Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0344307 (analgesia)
 28,200 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The action of electroacupuncture (EA) may be similar to analgesia by electrode stimulation or transcutaneous nerve stimulation. Since EA may directly stimulate nerve activity or indirectly enhance the release of opiate peptides and other neurotransmitter substances, we have used (Na+ + K+)-ATPase as a model to study the mechanism of action of EA. The membrane-bound (Na + K)-ATPase from purified synaptic plasma membranes inhibited slightly by high concentration of endorphin (30 microM), but not by met-enkephalin up to 6 X 10(-4) M. A single EA treatment for 30 min did not alter the (Na+ + K+)-ATPase activity in the cerebral cortex. However, when rats were treated with low (4 Hz) or high (200 Hz) frequency EA 30 min daily for 3 weeks, both (Na+ + K+)-ATPase and acetylcholinesterase were significantly elevated. The enhanced (Na+ + K+)-ATPase activity after high frequency EA was only partially blocked by i.p. injection of naloxone prior to EA during the last week of the EA treatment program. The results indicated that EA treatment may involve some other neurotransmitter pathways besides opiate peptides.
 ...
PMID:Effect of electroacupuncture on synaptosomal (Na+ + K+)-ATPase. 614 70

We have previously observed that, while acute stress induces analgesia, chronic stress causes a hyperalgesic response in male rats. No effect was observed in females. There is increasing evidence that both ATP and adenosine can modulate pain. Extracellular ATP and ADP are hydrolyzed by an apyrase in synaptosomes from the peripheral and central nervous systems. In the present study, we investigated the effect of chronic and acute stress on ATPase-ADPase and 5'-nucleotidase activities in spinal cord of male and female rats. Adult male and female Wistar rats were submitted to 1 h restraint stress/day for 1 day (acute) or 40 days (chronic) and were sacrificed 24 h later. ATPase-ADPase activities were assayed in the synaptosomal fraction obtained from the spinal cord of control and stressed animals. ADP hydrolysis was decreased 25% in chronically stressed males, while no change was observed on ATPase activity. There was an increase in the 5'-nucleotidase activity in the same group. No effect on ADPase, ATPase or on 5'-nucleotidase activity was observed in females with chronic stress, or after acute stress neither in males or females. Chronic stress reduced ADP hydrolysis and increased 5'-nucleotidase activity in the spinal cord in male rats.
 ...
PMID:Effect of chronic and acute stress on ectonucleotidase activities in spinal cord. 1189 Sep 46

It is known that opioid analgesics given systemically have limited distribution into the brain because of their interaction with P-glycoprotein (P-gp), an ATP-dependent efflux pump acting at the blood-brain barrier (BBB). We previously found that morphine and fentanyl showed higher analgesic potencies in P-gp-deficient mice compared with those in wild-type mice, suggesting that their analgesic effects are considerably dependent on P-gp expression. In this study, we focused on individual differences in the analgesic effectiveness of morphine, in cortical P-gp expression, and in basal P-gp ATPase activity in male ICR mice. We found that there were 3- to 10-fold differences between the magnitude of morphine analgesia (3 mg/kg, s.c.; tail-pinch method) in mice. Furthermore, there was a significant negative correlation between morphine's analgesic effects and individual P-gp expression in the cortex as estimated by western blot analysis. In addition, basal P-gp ATPase activities in isolated membrane preparations of brain capillary endothelial cells (BCECs) were negatively correlated with the magnitude of the analgesic effect of morphine. These results indicate that the individual differences in morphine analgesia may be due to some functional or quantitative differences in individual P-gp in BCECs, acting at the BBB.
 ...
PMID:Negative relationship between morphine analgesia and P-glycoprotein expression levels in the brain. 1807 Dec 74

It has been documented that adenosine triphosphate (ATP) is a multifunctional nucleoside triphosphate used in cells, including chemical energy transportation, extra- and intracellular signaling, cell structure maintaining, DNA and RNA synthesis, etc. In the present paper, the authors reviewed studies on the involvement of ATP in different efficacies of acupuncture intervention from the following four aspects. 1) ATP release in the stimulated acupoint area is one of the key factors for producing acupuncture analgesia; 2) Acupuncture induced suppression of ATP activity in the central nervous system results in pain relief; 3) ATP application on the human body surface may strengthen the sensation propagation along the meridian; 4) Favorable regulation of acupuncture intervention on the abnormal functional activities of some viscera often accompanies with an increase of ATP content and ATPase activity in the related internal organs. It has been proposed that ATP, Ca2+ and reactive oxygen species (ROS) are closely related each other in the life activities of the organism. Hence, a reasonable regulation on ATP levels in the related organs of the body may be a new approach for raising clinical therapeutic effects of acupuncture therapy.
 ...
PMID:[A review of recent researches on correlation between ATP and acupuncture efficacies]. 2314 59

Benzimidazole is an important pharmacophore for clinically active drugs against inflammation and treatment of pain, however, it is associated with gastrointestinal side effects. Here we synthesized benzimidazole based agents with significant analgesic/anti-inflammatory potential but with less gastrointestinal adverse effects. In this study, we synthesized novel, orally bioavailable 2-mercaptobenzimidazole amino acid conjugates (4a-4o) and screened them for analgesic, anti-inflammatory and gastro-protective effects. The synthesized 2-mercaptbenzimidazole derivatives were characterized for their structure using FTIR, 1 H NMR and 13 C NMR spectroscopic techniques. The 2-mercaptobenzimidazole amino acid conjugates have found to possess potent analgesic, anti-inflammatory and gastroprotective activities, particularly with compound 4j and 4k. Most of the compounds exhibited remarkable anti-ulcer and antisecretory effects. Molecular docking studies were carried out to study the binding affinities and interactions of the synthesized compounds with target proteins COX-2 (PDB ID: 3LN1) and H+ /K+ -ATPase (PDB ID: 5Y0B). Our results support the clinical promise of these newly synthesized 2-mercaptobezimidazol conjugates as a component of therapeutic strategies for inflammation and analgesia, for which the gastric side effects are always a major limitation.
 ...
PMID:Amino acid conjugates of 2-mercaptobenzimidazole provide better anti-inflammatory pharmacology and improved toxicity profile. 3278 Apr 91