagonist 8.3 – 9.0 pKi 50
pKi 8.3 – 9.0 (Ki 5.01x10-9 – 1x10-9 M) [50]
DMP696 Hs Antagonist 8.3 – 9.0 pKi 18
pKi 8.3 – 9.0 (Ki 5.01x10-9 – 1x10-9 M) [18]
NBI27914 Hs Antagonist 8.3 – 9.0 pKi 5
pKi 8.3 – 9.0 (Ki 5x10-9 – 1x10-9 M) [5]
R121919 Hs Antagonist 8.3 – 9.0 pKi 52
pKi 8.3 – 9.0 (Ki 5x10-9 – 1x10-9 M) [52]
NBI-34041 Hs Antagonist 8.3 pKi 16
pKi 8.3 (Ki 5.1x10-9 M) [16]
verucerfont Hs Antagonist 8.2 pKi 45
pKi 8.2 (Ki 6.31x10-9 M) [45]
CP-316,311 Hs Antagonist 8.1 pKi 7
pKi 8.1 (Ki 8.5x10-9 M) [7]
Description: Antagonism of CRF-stimulated adenylate cyclase activity by the CRF1 receptor endogenously expressed in human IMR32 cells.
CP 154,526 Rn Antagonist 9.3 – 10.4 pIC50 26
pIC50 9.3 – 10.4 (IC50 5.1x10-10 – 3.9x10-11 M) [26]
astressin Hs Antagonist 9.1 pIC50 37
pIC50 9.1 (IC50 7.2x10-10 M) [37]
ONO-2333MS Hs Antagonist 8.4 pIC50 39
pIC50 8.4 (IC50 4x10-9 M) [39]
CP 376,395 Rn Antagonist 8.3 pIC50 8
pIC50 8.3 (IC50 5.01x10-9 M) [8]
CP-316,311 Rn Antagonist 8.2 pIC50 7
pIC50 8.2 (IC50 6.8x10-9 M) [7]
Description: In vitro binding to rat cortex.
pexacerfont Rn Antagonist 6.9 pIC50 27
pIC50 6.9 (IC50 1.29x10-7 M) [27]
Description: Antagonism of CRF-mediated ACTH production in rat pituitary cells.
CRA1000 Hs Antagonist 6.4 – 7.1 pIC50 3
pIC50 6.4 – 7.1 (IC50 3.98x10-7 – 7.94x10-8 M) [3]
pexacerfont Hs Antagonist 6.5 pIC50 27
pIC50 6.5 (IC50 3.4x10-7 M) [27]
Description: Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes.
astressin 2B Hs Antagonist <6.3 pIC50 37
pIC50 <6.3 (IC50 >5x10-7 M) [37]
View species-specific antagonist tables
Primary Transduction Mechanisms
Transducer Effector/Response
Gs family Adenylate cyclase stimulation
References:  1,4,6,9,28,30-32,35,49,51
Secondary Transduction Mechanisms
Transducer Effector/Response
Gq/G11 family Phospholipase C stimulation
Comments:  So far only conclusively shown for recombinant expression systems
References:  10,51
Tissue Distribution
Widespread distribution of CRF1 mRNA in neocortex, limbic structures, cerebellum and pituitary. In the periphery only limited expression in adrenal gland, testis, ovaries and skin.
Species:  Rat
Technique:  immunocytochemistry.
References:  29,36
Expression Datasets

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Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

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Functional Assays
COS-7 cells transiently transfected with CRF1.
Species:  Human
Tissue:  COS-7 cells.
Response measured:  increase of intracellular cAMP.
References:  32
HEK 293 cells stably transfected with CRF1.
Species:  Human
Tissue:  HEK 293 cells.
Response measured:  Increase of intracellular cAMP.
References:  9,13,31
Physiological Functions
Agonist-induced CRF1 receptor activation increases anxiety-like behavior in open field, elevated plus maze, and many other tests measuring forms of defensive behavior, Moreover, CRF1 receptor activation is both necessary and sufficient to define the behavioral stress response.
Species:  Human
Tissue:  Brain
References:  2,19-20,23,41-42,44,46
Activation of CRF1 receptors on anterior pituitary corticotropes by direct agonist administration or acute stress exposure rapidly increases ACTH secretion. Increases in circulating levels of ACTH then activate ACTH receptors in the adrenal cortex leading to release of glucorcorticoids.
Species:  Human
Tissue:  Pituitary
References:  11-12,17,42,46-47
CRF1 receptor activation mediates stress-induced stimulation of colonic secretory and motor function.
Species:  Rat
Tissue:  Colon
References:  43
Physiological Consequences of Altering Gene Expression
Less anxiety-like behavior in CRF1-deficient animals. ACTH and CORT levels reduced under stress conditions in these animals.
Species:  Mouse
Tissue: 
Technique:  Transgenesis.
References:  42,46
Less anxiety-like behavior in socially stressed rats after infusion of CRF1 antisense oligonucleotides when compared to control groups.
Species:  Rat
Tissue: 
Technique:  Antisense oligonucleotide.
References:  21,25
Phenotypes, Alleles and Disease Models Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Crhr1tm1Wrst Crhr1tm1Wrst/Crhr1tm1Wrst
either: (involves: 129P2/OlaHsd * 129P/Ola) or (involves: 129P2/OlaHsd * CD-1)
MGI:88498  MP:0008289 abnormal adrenal medulla morphology PMID: 9620773 
Crhr1tm1Klee Crhr1tm1Klee/Crhr1tm1Klee
involves: 129S4/SvJae * C57BL/6
MGI:88498  MP:0001362 abnormal anxiety-related response PMID: 11756502 
Crhr1tm1Klee|Crhr2tm1Klee Crhr1tm1Klee/Crhr1tm1Klee,Crhr2tm1Klee/Crhr2tm1Klee
involves: 129S4/SvJae * C57BL/6
MGI:88498  MGI:894312  MP:0001362 abnormal anxiety-related response PMID: 11756502 
Crhr1tm1Klee Crhr1tm1Klee/Crhr1tm1Klee
involves: 129S4/SvJae * C57BL/6
MGI:88498  MP:0005449 abnormal food intake PMID: 10919255 
Crhr1tm1Klee Crhr1tm1Klee/Crhr1tm1Klee
involves: 129S4/SvJae * C57BL/6
MGI:88498  MP:0003953 abnormal hormone level PMID: 9655498 
Crhr1tm1Klee|Crhr2tm1Klee Crhr1tm1Klee/Crhr1tm1Klee,Crhr2tm1Klee/Crhr2tm1Klee
involves: 129S4/SvJae * C57BL/6
MGI:88498  MGI:894312  MP:0003953 abnormal hormone level PMID: 11756502 
Crhr1tm1Wrst Crhr1tm1Wrst/Crhr1tm1Wrst
either: (involves: 129P2/OlaHsd * 129P/Ola) or (involves: 129P2/OlaHsd * CD-1)
MGI:88498  MP:0003953 abnormal hormone level PMID: 9620773 
Crhr1tm1Klee Crhr1tm1Klee/Crhr1tm1Klee
involves: 129S4/SvJae * C57BL/6
MGI:88498  MP:0001449 abnormal learning/ memory PMID: 10448190 
Crhr1tm1Klee Crhr1tm1Klee/Crhr1tm1Klee
involves: 129S4/SvJae * C57BL/6
MGI:88498  MP:0001175 abnormal lung morphology PMID: 9655498 
Crhr1tm1Klee Crhr1tm1Klee/Crhr1tm1Klee
involves: 129S4/SvJae * C57BL/6
MGI:88498  MP:0002270 abnormal respiratory alveoli morphology PMID: 9655498 
Crhr1tm1Klee Crhr1tm1Klee/Crhr1tm1Klee
involves: 129S4/SvJae * C57BL/6
MGI:88498  MP:0008294 abnormal zona fasciculata morphology PMID: 9655498 
Crhr1tm1Klee|Crhr2tm1Klee Crhr1tm1Klee/Crhr1tm1Klee,Crhr2tm1Klee/Crhr2tm1Klee
involves: 129S4/SvJae * C57BL/6
MGI:88498  MGI:894312  MP:0008294 abnormal zona fasciculata morphology PMID: 11756502 
Crhr1tm1Klee Crhr1tm1Klee/Crhr1tm1Klee
involves: 129S4/SvJae * C57BL/6
MGI:88498  MP:0000640 adrenal gland hypoplasia PMID: 11756502  9655498 
Crhr1tm1Klee|Crhr2tm1Klee Crhr1tm1Klee/Crhr1tm1Klee,Crhr2tm1Klee/Crhr2tm1Klee
involves: 129S4/SvJae * C57BL/6
MGI:88498  MGI:894312  MP:0000640 adrenal gland hypoplasia PMID: 11756502 
Crhr1tm1Wrst Crhr1tm1Wrst/Crhr1tm1Wrst
either: (involves: 129P2/OlaHsd * 129P/Ola) or (involves: 129P2/OlaHsd * CD-1)
MGI:88498  MP:0001987 alcohol preference PMID: 11988580 
Crhr1tm1Klee Crhr1tm1Klee/Crhr1tm1Klee
involves: 129S4/SvJae * C57BL/6
MGI:88498  MP:0001364 decreased anxiety-related response PMID: 10448190  9655498 
Crhr1tm2Wrst|Tg(Camk2a-cre)159Kln Crhr1tm2Wrst/Crhr1tm2Wrst,Tg(Camk2a-cre)159Kln/0
involves: 129S2/SvPas * C57BL/6
MGI:2176751  MGI:88498  MP:0001364 decreased anxiety-related response PMID: 12973355 
Crhr1tm1Wrst Crhr1tm1Wrst/Crhr1tm1Wrst
either: (involves: 129P2/OlaHsd * 129P/Ola) or (involves: 129P2/OlaHsd * CD-1)
MGI:88498  MP:0001364 decreased anxiety-related response PMID: 9620773 
Crhr1+|Crhr1tm1Wrst Crhr1tm1Wrst/Crhr1+
either: (involves: 129P2/OlaHsd * 129P/Ola) or (involves: 129P2/OlaHsd * CD-1)
MGI:88498  MP:0001364 decreased anxiety-related response PMID: 9620773 
Crhr1tm1Wrst Crhr1tm1Wrst/Crhr1tm1Wrst
either: (involves: 129P2/OlaHsd * 129P/Ola) or (involves: 129P2/OlaHsd * CD-1)
MGI:88498  MP:0009776 decreased behavioral withdrawal response PMID: 9620773 
Crhr1+|Crhr1tm1Wrst Crhr1tm1Wrst/Crhr1+
either: (involves: 129P2/OlaHsd * 129P/Ola) or (involves: 129P2/OlaHsd * CD-1)
MGI:88498  MP:0009776 decreased behavioral withdrawal response PMID: 9620773 
Crhr1tm2Wrst|Tg(Camk2a-cre)159Kln Crhr1tm2Wrst/Crhr1tm2Wrst,Tg(Camk2a-cre)159Kln/0
involves: 129S2/SvPas * C57BL/6
MGI:2176751  MGI:88498  MP:0001399 hyperactivity PMID: 12973355 
Crhr1tm2Wrst|Tg(Camk2a-cre)159Kln Crhr1tm2Wrst/Crhr1tm2Wrst,Tg(Camk2a-cre)159Kln/0
involves: 129S2/SvPas * C57BL/6
MGI:2176751  MGI:88498  MP:0001748 increased circulating adrenocorticotropin level PMID: 12973355 
Crhr1tm2Wrst|Tg(Camk2a-cre)159Kln Crhr1tm2Wrst/Crhr1tm2Wrst,Tg(Camk2a-cre)159Kln/0
involves: 129S2/SvPas * C57BL/6
MGI:2176751  MGI:88498  MP:0001745 increased circulating corticosterone level PMID: 12973355 
Crhr1tm2Wrst Crhr1tm2Wrst/Crhr1tm2Wrst
involves: 129S2/SvPas * C57BL/6
MGI:88498  MP:0002169 no abnormal phenotype detected PMID: 12973355 
Crhr1tm1Klee Crhr1tm1Klee/Crhr1tm1Klee
involves: 129S4/SvJae * C57BL/6
MGI:88498  MP:0002083 premature death PMID: 9655498 
Crhr1tm1Wrst Crhr1tm1Wrst/Crhr1tm1Wrst
either: (involves: 129P2/OlaHsd * 129P/Ola) or (involves: 129P2/OlaHsd * CD-1)
MGI:88498  MP:0002083 premature death PMID: 9620773 
Crhr1tm1Klee Crhr1tm1Klee/Crhr1tm1Klee
involves: 129S4/SvJae * C57BL/6
MGI:88498  MP:0001954 respiratory distress PMID: 9655498 
General Comments
A similar tissue distribution of CRF1 mRNA exists in rhesus monkey as in rodents.
Technique: Receptor autoradiography and immunocytochemistry.
Reference: [40]

References

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1. Arai M, Assil IQ, Abou-Samra AB. (2001) Characterization of three corticotropin-releasing factor receptors in catfish: a novel third receptor is predominantly expressed in pituitary and urophysis. Endocrinology., 142: 446-454. [PMID:11145609]

2. Bale TL, Vale WW. (2004) CRF and CRF receptors: role in stress responsivity and other behaviors. Annu Rev Pharmacol Toxicol., 44: 525-557. [PMID:14744257]

3. Chaki S, Okuyama S, Nakazato A, Kumagai T, Okubo T, Ikeda Y, Oshida Y, Hamajima Y, Tomisawa K. (1999) In vitro pharmacological profile of nonpeptide CRF1 receptor antagonists, CRA1000 and CRA1001. Eur. J. Pharmacol., 371 (2-3): 205-11. [PMID:10357258]

4. Chang CP, Pearse RV2nd, O'Connell S, Rosenfeld MG. (1993) Identification of a seven transmembrane helix receptor for corticotropin-releasing factor and sauvagine in mammalian brain. Neuron., 11: 1187-1195. [PMID:8274282]

5. Chen C, Dagnino R, De Souza EB, Grigoriadis DE, Huang CQ, Kim KI, Liu Z, Moran T, Webb TR, Whitten JP et al.. (1996) Design and synthesis of a series of non-peptide high-affinity human corticotropin-releasing factor1 receptor antagonists. J. Med. Chem., 39 (22): 4358-60. [PMID:8893829]

6. Chen R, Lewis KA, Perrin MH, Vale WW. (1993) Expression cloning of a human corticotropin-releasing-factor receptor. Proc Natl Acad Sci U S A., 90: 8967-8971. [PMID:7692441]

7. Chen YL, Braselton J, Forman J, Gallaschun RJ, Mansbach R, Schmidt AW, Seeger TF, Sprouse JS, Tingley 3rd FD, Winston E et al.. (2008) Synthesis and SAR of 2-aryloxy-4-alkoxy-pyridines as potent orally active corticotropin-releasing factor 1 receptor antagonists. J. Med. Chem., 51 (5): 1377-84. [PMID:18260619]

8. Chen YL, Obach RS, Braselton J, Corman ML, Forman J, Freeman J, Gallaschun RJ, Mansbach R, Schmidt AW, Sprouse JS et al.. (2008) 2-aryloxy-4-alkylaminopyridines: discovery of novel corticotropin-releasing factor 1 antagonists. J. Med. Chem., 51 (5): 1385-92. [PMID:18288792]

9. Dautzenberg FM, Dietrich K, Palchaudhuri MR, Spiess J. (1997) Identification of two corticotropin-releasing factor receptors from Xenopus laevis with high ligand selectivity: unusual pharmacology of the type 1 receptor. J Neurochem., 69: 1640-1649. [PMID:9326293]

10. Dautzenberg FM, Gutknecht E, Van der Linden I, Olivares-Reyes JA, Dürrenberger F, Hauger RL. (2004) Cell type specific calcium signaling by corticotropin-releasing factor type 1 (CRF1) and 2a (CRF2(a)) receptors: Gq coupling in human embryonic kidney 293 but not SK-N-MC neuroblastoma cells. Biochem Pharmacol., 68: 1833-1844. [PMID:15450949]

11. Dautzenberg FM, Hauger RL. (2002) The CRF peptide family and their receptors: yet more partners discovered. Trends Pharmacol Sci., 23: 71-77. [PMID:11830263]

12. Dautzenberg FM, Kilpatrick GJ, Hauger RL, Moreau J. (2001) Molecular biology of the CRH receptors-- in the mood. Peptides., 22: 753-760. [PMID:11337088]

13. Dautzenberg FM, Py-Lang G, Higelin J, Fischer C, Wright MB, Huber G. (2001) Different binding modes of amphibian and human corticotropin-releasing factor type 1 and type 2 receptors: evidence for evolutionary differences. J Pharmacol Exp Ther., 296: 113-120. [PMID:11123370]

14. Donaldson CJ, Sutton SW, Perrin MH, Corrigan AZ, Lewis KA, Rivier JE, Vaughan JM, Vale WW. (1996) Cloning and characterization of human urocortin. Endocrinology., 137: 2167-2170. [PMID:8612563]

15. 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 factor(1) receptor antagonist. I. Biochemical and pharmacological characterization. J. Pharmacol. Exp. Ther., 301 (1): 322-32. [PMID:11907190]

16. Guo Z, Tellew JE, Gross RS, Dyck B, Grey J, Haddach M, Kiankarimi M, Lanier M, Li BF, Luo Z et al.. (2005) Design and synthesis of tricyclic imidazo[4,5-b]pyridin-2-ones as corticotropin-releasing factor-1 antagonists. J. Med. Chem., 48 (16): 5104-7. [PMID:16078829]

17. Hauger RL, Dautzenberg FM. (1999) Regulation of the stress response by corticotropin-releasing factor receptors. In Physiology and Medicine. Edited by Conn PM, Freedman ME (Humana Press Inc.) 261-286. [ISBN:0896037250]

18. He L, Gilligan PJ, Zaczek R, Fitzgerald LW, McElroy J, Shen HS, Saye JA, Kalin NH, Shelton S, Christ D et al.. (2000) 4-(1,3-Dimethoxyprop-2-ylamino)-2,7-dimethyl-8-(2, 4-dichlorophenyl)pyrazolo[1,5-a]-1,3,5-triazine: a potent, orally bioavailable CRF(1) receptor antagonist. J. Med. Chem., 43 (3): 449-56. [PMID:10669572]

19. Heinrichs SC, De Souza EB. (1999) Corticotropin-releasing factor antagonists, binding-protein and receptors: implications for central nervous system disorders. Baillieres Best Pract Res Clin Endocrinol Metab., 13: 541-554. [PMID:10903813]

20. Heinrichs SC, Koob GF. (2004) Corticotropin-releasing factor in brain: a role in activation, arousal and affect regulation. J Pharmacol Exp Therap., 311: 427-440. [PMID:15297468]

21. Heinrichs SC, Lapsansky J, Lovenberg TW, De Souza EB, Chalmers DT. (1997) Corticotropin-releasing factor CRF1, but not CRF2, receptors mediate anxiogenic-like behavior. Regul Pept., 71: 15-21. [PMID:9299637]

22. Hollenstein K, Kean J, Bortolato A, Cheng RK, Doré AS, Jazayeri A, Cooke RM, Weir M, Marshall FH. (2013) Structure of class B GPCR corticotropin-releasing factor receptor 1. Nature, 499 (7459): 438-43. [PMID:23863939]

23. Kishimoto T, Radulovic J, Radulovic M, Line CR, Schrick C, Hooshmand F, Hermanson O, Rosenfeld MG, Spiess J. (2000) Abnormal adaptations to stress and impaired cardiovascular function in mice lacking corticotropin-releasing hormone receptor-2. Nat Genet., 24: 415-419. [PMID:10742107]

24. 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 U S A., 98: 7570-7575. [PMID:11416224]

25. Liebsch G, Landgraf R, Engelmann M, Lorscher P, Holsboer F. (1999) Differential behavioural effects of chronic infusion of CRH 1 and CRH 2 receptor antisense oligonucleotides into the rat brain. J Psychiatr Res., 33: 153-163. [PMID:10221747]

26. Lundkvist J, Chai Z, Teheranian R, Hasanvan H, Bartfai T, Jenck F, Widmer U, Moreau JL. (1996) A non peptidic corticotropin releasing factor receptor antagonist attenuates fever and exhibits anxiolytic-like activity. Eur. J. Pharmacol., 309 (2): 195-200. [PMID:8874139]

27. Mochizuki M, Kojima T, Kobayashi K, Kotani E, Ishichi Y, Kanzaki N, Nakagawa H, Okuda T, Kosugi Y, Yano T et al.. (2017) Discovery of 4-chloro-2-(2,4-dichloro-6-methylphenoxy)-1-methyl-7-(pentan-3-yl)-1H-benzimidazole, a novel CRF1 receptor antagonist. Bioorg. Med. Chem., 25 (5): 1556-1570. [PMID:28174066]

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Frank M. Dautzenberg, Dimitri E. Grigoriadis, Richard L. Hauger, Thomas Steckler, Wylie W. Vale.
Corticotropin-releasing factor receptors: CRF1 receptor. Last modified on 16/05/2019. Accessed on 20/08/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=212.