INT6270

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Context Info
Confidence 0.47
First Reported 1989
Last Reported 2010
Negated 3
Speculated 0
Reported most in Abstract
Documents 55
Total Number 55
Disease Relevance 9.54
Pain Relevance 22.86

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 (HTR1D) signal transducer activity (HTR1D)
Anatomy Link Frequency
brain 4
cranial 2
caudate nucleus 1
ergots 1
central nervous system 1
HTR1D (Homo sapiens)
Pain Link Frequency Relevance Heat
Sumatriptan 214 100.00 Very High Very High Very High
agonist 103 100.00 Very High Very High Very High
Serotonin 41 100.00 Very High Very High Very High
Opioid 3 100.00 Very High Very High Very High
Migraine 139 99.46 Very High Very High Very High
antagonist 22 99.26 Very High Very High Very High
Potency 24 98.92 Very High Very High Very High
ergotamine 4 98.64 Very High Very High Very High
Triptan 39 97.54 Very High Very High Very High
Substantia nigra 13 97.08 Very High Very High Very High
Disease Link Frequency Relevance Heat
Eating Disorder 8 99.76 Very High Very High Very High
Cluster Headache 15 99.72 Very High Very High Very High
Nociception 2 99.62 Very High Very High Very High
Alcohol Addiction 123 99.46 Very High Very High Very High
Migraine Disorders 38 99.46 Very High Very High Very High
Headache 119 99.30 Very High Very High Very High
Epilepsy 3 98.72 Very High Very High Very High
Increased Venous Pressure Under Development 6 98.16 Very High Very High Very High
Autism 2 97.44 Very High Very High Very High
Glioma 3 96.24 Very High Very High Very High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
The present data show that GR 43175 interacts preferentially as an agonist with 5-HT1B and 5-HT1D receptors.
5-HT1D Binding (interacts) of associated with agonist
1) Confidence 0.47 Published 1989 Journal Naunyn Schmiedebergs Arch. Pharmacol. Section Abstract Doc Link 2552330 Disease Relevance 0.06 Pain Relevance 0.34
The clinical effective dose of ergotamine, beginning from the minimal dose of 1 mg, correlates well with its affinity for 5-HT1B and 5-HT1D receptors, and the rank order of clinical potency of ergotamine is superior to sumatriptan.
5-HT1D Binding (affinity) of in superior associated with sumatriptan, potency and ergotamine
2) Confidence 0.47 Published 1994 Journal Headache Section Abstract Doc Link 7928330 Disease Relevance 0.25 Pain Relevance 0.58
Sumatriptan displaced [3H]5-HT from frontal cortical and striatal membranes in a biphasic manner, with a high-affinity site corresponding to binding to the 5-HT1D receptor.
5-HT1D Binding (binding) of associated with sumatriptan
3) Confidence 0.47 Published 1993 Journal Neurosci. Lett. Section Abstract Doc Link 8152617 Disease Relevance 0 Pain Relevance 0.67
Evidence of impaired serotonergic innervation associated with alcoholism is also confirmed by less 5-HT1D terminal autoreceptor binding in alcoholics.
5-HT1D Binding (binding) of associated with alcohol addiction
4) Confidence 0.47 Published 2010 Journal International Journal of Environmental Research and Public Health Section Body Doc Link PMC2872355 Disease Relevance 1.08 Pain Relevance 0.23
Sumatriptan is an antimigraine agent, which interacts most potently with 5HT1D receptors.
5HT1D Binding (interacts) of associated with cluster headache and sumatriptan
5) Confidence 0.47 Published 1998 Journal Eur Neuropsychopharmacol Section Abstract Doc Link 9928925 Disease Relevance 0.44 Pain Relevance 0.47
Binding of O-alkyl derivatives of serotonin at human 5-HT1D beta receptors.
5-HT1D Binding (Binding) of associated with serotonin
6) Confidence 0.47 Published 1996 Journal J. Med. Chem. Section Title Doc Link 8568822 Disease Relevance 0.09 Pain Relevance 0.37
Examination of a series of 5-(alkyloxy)tryptamine derivatives demonstrated that compounds with unbranched alkyl groups of up to eight carbon atoms bind with high affinity at human 5-HT1D beta receptors (Ki < 5 nM) but demonstrate less than 50-fold selectivity relative to 5-HT1A receptors.
5-HT1D Binding (bind) of
7) Confidence 0.47 Published 1996 Journal J. Med. Chem. Section Abstract Doc Link 8568822 Disease Relevance 0.08 Pain Relevance 0.31
Naratriptan has high affinity for human recombinant 5HT1B and 5HT1D receptors (pKi = 8.7 +/- 0.03 and 8.3 +/- 0.1, respectively) and causes contractions of dog isolated basilar and middle cerebral artery (EC50 values of 0.11 and 0.07 microM, respectively).
5HT1D Binding (affinity) of in middle cerebral artery
8) Confidence 0.47 Published 1997 Journal Cephalalgia Section Abstract Doc Link 9170336 Disease Relevance 0.24 Pain Relevance 0.26
The efficacy of sumatriptan in migraine relief has been attributed to its interaction with 5-hydroxytryptamine1D (5-HT1D) receptors in cerebral blood vessels and/or on nerve endings of the trigeminovascular system in the dura mater.
5-HT1D Binding (interaction) of in nerve associated with sumatriptan and migraine
9) Confidence 0.47 Published 1996 Journal Mol. Pharmacol. Section Abstract Doc Link 8700126 Disease Relevance 0.10 Pain Relevance 0.36
Stable and separate transfection of a pcDNA3 or pRcRSV plasmid, each containing a cloned human 5-HT1D receptor gene, in rat C6-glial cells was confirmed with RT-PCR of 5-HT1D receptor mRNA and radioligand binding with [3H] 5-carboxamidotryptamine (5-CT) and [3H] sumatriptan.
5-HT1D Binding (binding) of in glial cells associated with sumatriptan
10) Confidence 0.47 Published 1996 Journal Naunyn Schmiedebergs Arch. Pharmacol. Section Abstract Doc Link 8717154 Disease Relevance 0 Pain Relevance 0.25
In the human brain sumatriptan binds to at least two 5-HT1 receptors, 5-HT1D and 5-HT1F.
5-HT1D Binding (binds) of in brain associated with sumatriptan
11) Confidence 0.47 Published 1996 Journal Eur. J. Pharmacol. Section Abstract Doc Link 8720594 Disease Relevance 0.09 Pain Relevance 0.58
Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors.
5-HT1D Binding (binding) of
12) Confidence 0.47 Published 1999 Journal Eur. J. Pharmacol. Section Title Doc Link 10193663 Disease Relevance 0.09 Pain Relevance 0.49
The only pharmacological property shared by both agents is high affinity for 5-HT1D and 5-HT1A receptors.
5-HT1D Binding (affinity) of
13) Confidence 0.47 Published 1989 Journal Headache Section Abstract Doc Link 2547733 Disease Relevance 0.10 Pain Relevance 0.43
These data indicate that sumatriptan interacts selectively with 5-HT1B and 5-HT1D sites and suggest that these interactions may be the basis of its apparent efficacy in the acute treatment of migraine.
5-HT1D Binding (interacts) of associated with sumatriptan and migraine
14) Confidence 0.47 Published 1989 Journal Eur. J. Pharmacol. Section Abstract Doc Link 2545459 Disease Relevance 0.10 Pain Relevance 0.57
Sumatriptan (GR 43175) interacts selectively with 5-HT1B and 5-HT1D binding sites.
5-HT1D Binding (interacts) of associated with sumatriptan
15) Confidence 0.47 Published 1989 Journal Eur. J. Pharmacol. Section Title Doc Link 2545459 Disease Relevance 0 Pain Relevance 0.57
These data indicate that 10(-5) M 5-HT should not be used to define specific binding to 5-HT1D receptors in radioligand binding assays.
5-HT1D Binding (binding) of
16) Confidence 0.47 Published 1991 Journal Brain Res. Section Abstract Doc Link 1657281 Disease Relevance 0 Pain Relevance 0.34
Eletriptan, like sumatriptan, zolmitriptan, naratriptan and rizatriptan had highest affinity for the human 5-HT1B, 5-HT1D and putative 5-ht1f receptor.
5-HT1D Binding (affinity) of associated with sumatriptan
17) Confidence 0.36 Published 1999 Journal Eur. J. Pharmacol. Section Abstract Doc Link 10193663 Disease Relevance 0.10 Pain Relevance 0.47
In contrast to the hypothesis, 5-alkyltryptamines all exhibit high binding affinities for the human 5-HT1D receptor.
5-HT1D Binding (affinities) of
18) Confidence 0.36 Published 1999 Journal J. Med. Chem. Section Abstract Doc Link 9986723 Disease Relevance 0 Pain Relevance 0.15
We demonstrated that alniditan is a potent agonist at h5-HT1D alpha and h5-HT1D beta receptors; its properties probably underlie its cranial vasoconstrictive and antimigraine properties.
5-HT1D Binding (underlie) of in cranial associated with cluster headache and agonist
19) Confidence 0.36 Published 1996 Journal Mol. Pharmacol. Section Abstract Doc Link 8967979 Disease Relevance 0.24 Pain Relevance 0.27
We further compared the properties of [3H]alniditan, as a new radioligand for 5-HT1D-type receptors, with those of [3H]5-HT in membrane preparations of calf substantia nigra, C6 glioma cells expressing h5-HT1D alpha, and L929 cells expressing h5-HT1D beta receptors. [3H]Alniditan revealed very rapid association and dissociation binding kinetics and showed slightly higher affinity (Kd = 1-2 nM) than [3H]5-HT.
5-HT1D Binding (radioligand) of in L929 associated with substantia nigra and glioma
20) Confidence 0.36 Published 1996 Journal Mol. Pharmacol. Section Abstract Doc Link 8967979 Disease Relevance 0.17 Pain Relevance 0.54

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