INT6594

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Context Info
Confidence 0.75
First Reported 1992
Last Reported 2010
Negated 2
Speculated 3
Reported most in Abstract
Documents 60
Total Number 66
Disease Relevance 10.15
Pain Relevance 27.13

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
ovary 6
trigeminal ganglia 4
HeLa 3
fibroblasts 2
blood vessels 2
HTR1D (Homo sapiens)
Pain Link Frequency Relevance Heat
Sumatriptan 521 100.00 Very High Very High Very High
Serotonin 84 100.00 Very High Very High Very High
adenocard 7 100.00 Very High Very High Very High
agonist 144 99.96 Very High Very High Very High
fifth nerve 4 99.84 Very High Very High Very High
noradrenaline 3 99.74 Very High Very High Very High
trigeminal ganglion 20 99.68 Very High Very High Very High
Substantia nigra 19 99.64 Very High Very High Very High
Periaqueductal grey 4 99.44 Very High Very High Very High
Central nervous system 7 99.36 Very High Very High Very High
Disease Link Frequency Relevance Heat
Cluster Headache 18 100.00 Very High Very High Very High
Glioma 39 99.86 Very High Very High Very High
Increased Venous Pressure Under Development 28 99.78 Very High Very High Very High
Ganglion Cysts 22 99.24 Very High Very High Very High
Headache 242 99.20 Very High Very High Very High
Pain 90 98.52 Very High Very High Very High
Cancer 4 97.28 Very High Very High Very High
Bordatella Infection 15 96.68 Very High Very High Very High
Neurogenic Inflammation 18 95.88 Very High Very High Very High
Urological Neuroanatomy 5 89.48 High High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
CHO K1 cells expressing the human serotonin 5-HT1D beta receptor were assayed to determine the second messenger system of this receptor.
Gene_expression (expressing) of 5-HT1D associated with serotonin
1) Confidence 0.75 Published 1992 Journal Eur. J. Pharmacol. Section Abstract Doc Link 1330643 Disease Relevance 0.07 Pain Relevance 0.49
In C6 glioma cells expressing either recombinant h 5-HT1B or h 5-HT1D receptors, sumatriptan similarly increased IK in a concentration-dependent manner (maximum increase 19.4+/-7.2%, n=8, P<0.05 and 25.1+/-3.9%, n=6, P<0.001, respectively) with EC50 values (geometric mean with 95% confidence intervals in parentheses) of 56.3 nM (7.9-140 nM) and 68.7 nM (16-120 nM), respectively.
Gene_expression (expressing) of 5-HT1D associated with sumatriptan and glioma
2) Confidence 0.75 Published 1998 Journal Naunyn Schmiedebergs Arch. Pharmacol. Section Abstract Doc Link 9879718 Disease Relevance 0.35 Pain Relevance 0.26
In C6 cells expressing either cloned h 5-HT1B or h 5-HT1D receptors, sumatriptan-induced increases in IK were prevented by the calcium chelator EGTA (5 mM) when included in the patch pipette (maximum increase 0.57+/-0.6%, n=3, P=NS and -2.8+/-1.6%, n=5, P=NS, respectively).
Gene_expression (expressing) of 5-HT1D associated with sumatriptan
3) Confidence 0.75 Published 1998 Journal Naunyn Schmiedebergs Arch. Pharmacol. Section Abstract Doc Link 9879718 Disease Relevance 0.13 Pain Relevance 0.62
The putative coupling between stably expressed recombinant h 5-HT1B or h 5-HT1D receptors and K+ channels which regulate excitability was investigated in C6 glioma cells.
Gene_expression (expressed) of 5-HT1D associated with glioma
4) Confidence 0.75 Published 1998 Journal Naunyn Schmiedebergs Arch. Pharmacol. Section Abstract Doc Link 9879718 Disease Relevance 0.33 Pain Relevance 0.06
Messages for the 5-HT1D alpha and 5-HT1D beta receptors were expressed in all except one of the 10 trigeminal ganglia studied.
Neg (except) Gene_expression (expressed) of 5-HT1D in trigeminal ganglia
5) Confidence 0.75 Published 1996 Journal Mol. Pharmacol. Section Abstract Doc Link 8700126 Disease Relevance 0.08 Pain Relevance 0.32
In contrast, the data point to a preferential expression of 5-HT1D alpha receptors in neural versus vascular tissues and strongly reemphasize the need for selective 5-HT1D alpha agonists in the identification of the target tissue(s) for antimigraine drugs.
Gene_expression (expression) of 5-HT1D in neural associated with cluster headache and agonist
6) Confidence 0.75 Published 1996 Journal Mol. Pharmacol. Section Abstract Doc Link 8700126 Disease Relevance 0.18 Pain Relevance 0.23
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.
Gene_expression (expressing) of 5-HT1D in L929 associated with substantia nigra and glioma
7) Confidence 0.75 Published 1996 Journal Mol. Pharmacol. Section Abstract Doc Link 8967979 Disease Relevance 0.17 Pain Relevance 0.43
In signal transduction assays using cells expressing recombinant h5-HT1D alpha, h5-HT1D beta, or h5-HT1A receptors, alniditan (like 5-HT) was a full agonist for inhibition of stimulated adenylyl cyclase (IC50 = 1.1, 1.3, and 74 nM, respectively, for alniditan).
Gene_expression (expressing) of 5-HT1D associated with agonist
8) Confidence 0.75 Published 1996 Journal Mol. Pharmacol. Section Abstract Doc Link 8967979 Disease Relevance 0.19 Pain Relevance 0.78
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.
Gene_expression (expressing) of 5-HT1D in L929 associated with substantia nigra and glioma
9) Confidence 0.75 Published 1996 Journal Mol. Pharmacol. Section Abstract Doc Link 8967979 Disease Relevance 0.17 Pain Relevance 0.47
In signal transduction assays using cells expressing recombinant h5-HT1D alpha, h5-HT1D beta, or h5-HT1A receptors, alniditan (like 5-HT) was a full agonist for inhibition of stimulated adenylyl cyclase (IC50 = 1.1, 1.3, and 74 nM, respectively, for alniditan).
Gene_expression (expressing) of 5-HT1D associated with agonist
10) Confidence 0.75 Published 1996 Journal Mol. Pharmacol. Section Abstract Doc Link 8967979 Disease Relevance 0.19 Pain Relevance 0.78
Recombinant human 5-HT1D alpha and 5-HT1D beta receptor subtypes were stably expressed in NIH-3T3 fibroblasts (1D alpha cell line) and Y-1 adrenocortical tumor cells (1D beta cell line), respectively, for pharmacological evaluations of serotonergic compounds to inhibit forskolin-stimulated cAMP accumulation (FSCA). [3H]LSD saturation studies indicated that 5-HT1D receptor expression levels were slightly higher in the 1D beta cell line (Bmax = 1334 +/- 134 fmol/mg protein) than in the 1D alpha cell line (Bmax = 900 +/- 218 fmol/mg protein). 5-HT inhibited FSCA with similar potencies (EC50 approximately 2 nM) in both assay systems.
Gene_expression (expression) of 5-HT1D in Y-1 associated with cancer
11) Confidence 0.75 Published 1996 Journal Naunyn Schmiedebergs Arch. Pharmacol. Section Abstract Doc Link 8878051 Disease Relevance 0.10 Pain Relevance 0.10
Recombinant human 5-HT1D alpha and 5-HT1D beta receptor subtypes were stably expressed in NIH-3T3 fibroblasts (1D alpha cell line) and Y-1 adrenocortical tumor cells (1D beta cell line), respectively, for pharmacological evaluations of serotonergic compounds to inhibit forskolin-stimulated cAMP accumulation (FSCA). [3H]LSD saturation studies indicated that 5-HT1D receptor expression levels were slightly higher in the 1D beta cell line (Bmax = 1334 +/- 134 fmol/mg protein) than in the 1D alpha cell line (Bmax = 900 +/- 218 fmol/mg protein). 5-HT inhibited FSCA with similar potencies (EC50 approximately 2 nM) in both assay systems.
Gene_expression (expressed) of 5-HT1D in beta cell associated with cancer
12) Confidence 0.75 Published 1996 Journal Naunyn Schmiedebergs Arch. Pharmacol. Section Abstract Doc Link 8878051 Disease Relevance 0.10 Pain Relevance 0.03
Recombinant human 5-HT1D alpha and 5-HT1D beta receptor subtypes were stably expressed in NIH-3T3 fibroblasts (1D alpha cell line) and Y-1 adrenocortical tumor cells (1D beta cell line), respectively, for pharmacological evaluations of serotonergic compounds to inhibit forskolin-stimulated cAMP accumulation (FSCA). [3H]LSD saturation studies indicated that 5-HT1D receptor expression levels were slightly higher in the 1D beta cell line (Bmax = 1334 +/- 134 fmol/mg protein) than in the 1D alpha cell line (Bmax = 900 +/- 218 fmol/mg protein). 5-HT inhibited FSCA with similar potencies (EC50 approximately 2 nM) in both assay systems.
Gene_expression (expressed) of 5-HT1D in beta cell associated with cancer
13) Confidence 0.75 Published 1996 Journal Naunyn Schmiedebergs Arch. Pharmacol. Section Abstract Doc Link 8878051 Disease Relevance 0.10 Pain Relevance 0.03
Although the potencies (EC50 values) of compounds matched their respective affinity constants (Ki values) for the closely-related 5-HT1D subtypes, differences in intrinsic activities were observed for a few compounds between the two 5-HT1D receptor expression systems.
Gene_expression (expression) of 5-HT1D
14) Confidence 0.75 Published 1996 Journal Naunyn Schmiedebergs Arch. Pharmacol. Section Abstract Doc Link 8878051 Disease Relevance 0 Pain Relevance 0.17
Pharmacological characterisation of [35S]-GTPgammaS binding to Chinese hamster ovary cell membranes stably expressing cloned human 5-HT1D receptor subtypes.

[35S]-GTPgammaS binding has been used to study the function of cloned human 5-HT1D receptor subtypes stably expressed in chinese hamster ovary (CHO) cells. 5-HT stimulated [35S]-GTPgammaS binding to membranes from cells expressing 5-HT1Dalpha or 5-HT1Dbeta receptors.

Gene_expression (expressing) of 5-HT1D in ovary
15) Confidence 0.75 Published 1995 Journal J. Recept. Signal Transduct. Res. Section Title Doc Link 8903941 Disease Relevance 0 Pain Relevance 0.32
Pharmacological characterisation of [35S]-GTPgammaS binding to Chinese hamster ovary cell membranes stably expressing cloned human 5-HT1D receptor subtypes.

[35S]-GTPgammaS binding has been used to study the function of cloned human 5-HT1D receptor subtypes stably expressed in chinese hamster ovary (CHO) cells. 5-HT stimulated [35S]-GTPgammaS binding to membranes from cells expressing 5-HT1Dalpha or 5-HT1Dbeta receptors.

Gene_expression (expressed) of 5-HT1D in ovary
16) Confidence 0.75 Published 1995 Journal J. Recept. Signal Transduct. Res. Section Title Doc Link 8903941 Disease Relevance 0 Pain Relevance 0.31
Outward K+ currents (IK) were examined in nontransfected C6 glioma cells and in cells expressing cloned h 5-HT1B or h 5-HT1D receptors using the patch-clamp technique in the whole-cell configuration.
Gene_expression (expressing) of 5-HT1D associated with glioma
17) Confidence 0.75 Published 1998 Journal Naunyn Schmiedebergs Arch. Pharmacol. Section Abstract Doc Link 9879718 Disease Relevance 0.36 Pain Relevance 0.14
The expression of the mRNA 5-HT1D serotonin receptor was also detected in blastocysts cultured in vitro.
Gene_expression (expression) of 5-HT1D associated with serotonin
18) Confidence 0.75 Published 2003 Journal Physiol Res Section Abstract Doc Link 12678665 Disease Relevance 0 Pain Relevance 0.61
Peripherally, 5-HT1B receptor is expressed on cranial blood vessels and mediates vasoconstriction while the 5-HT1D receptor is expressed on trigeminal nerve endings.
Gene_expression (expressed) of 5-HT1D in trigeminal nerve associated with fifth nerve and increased venous pressure under development
19) Confidence 0.75 Published 2010 Journal Drug design, development and therapy Section Body Doc Link PMC2846149 Disease Relevance 0.85 Pain Relevance 1.16
Both transfected cell lines expressed a similar 5-HT1D beta receptor density (361 to 448 fmol/mg protein) and displayed a number of similar cAMP responses: marked inhibition of forskolin-stimulated cAMP formation by 5-HT; a similar agonist potency and efficacy with 5-carboxamidotryptamine (5-CT), 5-methoxytryptamine, bufotenine, sumatriptan, 7-trifluoromethyl-4(4-methyl-1-piperazinyl)-pyrolo-(1,2-a)quinoxal ine (CGS 12066B), 5-methoxy-3(1,2,3,6-tetrahydro-4-pyridinyl)1H-indole (RU 24,969), and tryptamine, their maximal effect being comparable to that of 5-HT; less agonist efficacy with m-trifluoro-phenyl-piperazine (TFMPP) (it inhibited at most 63% of stimulated cAMP formation); and antagonist activity against the 5-CT-mediated agonist response with methiothepin, 2'-methyl-4-(5-methyl-[1,2,4]oxadiazol-3-yl)-biphenyl-4-carboxylic acid [4-methoxy-3-(4-methyl-piperazin-1-yl)-phenyl]-amide (GR 127,935), and ritanserin.
Gene_expression (expressed) of 5-HT1D associated with sumatriptan, antagonist, agonist and potency
20) Confidence 0.75 Published 1995 Journal Biochem. Pharmacol. Section Abstract Doc Link 7503768 Disease Relevance 0 Pain Relevance 0.38

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