INT257299

From wiki-pain
Jump to: navigation, search
Context Info
Confidence 0.27
First Reported 2006
Last Reported 2010
Negated 2
Speculated 0
Reported most in Body
Documents 14
Total Number 14
Disease Relevance 4.31
Pain Relevance 2.45

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

cytosol (Pde5a) signal transduction (Pde5a)
Anatomy Link Frequency
corpus 1
neurons 1
lung 1
optic nerve 1
Pde5a (Rattus norvegicus)
Pain Link Frequency Relevance Heat
Bioavailability 6 97.96 Very High Very High Very High
GABA receptor 10 96.16 Very High Very High Very High
gABA 11 95.92 Very High Very High Very High
backache 12 92.72 High High
nud 11 91.92 High High
headache 19 91.24 High High
antinociception 23 90.36 High High
Morphine 36 90.28 High High
Neuropathic pain 26 89.60 High High
Calcium channel 11 88.28 High High
Disease Link Frequency Relevance Heat
Increased Venous Pressure Under Development 72 99.98 Very High Very High Very High
Erectile Dysfunction 460 99.80 Very High Very High Very High
Reprotox - General 2 32 99.78 Very High Very High Very High
Sensorineural Hearing Loss 1 99.48 Very High Very High Very High
Convulsion 1 94.08 High High
Disease 68 93.76 High High
Low Back Pain 6 92.72 High High
Dyspepsia 11 91.92 High High
Headache 20 91.24 High High
Hypertension 50 90.64 High High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
The mechanism of action leading to penile erection involves inhibition of PDE5, the major cyclic guanosine monophospate (cGMP) hydrolyzing enzyme located in the vascular smooth muscle cells of corpus cavernosum.
PDE5 Neg (inhibition) Binding (inhibition) of in corpus associated with erectile dysfunction
1) Confidence 0.27 Published 2006 Journal Clinical Interventions in Aging Section Body Doc Link PMC2699638 Disease Relevance 0.71 Pain Relevance 0.03
Although frequently asked about by patients, priapism is rarely associated with PDE5 inhibitors.
PDE5 Binding (associated) of associated with reprotox - general 2
2) Confidence 0.19 Published 2008 Journal Therapeutics and Clinical Risk Management Section Body Doc Link PMC2643112 Disease Relevance 1.06 Pain Relevance 0.23
All three have a heterocyclic nitrogen-containing doublering system, with a central ring that is analogous to that of cGMP and allows for competitive binding of the drug with PDE5 at the catalytic site (Francis et al 2001).
PDE5 Binding (binding) of
3) Confidence 0.19 Published 2008 Journal Therapeutics and Clinical Risk Management Section Body Doc Link PMC2643112 Disease Relevance 0.05 Pain Relevance 0
In particular, sildenafil is different from zaprinast in terms of specificity for cGMP.
cGMP Binding (specificity) of
4) Confidence 0.15 Published 2008 Journal Journal of Korean Medical Science Section Body Doc Link PMC2610640 Disease Relevance 0.13 Pain Relevance 0.96
They exhibit high affinity for both cAMP and cGMP but the Vmax for cGMP hydrolysis is 4–10 times higher (Degerman et al 1997).
cGMP Binding (affinity) of
5) Confidence 0.13 Published 2008 Journal International Journal of Chronic Obstructive Pulmonary Disease Section Body Doc Link PMC2650605 Disease Relevance 0.18 Pain Relevance 0.04
Vardenafil, with a bioavailability of 15% after oral administration, may benefit from these structural changes through stronger binding interaction to the PDE-5 catalytic site.
PDE-5 Binding (interaction) of associated with bioavailability
6) Confidence 0.10 Published 2010 Journal Advances in Pharmacological Sciences Section Body Doc Link PMC2997760 Disease Relevance 0.67 Pain Relevance 0.25
Current evidence suggests that substrate specificity is conferred by the orientation of a single glutamine residue within the catalytic site which can either form hydrogen bonds with cAMP, cGMP or both depending on its fixed orientation or ability to rotate (Zhang et al 2004).
cGMP Binding (cAMP) of
7) Confidence 0.10 Published 2008 Journal International Journal of Chronic Obstructive Pulmonary Disease Section Body Doc Link PMC2650605 Disease Relevance 0.06 Pain Relevance 0
PDE3 differs from PDE4 in that it has high affinity for both cAMP and cGMP so that these substrates are mutually competitive and thus PDE3 hydrolysis of cAMP can be inhibited by cGMP.
cGMP Binding (affinity) of
8) Confidence 0.10 Published 2008 Journal International Journal of Chronic Obstructive Pulmonary Disease Section Body Doc Link PMC2650605 Disease Relevance 0.17 Pain Relevance 0.04
Thus, when intracellular cGMP levels rise, cGMP breakdown is enhanced both by increased activity at the catalytic site, followed by enhanced cGMP binding at the allosteric sites, leading to increased enzymatic activity as a result of phosphorylation.
cGMP Binding (binding) of
9) Confidence 0.09 Published 2008 Journal International Journal of Chronic Obstructive Pulmonary Disease Section Body Doc Link PMC2650605 Disease Relevance 0.06 Pain Relevance 0
Furthermore, this phosphodiesterase 5 plays a pivotal role in the regulation of the vasodilatation associated to cGMP.
cGMP Binding (associated) of associated with increased venous pressure under development
10) Confidence 0.09 Published 2010 Journal Yonsei Medical Journal Section Abstract Doc Link PMC2799976 Disease Relevance 0.41 Pain Relevance 0.59
PDE5Is have also been associated with sudden sensorineural hearing loss,61 and studies of audiometric properties in men and experimental animals using sildenafil or vardenafil have suggested changes in hearing.62,63 Although we are not aware of any published studies directly linking tadalafil to hearing changes, the possibility of a PDE5I class effect on hearing must be considered and taken seriously by patients and providers.


PDE5Is Binding (associated) of associated with sensorineural hearing loss
11) Confidence 0.04 Published 2010 Journal Drug Design, Development and Therapy Section Body Doc Link PMC2939761 Disease Relevance 0.25 Pain Relevance 0
Sildenafil, a phosphodiesterase inhibitor, given orally, has been shown to be a potent and selective pulmonary vasodilator.60 Sildenafil works by selectively inhibiting phos-phodiesterase V (PDE V),61 which is responsible for cGMP breakdown in lung tissue.
PDE V Binding (inhibiting) of in lung
12) Confidence 0.02 Published 2009 Journal Vascular Health and Risk Management Section Body Doc Link PMC2697585 Disease Relevance 0.53 Pain Relevance 0.31
These results indicate that endogenous NO, possibly produced by nNOS in DRG neurons, does not affect basal KATP channel activity in either SS or SNL neurons.

8-Br-cGMP activates KATP channels, but fails to mimic completely the activation induced by NO

cGMP Neg (fails) Binding (fails) of in neurons
13) Confidence 0.02 Published 2009 Journal Mol Pain Section Body Doc Link PMC2673211 Disease Relevance 0 Pain Relevance 0
In optic nerve axons, hyperpolarization-activated cyclic nucleotide-modulated cation (HCN) channels, which bind cGMP or cAMP directly, were recently suggested to be a target.
cGMP Binding (bind) of in optic nerve
14) Confidence 0.01 Published 2010 Journal The European Journal of Neuroscience Section Abstract Doc Link PMC2955965 Disease Relevance 0 Pain Relevance 0

General Comments

This test has worked.

Personal tools
Namespaces

Variants
Actions
Navigation
Toolbox