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)

Previous work has shown that activation of catecholamine in the preoptic area is to the disadvantage of acupuncture analgesia. In this work microinjection and push-pull perfusion as well as HPLC-ECD were used to observe the effect of noradrenaline and dopamine in this area on acupuncture analgesia. The results indicated that microinjection of noradrenaline (0.5 microgram/unilateral) into the preoptic area could attenuate acupuncture analgesia, while dopamine (2 micrograms/unilateral) had no effect on acupuncture analgesia. During acupuncture analgesia, the contents of noradrenaline and MHPG in the perfusate from the preoptic area were markedly decreased, and that of dopamine, however, was not changed significantly. The above results suggest that activating noradrenaline, but not dopamine, exerts antagonistic effect on acupuncture analgesia.
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PMID:[Effects of noradrenaline and dopamine in preoptic area on acupuncture analgesia]. 212 59

RIA and HPLC-ECD were used respectively to detect beta-endorphin-like immunoreactive substances (beta-EPIS), noradrenaline and 3-methoxy-4-hydroxyphenyloglycol (MHPG), a noradrenaline metabolite, in the perfusate from the rabbit's preoptic area before and after 10 min of electroacupuncture (EA). It was found that, the content of beta-EPIS in the perfusate increased during acupuncture analgesia, while those of noradrenaline and MHPG decreased. A negative correlation (r = -0.831; P less than 0.05) was shown between the changes of beta-EPIS and MHPG contents during acupuncture analgesia, indicating that beta-endorphin may be related to the inhibition of noradrenaline release during acupuncture analgesia.
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PMID:[Changes of releases of beta-endorphin-like immunoreactive substances and noradrenaline in rabbit's preoptic area during acupuncture analgesia]. 214 11

The present study was to investigate the effect of metoclopramide (MCP) on electroacupuncture analgesia (EAA) and its mechanism on a rabbit visceral pain model. The results showed that MCP 8mg/kg i.v. could potentiate EAA and prolong the analgesic duration. The potentiation effect could be attenuated by icv apomorphine (APO) (a mixed D1/D2 agonist). The analgesic duration was shortened by icv SKF38393 (a selective D1 agonist) or LY171555 (a selective D2 agonist). Using HPLC-ECD, we also found that the HVA content in CSF significantly increased at 20 min. after electroacupuncture (EA) or MCP 8mg/kg i.v. (P < 0.05), but the change of HVA content was not significant when EA and MCP 8mg/kg i.v. were used together. All these observations indicate that MCP have effects of potentiating EAA and prolonging analgesic duration. These effects are related to the blockade of the central DA receptor. The activations of D1 or D2 receptor is unfavourable to the expression of EA after effect.
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PMID:[Potentiation of electroacupuncture analgesia on visceral pain by metoclopramide and its mechanism]. 783 58

We and others previously reported that the antinociceptive effect of clonidine, measured by the hot plate method, was greater in spontaneously hypertensive rats (SHRs) than in Wistar-Kyoto rats (WKYs). In the present study, we found that the difference in clonidine-induced analgesia between these two strains was abolished after lesioning the presynaptic noradrenergic neurons with N-(2-chloroethyl)-N-ethyl-2-bromobenzylamine (DSP4). Previous studies indicated that clonidine increases tissue norepinephrine (NE) content by inhibiting NE release. We found that the basal NE concentration in locus coeruleus (LC), as measured by HPLC-ECD, was not different between WKYs and SHRs. Systemic application of clonidine (0.69 mg/kg, I.P.) significantly increased the tissue content of NE in the SHRs, but not in WKYs. Using pressure microinjection and high-speed chronoamperometric recording techniques, we found that local application of KCl to the LC brain slices increased extracellular NE levels in both strains. Perfusion of slices with clonidine (1 microM) selectively attenuated KCl-evoked NE release in SHRs, suggesting that clonidine-induced presynapitc inhibition is more effective in SHRs than in WKYs. In conclusion, our data indicate that SHRs possess augmented sensitivity to clonidine to inhibit presynaptic NE release, which may be responsible for the enhanced antinociceptive effect of clonidine in this strain.
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PMID:Enhanced antinociception of clonidine in spontaneously hypertensive rats involves a presynaptic noradrenergic mechanism. 944 44

The pharmacokinetic parameters of buprenorphine (BN) after a single bolus dose of 10 microg/kg i.v. was investigated in 6 male patients whose age averaged 59+/-9.8 years and body weight of 65.8+/-5.7 kg undergoing coronary artery bypass graft surgery (CABG). The unbound BN plasma concentrations were detected using ultrafiltration and high performance liquid chromatography/electro-chemical detection (HPLC/ECD) method. During cardiopulmonary bypass (CPB) there was a fall in BN plasma concentrations, observations similar to reports on fentanyl, sufentanil and alfentanil. This is probably due to haemodilution, hypothermia and hydrophobic sequestration of drug on to the CPB tubing. After CPB the concentrations rose to values higher than during CPB, though it did not attain pre CPB concentrations. These variations were not statistically significant indicating that plasma levels were adequately stable during CPB. The plasma concentration time curves were biexponential and the pharmacokinetic parameters obtained were : distribution half-life 37.24+/-6.57 min, elimination half-life 482.69+/-79 min, clearance 1221.97+/-209.42 ml/min, and volume of distribution 736.46+/-71.25 L. BN in the dose used follows the pharmacokinetic pattern of other commonly used narcotics during CABG. The mean +/- SEM plasma BN concentration during CPB was 0.51+/-0.03 ng/ml which was adequate for the maintenance of analgesia and anaesthesia, as none of our patients expressed the signs and symptoms of awareness during surgery. Further, unlike the other narcotics muscle rigidity was absent. Thus BN is a safe and good alternative to other narcotics for patients undergoing CABG.
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PMID:Buprenorphine pharmacokinetic parameters during coronary artery bypass graft surgery. 1023 58

The Bennett and Xie model of peripheral nerve injury was used to study the effects of aging on the onset and progression of sciatic nerve ligation (SNL)-induced thermal hyperalgesia and tactile-evoked allodynia in young, mature, and aged Fischer 344 FBNF1 male rats (4-6, 14-16, and 24-26 months old, respectively). A plantar analgesia meter and calibrated von Frey pressure filaments were employed as the analgesiometric assays. In the absence of nerve injury, aged rats were found to be more sensitive than younger animals to noxious thermal stimuli. Following the SNL surgery, thermal hyperalgesia was observed in all three age groups within 3 days. On post-SNL day 35, the paw-withdrawal latency values of the young and mature animals returned to presurgical baseline levels, while the aged rats continued to exhibit thermal hyperalgesia. Tactile-evoked allodynia was apparent within 3 days following peripheral nerve injury in the oldest cohort, but was delayed in the younger animals. On post-SNL days 0 (control), 3, 21, and 35, young, mature, and aged rats were sacrificed and high-performance liquid chromatography and electrochemical detection (HPLC/ECD) methods were used for neurochemical analyses of spinal serotonin (5-HT), norepinephrine (NE), and 5-hydroxyindoleacetic acid (5-HIAA). Spinal 5-HT and NE levels were not significantly altered by the aging process, nor were they affected by peripheral nerve injury. However, spinal 5-HT turnover from the aged animals was greater than that detected in spinal tissue from the younger counterparts. Differences in spinal 5-HT turnover may contribute to age-related variability in spinal nociceptive processing.
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PMID:Changes in spinal serotonin turnover mediate age-related differences in the behavioral manifestations of peripheral nerve injury. 1097 28

P-glycoprotein (P-gp), one of the important drug-efflux pumps, is known to affect pharmacokinetics and pharmacodynamics of P-gp substrate drugs. We have previously reported that intestinal P-gp expression levels are transiently decreased in streptozotocin (STZ)-induced type 1 diabetic mouse model. Herein, we examined the analgesic effects of orally administered morphine and its pharmacokinetic properties under diabetic conditions, specifically focusing on the involvement of intestinal P-gp in a type 1 diabetic mouse model. Type 1 diabetes was induced in male ddY mice by an i.p. injection of STZ (230 mg/kg). We assessed the oral morphine analgesia using the tail-flick test. Serum and brain morphine content were determined on a HPLC-ECD system. Intestinal P-gp expression levels were significantly decreased on day 9 after STZ administration. On the other hands, oral morphine analgesia, and serum and brain morphine content were significantly increased on day 9 after STZ administration. The decrease in the intestinal P-gp expression levels were suppressed by aminoguanidine, a specific iNOS inhibitor. Interestingly, the increase in the analgesic effect of morphine, as well as serum and brain morphine content, was suppressed by aminoguanidine. Conversely, there was no change in the analgesic effect obtained with subcutaneous morphine in STZ-treated mice. In conclusions, our findings suggest that the oral morphine analgesia is dependent on intestinal P-gp expression, and that may be one of the problems against obtaining stable pharmacological effects of morphine in diabetic patients.
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PMID:[Altered intestinal P-glycoprotein expression levels affect pharmacodynamics under diabetic condition]. 2229 93