INT140887

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Context Info
Confidence 0.34
First Reported 2007
Last Reported 2007
Negated 0
Speculated 0
Reported most in Body
Documents 2
Total Number 6
Disease Relevance 0.26
Pain Relevance 1.22

This is a graph with borders and nodes. Maybe there is an Imagemap used so the nodes may be linking to some Pages.

plasma membrane (CRHR1) signal transducer activity (CRHR1)
Anatomy Link Frequency
face 1
CRHR1 (Homo sapiens)
Pain Link Frequency Relevance Heat
antagonist 152 100.00 Very High Very High Very High
agonist 70 100.00 Very High Very High Very High
Serotonin 4 79.52 Quite High
depression 10 59.60 Quite High
spastic colon 6 35.52 Quite Low
Migraine 5 5.00 Very Low Very Low Very Low
Potency 5 5.00 Very Low Very Low Very Low
Disease Link Frequency Relevance Heat
Carcinoid 1 81.40 Quite High
Anxiety Disorder 10 60.08 Quite High
Depression 10 59.60 Quite High
Stress 26 54.84 Quite High
Sensation Disorders 1 38.00 Quite Low
Functional Bowel Disorder 6 35.52 Quite Low
Diabetes Mellitus 10 5.00 Very Low Very Low Very Low
Disease 10 5.00 Very Low Very Low Very Low
Hyperglycemia 10 5.00 Very Low Very Low Very Low
Hypercalcemia 5 5.00 Very Low Very Low Very Low

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
The CRF1/2 ligand, rat/human (r/h)CRF (EC50 = 233 nM), and the selective CRF2 ligand, human urocortin 3 (Ucn 3) (EC50 = 48 nM), induced a dose-dependent increase in cAMP formation.
CRF1 Binding (induced) of
1) Confidence 0.34 Published 2007 Journal Biochem. Pharmacol. Section Abstract Doc Link 17184738 Disease Relevance 0.08 Pain Relevance 0.20
In the first case, certain characteristics of nonpeptide antagonists of the CRF1 receptor could potentially be explained by both mechanisms; nonpeptide antagonists only partially inhibit peptide ligand binding, and peptides only partially inhibit radiolabeled nonpeptide ligand binding [37].
CRF1 receptor Binding (binding) of associated with antagonist
2) Confidence 0.13 Published 2007 Journal Current Neuropharmacology Section Body Doc Link PMC2656815 Disease Relevance 0 Pain Relevance 0.10
Binding of a radiolabeled amino-terminal-truncated peptide ([125I] astressin, a CRF(12-41) analogue) to the wild-type CRF1 receptor is not appreciably inhibited by nonpeptide ligands [37, 38, 64], and nonpeptide antagonists completely block CRF-stimulated activation of a J-domain fragment [38, 59].
CRF1 receptor Binding (Binding) of associated with antagonist
3) Confidence 0.12 Published 2007 Journal Current Neuropharmacology Section Body Doc Link PMC2656815 Disease Relevance 0 Pain Relevance 0.21
Binding of peptide agonists to the CRF1 receptor is well-described by the two domain model described above and illustrated schematically in Fig. (1A) [25, 38, 64].
CRF1 receptor Binding (Binding) of associated with agonist
4) Confidence 0.12 Published 2007 Journal Current Neuropharmacology Section Body Doc Link PMC2656815 Disease Relevance 0 Pain Relevance 0.20
Taken together these findings suggest CRF1 receptor nonpeptide antagonists bind within the membrane-spanning region of the J-domain and peptide ligands bind to sites further towards the extracellular face of the receptor, implying allostetric interaction between peptide and nonpeptide ligand.
CRF1 receptor Binding (bind) of in face associated with antagonist
5) Confidence 0.12 Published 2007 Journal Current Neuropharmacology Section Body Doc Link PMC2656815 Disease Relevance 0.17 Pain Relevance 0.29
Radioligand binding studies are consistent with an allosteric interaction between nonpeptide antagonist and peptide ligands at the CRF1 receptor [37, 91].
CRF1 receptor Binding (interaction) of associated with antagonist
6) Confidence 0.12 Published 2007 Journal Current Neuropharmacology Section Body Doc Link PMC2656815 Disease Relevance 0 Pain Relevance 0.22

General Comments

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