Antagonist hyperalgesia. Medical search. Frequent questions

Two chemically unrelated NK 1 receptor antagonists, CP-99,994 (3-30 mg/kg) and SR 140333 (1-100 mg/kg), also dose dependently blocked the late phase, with respective MEDs of 3 and 10 mg/kg. (aspetjournals.org)
It is suggested that NK 1 receptor antagonists possess a superior side effect profile to carbamazepine and morphine and may have a therapeutic use for the treatment of inflammatory and neuropathic pain. (aspetjournals.org)
and c) peripheral administration of peptide CRF receptor antagonists blocked the colonic responses to exogenous CRF and was able to attenuate the colonic responses to stress. (uclahealth.org)
As stress plays a major role in the onset, maintenance and/or exacerbation of IBS symptoms, long-acting CRF receptor antagonists developed by J. Rivier are presently being evaluated by Dr. Muriel Larauche for their ability to prevent visceral pain and diarrhea in experimental models of IBS. (uclahealth.org)
Thus, orally active non-peptide B 1 receptor antagonists should have clinical therapeutic potential in the treatment of sensory polyneuropathy. (johnshopkins.edu)
4) Biaromatic P2X7 Antagonists Another variance of P2X7 receptor antagonists is usually presented within patent US20080146612A1, where inventors make use of a substituted biaromatic group [111]. (afl-journal.org)
This heterocylic amide derivative is usually unlike any of the other P2X7 receptor antagonists discussed up to this point, which do not target specific domains or motifs in the P2X7 receptor protein. (afl-journal.org)
Thus, when comparing the efficacy of different P2X7 receptor antagonists, one must take care not to directly compare complete IC50 values from study to study, as many factors may influence the reported values. (afl-journal.org)

We hypothesized that CRF-CRFR1 signaling in central amygdala (CeA) mediates stress-induced hyperalgesia in rats with high stress reactivity. (nature.com)
Finally, intra-CeA infusion of tetrodotoxin produced thermal hyperalgesia in unstressed rats and blocked the anti-hyperalgesic effect of systemic CRFR1 antagonist in stressed rats. (nature.com)
These data suggest that rats with high stress reactivity exhibit hyperalgesia that is mediated by CRF-CRFR1 signaling in CeA. (nature.com)
Remifentanil was delivered intravenously in rats to induce hyperalgesia. (iasp-pain.org)
Intraperitoneal (i.p.) injection of kainic acid induced a persistent thermal hyperalgesia, when tested using the hot plate (mice) and tail flick (mice and rats) assays, and mechanical hyperalgesia when tested using von Frey monofilaments (rats), but had no effect on acetic acid-induced chemical nociception (mice). (biopsychiatry.com)
The antagonist (10 mg kg -1 ) had no effect on plasma glucose and insulin, insulin resistance (HOMA index) and aortic superoxide anion production in glucose-fed rats. (johnshopkins.edu)
Supraspinal opioid receptor participation in EA anti-hyperalgesia in swollen rats is not 1226056-71-8 manufacture examined. (gasyblog.com)
This study inquired into whether and how GPR30 and GABA A -α4β1δ in the PAG promote preoperative anxiety-induced postoperative hyperalgesia in female rats. (biomedcentral.com)
After microinjection of G1 into the PAG, female rats with plantar incision continued to exhibit significant hyperalgesia until postoperative 48 h. (biomedcentral.com)
On the other hand, microinjection of G15 with SPS and plantar incision procedure relieved postoperative hyperalgesia in female rats. (biomedcentral.com)
Our results indicate that the GPR30-PKA-GABA A α4β1δ pathway in the PAG promotes preoperative anxiety-induced postoperative hyperalgesia in female rats. (biomedcentral.com)
This study has investigated the involvement of BK receptors in two models of persistent inflammatory hyperalgesia in rats. (cmich.edu)
In a Freund's adjuvant-induced hyperalgesia model and an ultraviolet (UV)-induced hyperalgesia model in rats the specific B 2 antagonist, D-Arg[Hyp 3 , Thi 5 , D-Tic 7 , Oic 8 ]-BK (HOE 140), was either ineffective or weakly active in reversing hyperalgesia. (cmich.edu)
In a Freund's adjuvant-induced hyperalgesia model and an ultraviolet (UV)-induced hyperalgesia model in rats the specific B2 antagonist, D-Arg[Hyp3, Thi5, D-Tic7, Oic8]-BK (HOE 140), was either ineffective or weakly active in reversing hyperalgesia. (cmich.edu)

Systemic blockade of corticotropin-releasing factor (CRF) type 1 receptors (CRFR1s) reduces stress-induced thermal hyperalgesia. (nature.com)
The pharmacology for opioid-induced hyperalgesia is more complicated, and is believed to involve the activation of NMDA receptors and increased excitatory peptide neurotransmitters (such as cholecystokinin). (wikipedia.org)
Together these data suggest that a persistent hyperalgesia results from the transient activation of AMPA/KA receptors that are located outside the spinal cord, perhaps on the distal projections of primary afferent fibers. (biopsychiatry.com)
1996), however the function of RVM and opioid receptors in EA-produced anti-hyperalgesia within an inflammatory discomfort rat model had not been examined. (gasyblog.com)
Data suggest that in persistent inflammatory conditions in the rat bradykinin B 1 receptors are involved in the accompanying hyperalgesia. (cmich.edu)
Commonly reported side effects of opioids are drowsiness, nausea, abdominal pain, confusion, and respiratory depression with variable incidence.Similar to other patients receiving treatment for chronic or recurrent pain, SCD patients may experience opioid-induced hyperalgesia, an enhanced pain response owing to the activation of the N-methyl-d-aspartate (NMDA) receptors. (everyonesmd.com)
The targeting ability of the compound patented was tested both and and exert anti-nociceptive effects as a measure of their antagonist activities at P2X7 receptors. (afl-journal.org)

Activated astrocytes & microglia (glia) release IL1β in response to gp120, and IT IL1 receptor antagonist or glial metabolic inhibitors prevent IT gp120-induced allodynia and thermal hyperalgesia. (atsbio.com)
Background and purpose: Diabetes causes sensory polyneuropathy with associated pain in the form of tactile allodynia and thermal hyperalgesia which are often intractable and resistant to current therapy. (johnshopkins.edu)

Using N-methyl-D-aspartate (NMDA) receptor antagonist drugs. (webmd.com)
NMDA receptor modulates spinal iron accumulation via activating DMT1(-)IRE in remifentanil-induced hyperalgesia. (iasp-pain.org)
N-methyl-D-aspartate (NMDA) receptor activation is known to be critical in remifentanil-induced hyperalgesia. (iasp-pain.org)
The NMDA receptor antagonist MK-801 was intrathecally administrated. (iasp-pain.org)
This study suggests that DMT1(-)IRE-mediated iron accumulation is likely to be the downstream event following NMDA receptor activation and Ca influx, contributing to remifentanil-induced hyperalgesia. (iasp-pain.org)
Ketamine, a noncompetitive NMDA receptor antagonist, may modulate opioid-induced hyperalgesia by impairing the sensitization of the spinal neurons to nociceptive stimuli. (everyonesmd.com)

When injected intrathecally (i.t.), kainic acid itself failed to induce hyperalgesia and AMPA/KA antagonists given i.t. also failed to attenuate the hyperalgesic effect of kainic acid administered i.p., indicating that the spinal cord is not the primary site of action. (biopsychiatry.com)

We used pharmacological, molecular, and immunohistochemical techniques to assess the role of CRF-CRFR1 signaling in CeA in stress-induced hyperalgesia. (nature.com)
Intra-CeA CRF infusion mimicked stress-induced hyperalgesia. (nature.com)
Enhanced nociception and pain sensitivity due to exposure to physical or psychological stressors is described as stress-induced hyperalgesia (SIH) [ 4 ]. (biomedcentral.com)

Avoiders exhibited thermal hyperalgesia that was reversed by systemic or intra-CeA injection of a CRFR1 antagonist. (nature.com)
Chronic constrictive injury (CCI) to a sciatic nerve in the rat induced spontaneous pain, thermal and mechanical hyperalgesia, and cold, dynamic, and static allodynia. (aspetjournals.org)
Summary: Intrathecal (IT) HIV-1 glycoprotein, gp120: (a) produces thermal hyperalgesia & low threshold mechanical allodynia, and (b) increases interleukin-1β (IL1β) protein levels in lumbosacral (LS) spinal cord tissue & surrounding cerebrospinal fluid (CSF). (atsbio.com)
A single intraperitoneal (i.p.) and intracerebroventricular (i.c.v.), but not intrathecal, pilocarpine administration attenuated ICS-induced thermal hyperalgesia and mechanical allodynia, and this action was abolished by muscarinic antagonist pirenzepine (i.c.v.). Treatment with 1-10 μg/kg donepezil (i.p.), which can easily penetrate into the brain, also showed similar therapeutic effects. (healthrising.org)

Such effect was completely reversed both by the opioid receptor antagonist naloxone and by the unselective muscarinic receptor antagonist atropine. (researchgate.net)

Additional acyl compounds were tested using a murine model in which IL-1 levels were decreased and latency of paw withdrawal was increased, indicating effective reductions in tactile allodynia, and hyperalgesia when tested using the Ching and CFA models. (afl-journal.org)

Several screening tools for study of receptor mechanism with agonist and antagonist have been developed. (stmjournals.in)
The selective GPR30 agonist G1 and antagonist G15 were locally microinjected into the PAG. (biomedcentral.com)
The B 1 agonist, des-Arg 9 -BK, produced a small exacerbation of hyperalgesia in both models. (cmich.edu)
The B1 agonist, des-Arg9-BK, produced a small exacerbation of hyperalgesia in both models. (cmich.edu)

for which patents have been applied since 2006, from the following groups: benzamide inhibitors, bicycloheteroaryl compounds, acylhdranzine antagonists, biaromatic P2X7 antagonists, heterocyclic compounds and amide derivatives, and aromatic amine antagonists. (afl-journal.org)

Two of the most commonly used opioid antagonists at the mu receptor are naltrexone and naloxone. (wikipedia.org)
Studies in healthful human beings demonstrate that naloxone, a particular opiate antagonist, reverses acupuncture analgesia (Jiang et al. (gasyblog.com)

Moreover, study with knockout and transgenic mice so far contributed in this regard suggests possibility of PAR2 selective antagonist as a useful drug for the treatment of pain and inflammatory disorders. (stmjournals.in)
2004), show that EA creates anti-hyperalgesia in inflammatory discomfort pet versions (Yang et al. (gasyblog.com)
2002). It's been demonstrated the fact that vertebral opioid receptor antagonist D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2 (CTOP) blocks 10 and100 Hz EA-produced anti-hyperalgesia within a comprehensive Freunds adjuvant (CFA)-induced inflammatory discomfort rat model, as the receptor antagonist nor-binaltorphimine (Nor-BNI) will not (Zhang et al. (gasyblog.com)

CI-1021 ([(2-benzofuran)-CH 2 OCO]-( R )-α-MeTrp-( S )-NHCH(CH 3 )Ph) is a selective and competitive neurokinin-1 (NK 1 ) receptor antagonist. (aspetjournals.org)
CPZ-induced calcium transients in human TRPA1-expressing HEK293t cells were blocked by the selective TRPA1 antagonists HC 030031 and A967079 and involved three cysteine residues in the N-terminal domain. (nature.com)
It has been shown that estrogen-induced mechanical hyperalgesia is produced by selective agonists of the GPR30 receptor, and is inhibited by knockdown of the GPR30 receptor [ 7 ]. (biomedcentral.com)

In opioid-induced hyperalgesia, sensitization of pronociceptive mechanisms occurs, resulting in a decrease in the pain threshold, or allodynia. (wikipedia.org)
They play important roles in the pain pathway where in concert with proinflammatory factors such as leukotrienes they mediate sensitization and hyperalgesia. (researchgate.net)
mediate sensitization and hyperalgesia. (researchgate.net)

Described herein are methods and compositions relating to inhibition of mechanically-induced TRPV4 activation, e.g., for the treatment of pulmonary edema, edema, inflammation, hypertension, and/or hyperalgesia. (google.com)

Hyperalgesia is an exaggerated response to noxious stimuli produced by peripheral or central plasticity. (nature.com)
Hyperalgesia is an exaggerated and prolonged response to noxious stimuli that can be produced by plasticity at peripheral sites (eg, reduced threshold and/or amplified nociceptor response to noxious stimuli) and centrally in the spinal cord or brain. (nature.com)

Inhibition by specific antagonists indicates that continuing activation of cAMP-PKA and cGMP-PKG pathways is required to maintain hyperexcitability after dissociation. (nih.gov)

11 Furthermore, we previously demonstrated that the prevention of mast cell degranulation largely reduced hyperalgesia in a model of postoperative pain. (asahq.org)

Whereas increasing the dose of opioid can be an effective way to overcome tolerance, doing so to compensate for opioid-induced hyperalgesia may worsen the patient's condition by increasing sensitivity to pain while escalating physical dependence. (wikipedia.org)
‌The main symptom of hyperalgesia is high sensitivity to pain. (webmd.com)

Tolerance, another condition that can arise from prolonged exposure to opioids, can often be mistaken for opioid-induced hyperalgesia and vice versa, as the clinical presentation can appear similar. (wikipedia.org)
Identifying the development of hyperalgesia is of great clinical importance since patients receiving opioids to relieve pain may paradoxically experience more pain as a result of treatment. (wikipedia.org)
PERSPECTIVE: Remifentanil-induced hyperalgesia is common even when used within clinical accepted doses. (iasp-pain.org)
[1] Specific clinical features include allodynia , hyperalgesia, sudomotor and vasomotor abnormalities, and trophic changes. (physio-pedia.com)
In light of these new tools, it is important to keep in mind that expected antagonist effects may be different from those in pre-clinical studies due to the variable extracellular environments encountered in different disease states. (afl-journal.org)
Despite the advances in understanding PAR2 pharmacology, it has taken almost 25 years for the first inhibitor to reach clinical trials, and so far, no PAR2 antagonist has been approved for human use. (silverchair.com)

Predator odor stress produces hyperalgesia in rodents. (nature.com)

a recent evaluate by Prof. Burnstock provides an in-depth summary of many currently available P2 receptor agonists and antagonists, and their potential uses in the treatment of CNS disorders [119]. (afl-journal.org)
Research has employed classical approaches to develop a wide array of PAR2 agonists and antagonists, consisting of peptides, peptoids and antibodies to name a few, with a surge in patent applications over this period. (silverchair.com)

Opioid-induced hyperalgesia (OIH) or opioid-induced abnormal pain sensitivity, also called paradoxical hyperalgesia, is an uncommon condition of generalized pain caused by the long-term use of high dosages of opioids such as morphine, oxycodone, and methadone. (wikipedia.org)
If you take opioids or opioid painkillers , you can develop opioid-induced hyperalgesia. (webmd.com)
‌The symptoms of opioid-induced hyperalgesia depend on the dose of opioids you take. (webmd.com)
Opioids like methadone , oxycodone , or tramadol are reported to be effective against opioid-induced hyperalgesia. (webmd.com)

Because TRPV4 appears to be more important in pathological pain conditions than in normal mechanical nociception, we investigated whether TRPV4 also is involved in mechanical hyperalgesia associated with painful peripheral neuropathy. (jneurosci.org)

Iron chelation may be a potential therapeutic strategy for the prevention of hyperalgesia in populations at high risk. (iasp-pain.org)
This mechanism might be a potential novel therapeutic target for hyperalgesia in females. (biomedcentral.com)

This study tested the beneficial effects of the non-peptide and orally active kinin B 1 receptor antagonist SSR240612 against tactile and cold allodynia in a rat model of insulin resistance. (johnshopkins.edu)
Publication of the first crystal structures of PAR2 resolved in complex with two novel non-peptide small molecule antagonists (AZ8838 and AZ3451) revealed two distinct binding pockets, originally presumed to be allosteric sites, with a PAR2 antibody (Fab3949) used to block tethered ligand engagement with the peptide-binding domain of the receptor. (silverchair.com)

With hyperalgesia, things that normally cause pain feel more painful than usual. (webmd.com)
Allodynia is different from hyperalgesia , an extreme, exaggerated reaction to a stimulus which is normally painful. (eclecticme.org)

In addition, what appears to be opioid tolerance can be caused by opioid-induced hyperalgesia lowering the baseline pain level, thus masking the drug's analgesic effects. (wikipedia.org)
‌The symptoms of opioid-induced hyperalgesia can be confused with those of opioid tolerance. (webmd.com)

Thus it's important to investigate systems of EA anti-hyperalgesia under pathological Rabbit Polyclonal to GANP circumstances. (gasyblog.com)

However, the conclusion of a report published in the Journal of Pain & Palliative Care Pharmacotherapy suggests that "[h]yperalgesia shares a common mechanism with tolerance and it may be that hyperalgesia is a manifestation of tolerance itself. (wikipedia.org)

Although tolerance and opioid-induced hyperalgesia both result in a similar need for dose escalation to receive the same level of effect to treat pain, they are nevertheless caused by two distinct mechanisms. (wikipedia.org)
Under chronic opioid treatment, a particular individual's requirement for dose escalation may be due to tolerance, opioid-induced hyperalgesia, or a combination of both. (wikipedia.org)
However, chronic opioid use can result in analgesic tolerance, hyperalgesia, and other side effects, which seriously affect the safety and comfort of patients [ 2 ]. (hindawi.com)

They make you more sensitive to pain and increase your risk of developing hyperalgesia. (webmd.com)
But with opioid-induced hyperalgesia, increasing the opioid dose will further increase your pain. (webmd.com)
Your doctor will immediately suspect opioid-induced hyperalgesia if you experience extreme pain after increasing your opioid dose. (webmd.com)
Some studies have even supported the possible role of long term opioid treatment in the development of hyperalgesia and allodynia which further exacerbate pain syndromes (66). (pancreapedia.org)

Secondary hyperalgesia. (webmd.com)

Recent results indicate that after chronic compression of DRG (CCD treatment), both hyperexcitability of neurons in intact DRG and behaviorally expressed hyperalgesia are maintained by concurrent activity in cAMP-protein kinase A (PKA) and cGMP-protein kinase G (PKG) signaling pathways. (nih.gov)

Taxol-induced TRPV4-mediated hyperalgesia and the enhanced osmotransduction in cultured nociceptors were dependent on integrin/Src tyrosine kinase signaling. (jneurosci.org)

If your hyperalgesia is caused by opioid use, your doctor will have you gradually decrease your opioid dose. (webmd.com)

This study presents that aberrant iron accumulation is involved in the development of remifentanil-induced hyperalgesia in vivo and in vitro. (iasp-pain.org)
This blocked the development of mechanical hyperalgesia and NGF mRNA upregulation not only after the first LC but also after the second LC. (painscience.com)
The specific B 1 antagonist, des-Arg 9 , [Leu 8 ]-BK, was effective in reversing or preventing the development of hyperalgesia in both Freund's adjuvant-induced hyperalgesia and UV-induced hyperalgesia. (cmich.edu)

Kainic acid injected subcutaneously in the back of mice decreased response latencies in the hot plate and tail flick assays, indicating that hyperalgesia is achieved by a variety of parenteral routes of injection. (biopsychiatry.com)
We are examining IT gp120 allodynia & hyperalgesia after an IT microglia-specific toxin (Saporin-linked Mac-1 antibody) injection that disrupts glial function. (atsbio.com)

This study aims to investigate the role of iron accumulation in remifentanil-induced hyperalgesia. (iasp-pain.org)

We then injected HOE140, a B2R antagonist with effects lasting only several hours, once before the first LC. (painscience.com)

G-protein coupled estrogen receptor 30 (GPR30) was proved the specific estrogen receptor relating to mechanical hyperalgesia. (biomedcentral.com)

The addition of the cyclohexylmethyl or cyclohephylmethal groups to the biaromatic-amide derivatives allows for high P2X7 receptor antagonist activity as assessed by their ability to inhibit BzATP-induced P2X7-dependent pore activity as assessed by ethidium bromide uptake. (afl-journal.org)

Antagonist activity at both the human and rat P2X7 receptor was shown to be comparable for one quinoline derived acyl hydrazide compound derivative (1-(4 methoxyphenyl)cyclohexyl). (afl-journal.org)

We also demonstrate that Taxol-induced TRPV4-mediated hyperalgesia is essentially dependent on integrin/Src tyrosine kinase signaling. (jneurosci.org)

When administered i.p., 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX), an (R,S)-alpha-amino-3-hydroxy-5-methylisoxazole-4-proprionic acid HBr/kainate (AMPA/KA) antagonist, completely blocked hyperalgesia. (biopsychiatry.com)
Furthermore, repeated donepezil treatments completely cured the ICS-induced hyperalgesia and allodynia even after the cessation of drug treatments. (healthrising.org)

Anatomy23

Organisms7

Diseases24

Chemicals and Drugs158

Analytical, Diagnostic and Therapeutic Techniques and Equipment23

Psychiatry and Psychology9

Phenomena and Processes19

Disciplines and Occupations1

Technology, Industry, Agriculture1

Health Care3

Receptor antagonists8

Rats14

Receptors7

Allodynia and thermal hyperalgesia2

NMDA6

Induce hyperalgesia1

Stress-induced hyperalgesia3

Thermal4

Muscarinic receptor a1

Tactile allodynia1

Agonist4

Inhibitors1

Naloxone2

Inflammatory3

Selective3

Sensitization3

Inflammation1

Stimuli2

Inhibition1

Postoperative1

Sensitivity to pain2

Clinical6

Rodents1

Agonists2

Opioids4

Nociception1

Therapeutic2

Peptide2

Painful2

Opioid tolerance2

Pathological1

Mechanism1

Tolerance3

Pain4

Secondary1

Neurons1

Nociceptors1

Dose1

Development3

Injection2

Investigate1

Effects1

Specific1

High1

Activity1

Demonstrate1

Completely2