INT95585

From wiki-pain
Jump to: navigation, search
Context Info
Confidence 0.43
First Reported 2001
Last Reported 2010
Negated 0
Speculated 0
Reported most in Body
Documents 18
Total Number 21
Disease Relevance 8.32
Pain Relevance 11.23

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

mitochondrion (Pde12)
Anatomy Link Frequency
spinal 1
spinal cord 1
neurons 1
lung 1
Pde12 (Rattus norvegicus)
Pain Link Frequency Relevance Heat
anesthesia 18 100.00 Very High Very High Very High
adenocard 120 99.84 Very High Very High Very High
Neuropathic pain 95 99.72 Very High Very High Very High
Antinociceptive 116 99.68 Very High Very High Very High
antinociception 100 99.64 Very High Very High Very High
GABA receptor 50 99.36 Very High Very High Very High
Glutamate 12 99.18 Very High Very High Very High
intrathecal 166 99.16 Very High Very High Very High
diclofenac 15 99.00 Very High Very High Very High
antagonist 122 98.96 Very High Very High Very High
Disease Link Frequency Relevance Heat
Neuropathic Pain 164 99.72 Very High Very High Very High
Increased Venous Pressure Under Development 24 99.28 Very High Very High Very High
Reprotox - General 2 11 98.96 Very High Very High Very High
Hyperalgesia 42 98.44 Very High Very High Very High
Convulsion 12 98.00 Very High Very High Very High
Cognitive Disorder 12 97.92 Very High Very High Very High
Pulmonary Fibrosis 6 97.64 Very High Very High Very High
Amnesia 4 96.76 Very High Very High Very High
INFLAMMATION 30 94.78 High High
Erectile Dysfunction 4 94.60 High High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
Since sildenafil is a potent and selective inhibitor of phosphodiesterase 5, our results suggest that this drug produced its antinociceptive activity, and increased that of diclofenac, probably through the inhibition of cyclic GMP degradation.
Negative_regulation (inhibitor) of phosphodiesterase 5 associated with diclofenac and antinociceptive
1) Confidence 0.43 Published 2001 Journal Eur. J. Pharmacol. Section Abstract Doc Link 11343689 Disease Relevance 0 Pain Relevance 0.65
The antinociceptive activity of an inhibitor of phosphodiesterase 5, alone or combined with diclofenac, was assessed in the formalin test.
Negative_regulation (inhibitor) of phosphodiesterase 5 associated with diclofenac and antinociceptive
2) Confidence 0.43 Published 2001 Journal Eur. J. Pharmacol. Section Abstract Doc Link 11343689 Disease Relevance 0 Pain Relevance 0.47
In contrast, 1-[4-ethoxy-3-(6,7-dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo [3,4-d]pyrimidin-5-yl)phenylsulfonyl]-4-methyl piperazine (sildenafil, an inhibitor of phosphodiesterase 5) produced significant antinociception, only during the second phase of the formalin test.
Negative_regulation (inhibitor) of phosphodiesterase 5 associated with antinociception
3) Confidence 0.38 Published 2001 Journal Eur. J. Pharmacol. Section Abstract Doc Link 11343689 Disease Relevance 0 Pain Relevance 0.65
The release of glutamate and aspartate was also increased by the inhibitor of phosphodiesterase 5, UK-114,542.
Negative_regulation (inhibitor) of phosphodiesterase 5 associated with glutamate
4) Confidence 0.13 Published 2002 Journal Neuroscience Section Abstract Doc Link 12044451 Disease Relevance 0 Pain Relevance 0.67
Phosphodiesterase-5 inhibitors oppose hyperoxic vasoconstriction and accelerate seizure development in rats exposed to hyperbaric oxygen.
Negative_regulation (inhibitors) of Phosphodiesterase-5 associated with anesthesia, convulsion and increased venous pressure under development
5) Confidence 0.11 Published 2009 Journal J. Appl. Physiol. Section Title Doc Link 19179645 Disease Relevance 0.59 Pain Relevance 0.13
The inhibition of phosphodiesterase 5 produces an antinociception through the increase of cyclic guanosine monophosphate (cGMP), and increasing cGMP levels enhance the release of ?
Negative_regulation (inhibition) of phosphodiesterase 5 associated with antinociception
6) Confidence 0.11 Published 2010 Journal Yonsei Medical Journal Section Abstract Doc Link PMC2799976 Disease Relevance 0.28 Pain Relevance 0.38
The following drugs were used in this study: sildenafil (phosphodiesterase 5 inhibitor), bicuculline (GABAA receptor antagonist, Sigma Aldrich Co., St.
Negative_regulation (inhibitor) of phosphodiesterase 5 associated with antagonist
7) Confidence 0.11 Published 2010 Journal Yonsei Medical Journal Section Body Doc Link PMC2799976 Disease Relevance 0.23 Pain Relevance 0.54
In this study, intrathecal administration of sildenafil, a specific phosphodiesterase 5 inhibitor, dose-dependently suppressed flinching during both phase 1 and phase 2 of the formalin test, consistent with previous observations,4,5,9 suggesting that sildenafil is active against acute pain and facilitated state at the spinal level.
Negative_regulation (inhibitor) of phosphodiesterase 5 in spinal associated with acute pain and intrathecal
8) Confidence 0.10 Published 2010 Journal Yonsei Medical Journal Section Body Doc Link PMC2995964 Disease Relevance 0.35 Pain Relevance 0.46
Locally injected dibutyryl-cGMP showed antinociception in inflammatory hyperalgesia model.27 Intrathecally administered 8-bromo-cGMP reduced the mechanical allodynia in a neuropathic model.28,29 Thus, our observations suggest that intrathecal sildenafil produces an antinociceptive effect via the accumulation of cGMP, through the inhibition of phosphodiesterase 5.
Negative_regulation (inhibition) of phosphodiesterase 5 associated with antinociception, hyperalgesia, allodynia, inflammation, neuropathic pain, antinociceptive and intrathecal
9) Confidence 0.10 Published 2010 Journal Yonsei Medical Journal Section Body Doc Link PMC2995964 Disease Relevance 0.67 Pain Relevance 0.90
Phosphodiesterase-5 inhibition by sildenafil citrate in a rat model of bleomycin-induced lung fibrosis.
Negative_regulation (inhibition) of Phosphodiesterase-5 in lung associated with fibrosis and pulmonary fibrosis
10) Confidence 0.10 Published 2010 Journal Pulm Pharmacol Ther Section Title Doc Link 19945540 Disease Relevance 0.30 Pain Relevance 0.20
Therefore, it is conceivable that the increased cGMP level by inhibition of phosphodiesterase 5 may contribute to the attenuation of the neuropathic pain at a systemic level.
Negative_regulation (inhibition) of phosphodiesterase 5 associated with neuropathic pain
11) Confidence 0.09 Published 2010 Journal Yonsei Medical Journal Section Body Doc Link PMC2799976 Disease Relevance 1.03 Pain Relevance 0.84
It would therefore, appear that cGMP analog increases the synaptic GABA release to labeled paraventricular nucleus neurons.32,33 And increasing cGMP level by superfusing slices with another phosphodiesterase inhibitor (zaprinast) increases GABA release in the brain stem, while a guanylyl cyclase inhibitor (ODQ) reduces GABA release.15 Recently, it has been demonstrated that potassium channels are downstream effectors of cGMP on GABA release.33 Furthermore, the antinociception provoked by sildenafil and dibutyryl-cGMP was reversed by potassium channel blockers.10,34 These findings together suggest that intravenous sildenafil increases the cGMP level by inhibition of phosphodiesterase 5 and then induces the release of GABA through a downstream mechanism, involving potassium channels which act on GABA receptors, in turn leading to an antinociceptive effect.
Negative_regulation (inhibition) of phosphodiesterase 5 in neurons associated with antinociception, gaba, gaba receptor, potassium channel and antinociceptive
12) Confidence 0.09 Published 2010 Journal Yonsei Medical Journal Section Body Doc Link PMC2799976 Disease Relevance 0.07 Pain Relevance 0.81
In summary, sildenafil, an inhibitor of phosphodiesterase 5, increased the cGMP level in the spinal cord, thereby resulting in its antinociceptive effect in the formalin test.
Negative_regulation (inhibitor) of phosphodiesterase 5 in spinal cord associated with antinociceptive and spinal cord
13) Confidence 0.09 Published 2010 Journal Yonsei Medical Journal Section Body Doc Link PMC2995964 Disease Relevance 0.06 Pain Relevance 1.29
Sildenafil (Viagra®; Pfizer US Pharmaceutical Group, New York, NY, USA) is a selective, potent inhibitor of cGMP-specific phosphodiesterase 5, which increases the cGMP concentration by inhibiting the hydrolysis of cGMP to GMP.1 It has been shown to have antinociceptive effects in the formalin test in rats and in the writhing response induced by acetic acid and zymosan in mice,2-8 which is mediated through the nitric oxide (NO)-cGMP-potassium channel pathway.4,6,8,9 Recently, intrathecal sildenafil was reported to produce antinociceptive effects, mediated through GABAB and opioid receptors.5,10
Negative_regulation (inhibitor) of phosphodiesterase 5 associated with opioid receptor, potassium channel, antinociceptive and intrathecal
14) Confidence 0.09 Published 2010 Journal Yonsei Medical Journal Section Body Doc Link PMC2995964 Disease Relevance 0.06 Pain Relevance 0.37
In this work, we examined the contribution of GABA receptors to the effect of sildenafil, a phosphodiesterase 5 inhibitor, in a neuropathic pain rat, and assessed the hemodynamic effect of sildenafil in normal rats.


Negative_regulation (inhibitor) of phosphodiesterase 5 associated with gaba receptor and neuropathic pain
15) Confidence 0.09 Published 2010 Journal Yonsei Medical Journal Section Abstract Doc Link PMC2799976 Disease Relevance 0.44 Pain Relevance 0.63
We aimed to determine which mechanism possibly accounts for the beneficial effect by investigating its vascular action in different in vitro preparations in comparison with other coxibs and reference phosphodiesterase-5 (PDE5) inhibitors.
Negative_regulation (inhibitors) of phosphodiesterase-5
16) Confidence 0.07 Published 2007 Journal Cardiovasc. Res. Section Abstract Doc Link 17383621 Disease Relevance 0.26 Pain Relevance 0.18
Furthermore, local sildenafil, a phosphodiesterase 5 inhibitor, caused antinociception in carrageenan-induced hyperalgesia, the writhing test and the second phase of the formalin test (25-29).
Negative_regulation (inhibitor) of phosphodiesterase 5 associated with antinociception and hyperalgesia
17) Confidence 0.07 Published 2008 Journal Journal of Korean Medical Science Section Body Doc Link PMC2610640 Disease Relevance 0.57 Pain Relevance 0.88
Sildenafil is an inhibitor of cGMP-specific phosphodiesterase 5, but zaprinast is an inhibitor for phosphodiesterase 5, 6, and 9.
Negative_regulation (inhibitor) of phosphodiesterase 5
18) Confidence 0.06 Published 2008 Journal Journal of Korean Medical Science Section Body Doc Link PMC2610640 Disease Relevance 0.14 Pain Relevance 0.87
Drug interactions studies demonstrate that tadalafil, a phosphodiesterase-5 inhibitors used in the treatment of ED, did not affect the pharmacokinetics of dapoxetine, whereas sildenafil increased the dapoxetine AUC by 22% (Dresser, Jazrawi, et al 2005).
Negative_regulation (inhibitors) of phosphodiesterase-5 associated with reprotox - general 2
19) Confidence 0.04 Published 2006 Journal Neuropsychiatric Disease and Treatment Section Body Doc Link PMC2671940 Disease Relevance 0.58 Pain Relevance 0.06
It is of interest that a combination of a phosphodiesterase-5 inhibitor and an adenosine ADORA2A antagonist, mimicking two major mechanisms of action of caffeine, prevented the memory impairment, though neither drug alone had such effect.
Negative_regulation (inhibitor) of phosphodiesterase-5 associated with cognitive disorder, adenocard and antagonist
20) Confidence 0.01 Published 2010 Journal Current Neuropharmacology Section Body Doc Link PMC2923369 Disease Relevance 1.35 Pain Relevance 0.14

General Comments

This test has worked.

Personal tools
Namespaces

Variants
Actions
Navigation
Toolbox