INT63104

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Context Info
Confidence 0.37
First Reported 1995
Last Reported 2010
Negated 0
Speculated 1
Reported most in Abstract
Documents 29
Total Number 33
Disease Relevance 13.62
Pain Relevance 12.42

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

protein transporter activity (CALCRL) endosome (CALCRL) endoplasmic reticulum (CALCRL)
plasma membrane (CALCRL) lysosome (CALCRL) signal transducer activity (CALCRL)
Anatomy Link Frequency
hypothalamus 3
platelet 2
lymphocyte 2
plasma 1
sensory neurons 1
CALCRL (Homo sapiens)
Pain Link Frequency Relevance Heat
agonist 80 100.00 Very High Very High Very High
antagonist 46 100.00 Very High Very High Very High
opioid receptor 38 100.00 Very High Very High Very High
Potency 14 100.00 Very High Very High Very High
chemokine 5 100.00 Very High Very High Very High
gABA 20 99.96 Very High Very High Very High
Cholecystokinin 3 99.94 Very High Very High Very High
Chronic pancreatitis 41 99.92 Very High Very High Very High
Morphine 35 99.78 Very High Very High Very High
b2 receptor 7 99.76 Very High Very High Very High
Disease Link Frequency Relevance Heat
Pancreatitis 72 99.92 Very High Very High Very High
Malignant Neoplastic Disease 48 99.14 Very High Very High Very High
Fever 8 99.12 Very High Very High Very High
Cancer 361 99.00 Very High Very High Very High
Hypercalcemia 33 98.88 Very High Very High Very High
Increased Venous Pressure Under Development 5 98.68 Very High Very High Very High
Pain 18 98.48 Very High Very High Very High
Thyroid Neoplasm 676 98.28 Very High Very High Very High
Leukemia 6 98.24 Very High Very High Very High
INFLAMMATION 73 98.12 Very High Very High Very High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
GABA(A) receptor blockade in dorsomedial and ventromedial nuclei of the hypothalamus evokes panic-like elaborated defensive behaviour followed by innate fear-induced antinociception.
Negative_regulation (blockade) of ) receptor in hypothalamus associated with antinociception, gaba and anxiety disorder
1) Confidence 0.37 Published 2009 Journal Brain Res. Section Title Doc Link 19799880 Disease Relevance 0.49 Pain Relevance 0.41
The escape responses organized by the dorsomedial and ventromedial hypothalamic nuclei were characteristically more elaborated, and a remarkable exploratory behaviour was recorded during GABA(A) receptor blockade in the medial hypothalamus.
Negative_regulation (blockade) of ) receptor in hypothalamus associated with gaba
2) Confidence 0.37 Published 2009 Journal Brain Res. Section Abstract Doc Link 19799880 Disease Relevance 0.53 Pain Relevance 0.46
Androgen deprivation may be achieved with: a. orchidectomy, b. exogenous oestrogen administration, c. drugs with the capacity to deplete the hypothalamus of luteinizing hormone-releasing hormone, d. antiandrogens administration: drugs, which block the conversion of testosterone to its active form of 5-alpha dihydrotestosterone (i.e. finasteride, dutasteride), and drugs which block the androgen receptor on individual cells (i.e. flutamide).
Negative_regulation (block) of receptor in hypothalamus
3) Confidence 0.25 Published 2007 Journal Histol. Histopathol. Section Abstract Doc Link 17128417 Disease Relevance 0.55 Pain Relevance 0.08
The sensory experience evoked by lipid was diminished by both topical mucosal anaesthesia and CCK-A receptor blockade.
Negative_regulation (blockade) of receptor associated with cholecystokinin
4) Confidence 0.24 Published 1998 Journal DTW. Dtsch. Tierarztl. Wochenschr. Section Abstract Doc Link 9932012 Disease Relevance 0.48 Pain Relevance 0.41
A domain of the h5-HT1D receptor encompassing the second extracellular loop and the fifth transmembrane domain is necessary and sufficient to promote higher affinity binding (Ki = 65-115 nM) for ketanserin to the h5-HT1B receptor.
Negative_regulation (domain) of receptor
5) Confidence 0.16 Published 1998 Journal Mol. Pharmacol. Section Abstract Doc Link 9855638 Disease Relevance 0.08 Pain Relevance 0.40
With the exception of caecum, the delta 2 opioid receptor agonist deltorphin II was a potent inhibitor in human colonic circular muscle. 10(-8) M Deltorphin caused a 74.4 +/- 9.6% (n = 4) inhibition which was reversed by 10(-6) M of delta receptor selective peptide antagonist BOC-Tyr-Pro-Gly-Phe-Leu-Thr(OtBu).
Negative_regulation (inhibitor) of receptor in muscle associated with antagonist, agonist and opioid receptor
6) Confidence 0.08 Published 2000 Journal J. Physiol. Paris Section Abstract Doc Link 10791695 Disease Relevance 0 Pain Relevance 0.58
In vitro studies in cells transfected with exaggerated receptor numbers can lead to unreliable estimates of agonist and antagonist activity, however, these studies suggest that animal experiments on the activity of novel compounds may not always be better predictors of the ultimate activity in humans.
Negative_regulation (numbers) of receptor associated with antagonist and agonist
7) Confidence 0.05 Published 2000 Journal Peptides Section Abstract Doc Link 10998550 Disease Relevance 0 Pain Relevance 0.32
Bradyzide is a potent antagonist at the rat B2 receptor, but a weak one at the human receptor; a series of analogues in which the diphenylmethyl moiety of this drug has been substituted with dibenzosuberane have been reported to gain potency at the human B2 receptor, with some loss of affinity at the rat receptor.
Negative_regulation (loss) of receptor associated with antagonist, b2 receptor, bradyzide and potency
8) Confidence 0.03 Published 2003 Journal Int. Immunopharmacol. Section Abstract Doc Link 12946450 Disease Relevance 0.08 Pain Relevance 0.82
More recently, the accumulating evidence suggesting that B(1) receptor blockade could be useful for the treatment of pain and inflammatory disorders has led to a shift in drug development efforts toward the synthesis of orally bioavailable nonpeptide B(1) receptor antagonists.
Negative_regulation (blockade) of receptor associated with pain, inflammation and antagonist
9) Confidence 0.03 Published 2006 Journal Curr Top Med Chem Section Abstract Doc Link 16918454 Disease Relevance 0.28 Pain Relevance 0.27
CaR, calcium sensing receptor; CASR, calcium receptor gene; CP, chronic pancreatitis; FHH, familial hypocalciuric hypercalcemia; HP, hereditary pancreatitis; ICP, idiopathic chronic pancreatitis; PRSS1; cationic trypsinogen gene; SPINK1, serine protease inhibitor Kazal type 1 gene.


Negative_regulation (gene) of receptor associated with pancreatitis, hypercalcemia and chronic pancreatitis
10) Confidence 0.03 Published 2003 Journal BMC Gastroenterol Section Body Doc Link PMC317302 Disease Relevance 1.56 Pain Relevance 0.89
As receptor diffusion influences postsynaptic receptor numbers on a time scale of minutes, postsynaptic responsiveness may change very rapidly.
Negative_regulation (numbers) of receptor
11) Confidence 0.02 Published 2008 Journal Frontiers in Molecular Neuroscience Section Body Doc Link PMC2526001 Disease Relevance 0.07 Pain Relevance 0.33
Several publications then showed that other neurotransmitter receptors, such as GABAA receptors (Bogdanov et al., 2006) and ionotropic glutamate receptors (Borgdorff and Choquet, 2002), are also mobile within the neuronal plasma membrane, providing a basis for dynamic activity-dependent regulation of postsynaptic receptor numbers.
Negative_regulation (numbers) of receptor in plasma associated with neurotransmitter and glutamate receptor
12) Confidence 0.02 Published 2008 Journal Frontiers in Molecular Neuroscience Section Body Doc Link PMC2526001 Disease Relevance 0 Pain Relevance 0.33
We observed a reduced OT receptor concentration in advanced labour and after OT infusion, which suggests that OT influences its own receptor.
Negative_regulation (reduced) of receptor
13) Confidence 0.01 Published 1995 Journal Adv. Exp. Med. Biol. Section Abstract Doc Link 8714023 Disease Relevance 0.15 Pain Relevance 0.22
Importantly the study was a proof of principle as levels of soluble VEGF receptor were consistently decreased and levels of VEGF in the blood were increased demonstrating pharmacodynamic activity against targeted VEGF receptors [132, 133].


Negative_regulation (decreased) of receptor in blood
14) Confidence 0.01 Published 2010 Journal Journal of Thyroid Research Section Body Doc Link PMC2956973 Disease Relevance 1.06 Pain Relevance 0
Gefitinib (Iressa) is a tyrosine kinase inhibitor of the epidermal growth factor receptor (EGFR).
Negative_regulation (inhibitor) of receptor
15) Confidence 0.01 Published 2010 Journal Journal of Thyroid Research Section Body Doc Link PMC2956973 Disease Relevance 1.31 Pain Relevance 0.09
Unlike the other angiogenesis inhibitors such as bevacizumab, an antibody against VEGF, or the VEGF receptor kinase inhibitors, CA4P is a tubulin-binding vascular disrupting agent that stops blood flow through existing blood vessels, depriving the tumor of its nutrients and oxygen.
Negative_regulation (inhibitors) of receptor in blood vessels associated with cancer
16) Confidence 0.01 Published 2010 Journal Journal of Thyroid Research Section Body Doc Link PMC2956973 Disease Relevance 1.07 Pain Relevance 0
Chronic morphine treatment inhibits opioid receptor desensitization and internalization.
Negative_regulation (desensitization) of receptor associated with opioid receptor and morphine
17) Confidence 0.01 Published 2002 Journal J. Neurosci. Section Title Doc Link 12451120 Disease Relevance 0.16 Pain Relevance 1.30
Chronic morphine treatment inhibits opioid receptor desensitization and internalization.
Negative_regulation (inhibits) of receptor associated with opioid receptor and morphine
18) Confidence 0.01 Published 2002 Journal J. Neurosci. Section Title Doc Link 12451120 Disease Relevance 0.16 Pain Relevance 1.29
Since it contains the same active ingredient as ReoPro®, Clotinab™ is expected to have the same efficacy as ReoPro® as a platelet GP IIb/IIIa receptor inhibitor.
Negative_regulation (inhibitor) of receptor in platelet
19) Confidence 0.01 Published 2008 Journal Yonsei Medical Journal Section Body Doc Link PMC2615343 Disease Relevance 0.60 Pain Relevance 0.09
Each delta-opioid receptor agonist tested down-regulated the full-length receptor.
Negative_regulation (down-regulated) of receptor associated with agonist and opioid receptor
20) Confidence 0.01 Published 2003 Journal Eur. J. Pharmacol. Section Abstract Doc Link 12505529 Disease Relevance 0.05 Pain Relevance 0.87

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