INT264847

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Context Info
Confidence 0.34
First Reported 2007
Last Reported 2011
Negated 2
Speculated 1
Reported most in Body
Documents 4
Total Number 6
Disease Relevance 1.88
Pain Relevance 2.87

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 (GRM1) nucleus (GRM1) signal transducer activity (GRM1)
Anatomy Link Frequency
brain 2
GRM1 (Homo sapiens)
Pain Link Frequency Relevance Heat
Glutamate receptor 28 100.00 Very High Very High Very High
agonist 75 99.42 Very High Very High Very High
Potency 15 98.40 Very High Very High Very High
antagonist 88 96.96 Very High Very High Very High
Glutamate 53 95.88 Very High Very High Very High
Analgesic 18 91.36 High High
nMDA receptor 4 90.40 High High
Cannabinoid receptor 18 87.40 High High
wide dynamic range 3 82.88 Quite High
Somatostatin 6 82.36 Quite High
Disease Link Frequency Relevance Heat
Hyperalgesia 5 98.46 Very High Very High Very High
Cognitive Disorder 12 94.96 High High
Neuropathic Pain 10 74.80 Quite High
Injury 6 72.20 Quite High
Nociception 17 71.40 Quite High
Neuroblastoma 6 71.36 Quite High
Headache 77 70.12 Quite High
Arthralgia 3 67.12 Quite High
Inflammatory Pain 3 64.88 Quite High
Pain 33 61.28 Quite High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
Taken together, the lack of separation between efficacy and side effects in pre-clinical models indicates that mGluR1 antagonism may not provide an adequate therapeutic window for the development of such antagonists as therapeutics in humans.


Gene_expression (antagonism) of mGluR1 associated with antagonist
1) Confidence 0.34 Published 2007 Journal Current Neuropharmacology Section Body Doc Link PMC2656819 Disease Relevance 0.53 Pain Relevance 0.87
This agent has been a useful tool to investigate the role of the mGluR1 subtype in vitro, however, its limited potency (only low micromolar IC50), its lack of bio-availability and brain penetration did not allow a broad use in vivo.
Spec (investigate) Gene_expression (role) of mGluR1 in brain associated with potency
2) Confidence 0.34 Published 2007 Journal Current Neuropharmacology Section Body Doc Link PMC2656819 Disease Relevance 0 Pain Relevance 0.26
Knoflach et al. [23] were the first to describe two chemical series, compounds 5, 6 and 7 (Fig. 3), capable to potently increase agonist-mediated responses in cells expressing the rat mGlu1 receptor and in rat brain tissues.
Gene_expression (expressing) of mGlu1 in brain associated with agonist
3) Confidence 0.31 Published 2007 Journal Current Neuropharmacology Section Body Doc Link PMC2656819 Disease Relevance 0.45 Pain Relevance 0.76
Interestingly, Grm1 is generally thought not to be present in BV2 cells, yet it was the only one that we significantly detected.
Neg (not) Gene_expression (present) of Grm1
4) Confidence 0.28 Published 2011 Journal BMC Genomics Section Body Doc Link PMC3024950 Disease Relevance 0.07 Pain Relevance 0.10
BV2 cells express only one Class C GPCR at a significant, albeit, low mRNA level: the metabotropic glutamate receptor, mGluR1 (Grm1).
Gene_expression (express) of Grm1 associated with glutamate receptor
5) Confidence 0.22 Published 2011 Journal BMC Genomics Section Body Doc Link PMC3024950 Disease Relevance 0.06 Pain Relevance 0.24
Metabotropic glutamate receptors, called mGluR, play an important modulating role on the hyperalgesic response; for some of them, like mGlu 4 and mGlu 6-8, positive, for others (mGlu1 and mGlu 5) negative.
Neg (negative) Gene_expression (negative) of mGlu1 associated with hyperalgesia and glutamate receptor
6) Confidence 0.13 Published 2009 Journal The Open Neurology Journal Section Body Doc Link PMC2771268 Disease Relevance 0.77 Pain Relevance 0.64

General Comments

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