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

The effects of centrally administered kentsin (H-Thr-Pro-Arg-Lys-OH) on intestinal motility and on pain perception were investigated in rats chronically equipped with lateral ventricle catheters. Intestinal motility was recorded electromyographically from electrodes placed on the duodeno-jejunum; analgesia was evaluated by the hot-plate and tail-flick tests. Kentsin (4.0 ug/kg), injected intracerebroventricularly (ICV) 2 hours after the beginning of a meal, restores the "fasted" i.e. the migrating myoelectric complex of intestinal motility, while a 5 times higher dose administered subcutaneously was inactive. The ICV effect of kentsin was blocked by previous ICV administration of naloxone (400 ug/kg). In contrast, kentsin administered ICV (40 ug/kg) or SC (200 ug/kg) did not affect significantly (P greater than 0.05) the time latency in the two analgesic tests during 90 minutes after its administration and did not significantly modify the analgesic effects of (D5-Ala2, Met5) enkephalinamide. We conclude that kentsin when centrally administered acts on opiate receptors to alter gastrointestinal motility but without effects on pain perception.
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PMID:A tetrapeptide isolated from hamster embryo with central opiate properties on gastrointestinal motility but not on pain perception. 301 51

Free amino acids in muscle were studied before and 96 hours after skin incision in 14 patients undergoing elective hip replacement and allocated to general anesthesia or epidural analgesia (T10-S5) effective before incision and maintained with intermittent 0.5% bupivacaine during the first 24 postoperative hours. The general anesthesia group (n = 8) showed the characteristic changes in muscle amino acids, with increase of branched chain amino acids and phenylalanine and decreased glutamine, arginine and lysine, as well as raised plasma levels of cortisol and glucose. The epidural group (n = 6), contrastingly, showed no significant changes in plasma cortisol and glucose and an attenuated postoperative response in all amino acids, without significant difference from the preoperative values. Differences in postoperative muscle amino acid concentrations between the epidural and the general anesthesia group were significant as regards glutamine, valine and asparagine. These results suggest that post-trauma changes in muscle amino acids are predominantly mediated by afferent neurogenic stimuli and the secondary increase in catabolic hormones.
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PMID:Effect of epidural analgesia on muscle amino acid pattern after surgery. 353 54

Kyotorphin (Tyr-Arg) is a unique neuropeptide which produces analgesia by releasing Met-enkephalin from slices of the brain and spinal cord. Recent studies revealed that kyotorphin possesses the properties of neurotransmitter/neuroregulator. In the present study, we identified a kyotorphin synthetase in the soluble fraction of rat brain synaptosomes (synaptosol) and characterized it. The enzyme partially purified with Sephacryl S-300 showed an absolute requirement for ATP, MgCl2, tyrosine, and arginine. The optimal pH was 7.5-9.0 and the pI was determined to be 6.1-6.2 by isoelectric focusing. The Km was 25.6 microM for tyrosine, 926 microM for arginine, 294 microM for ATP, and 442 microM for MgCl2. The Vmax was 34.0 pmol/mg of protein/h. The apparent molecular size of this "kyotorphin synthetase" further purified by the DE52 column was 240,000-245,000 daltons, estimated using TSKgel G4000SW column chromatography. The enzyme reaction is represented by the following equation: Tyr + Arg + ATP + MgCl2 + kyotorphin synthetase----Tyr-Arg (kyotorphin) + AMP + PPi + MgCl2 + kyotorphin synthetase. The regional distribution and subcellular localization of the synthetase showed a close correlation to that of kyotorphin levels in the rat brain. The amounts of kyotorphin formed from amino acids by the synthetase in the dialyzed synaptosol was 3.0-4.0 times higher than that from precursor proteins by processing enzymes within the 30 min incubation.
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PMID:Kyotorphin (tyrosine-arginine) synthetase in rat brain synaptosomes. 359 66

Complement activation was studied in 45 patients undergoing total hip arthroplasty under epidural anesthesia. The patients were randomly allocated to three groups. In Group I blood loss was replaced with microaggregate-poor erythrocyte concentrate (SAGM-ERC) plus 3% dextran-60 as plasma substitute, and postoperative analgesia was maintained with intramuscular ketobemidone. In Group II blood loss was replaced as in Group I, but epidural anesthesia was prolonged 12 h postoperatively and kept at a level of T4 with 0.5% bupivacaine. In Group III blood loss was replaced with non-frozen stored plasma plus SAGM-ERC, and postoperative analgesia was maintained with ketobemidone as in Group I. All groups received pre- and postoperative thrombo-prophylaxis with dextran. The plasma concentration of C3a-des-arginine (C3a-desArg) was measured by radioimmunoassay preoperatively, immediately after operation and 3, 6 and 18 h postoperatively. No significant differences in plasma C3 and C4 were found between the groups. C3a-desArg was significantly (P less than 0.01) increased up to 6 h postoperatively in Group III compared with both the preoperative value and Groups I and II. It is demonstrated that infusion of plasma can enhance or initiate endogenous complement activation. Blood component therapy with SAGM-ERC and 3% dextran-60, on the other hand, did not significantly increase the plasma level of C3a-desArg irrespective of the type of postoperative analgesia.
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PMID:Blood substitution and complement activation. 368 52

Phe-Met-Arg-Phe-NH2 (FMRF-NH2) was initially isolated from the macrocallista nimbosa clam and subsequently existence of FMRF-NH2-like immunoreactivity (FMRF-NH2-IR) was detected in mammalian CNS. Due to the structural similarity between FMRF-NH2 and the C-terminal extended form of met5-enkephalin, met5-enkephalin-arg6-phe7 (YGGFMRF), a possible interaction between these two peptides was explored. FMRF-NH2 injected intrathecally decreases the antinociceptive action of YGGFMRF or morphine. However, the FMRF-NH2-IR present in rat and bovine brains differs from FMRF-NH2. Intrathecally injected FMRF-NH2-IR partially purified from bovine brain reduces YGGFMRF antinociception. The antagonism elicited by FMRF-NH2 can be reversed by proglumide, which was reported to act as a CCK antagonist. In order to characterize the biological profile of FMRF-NH2-IR, the effect of proglumide and of the FMRF-NH2 antibody on morphine analgesia was tested. Both the IgG isolated from FMRF-NH2 antiserum and proglumide were found to potentiate the morphine analgesia. The results taken together suggest that endogenous FMRF-NH2-IR modulates opioid antinociception; perhaps by acting as an endogenous naloxone.
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PMID:Are Phe-Met-Arg-Phe-NH2 immunoreactive peptides endacoids modulating opiate antinociception? 390 60

Kyotorphin (Tyr-Arg) was rapidly degraded in rat brain homogenates and the Vmax and Km were 29.4 nmol/mg protein/min and 16.6 microM, respectively. This degradation was effectively inhibited by bestatin (IC 50; 0.08 microM) and p-chloromercuribenzoate (IC 50; 0.70 microM). Kyotorphin was also degraded by a membrane-bound aminopeptidase from monkey brains. The Vmax and Km of kyotorphin degradation by the aminopeptidase were 20.0 nmol/mg protein/min and 29.2 microM, respectively. The degradation of kyotorphin was also inhibited effectively by bestatin (KI; 0.4 microM). Co-administration with bestatin 50 micrograms (i.cist.) potentiated the analgesic effects of kyotorphin (i.cist.) by 4.8 times, and these effects were abolished by pretreatment with naloxone 0.5 mg/kg s.c. These results suggest that potentiation of analgesia by bestatin may be due to the protection against the degradation of kyotorphin and released enkephalin by a membrane-bound aminopeptidase.
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PMID:Degradation of kyotorphin by a purified membrane-bound-aminopeptidase from monkey brain: potentiation of kyotorphin-induced analgesia by a highly effective inhibitor, bestatin. 399 May 13

Social conflict and defeat in mice leads to an activation of endogenous opiate systems. The effects of intracerebroventricular administration of the peptide FMRFamide (Phe-Met-Arg-Phe-NH2) and the opiate antagonist naloxone, on aggressive encounters, defeat-induced analgesia and defeat-induced feeding were examined in male mice. Both substances reduced the number of bites required to cause defeat in subordinate mice during aggressive encounters, as well as suppressing the subsequent defeat-induced analgesia. Administration of FMRFamide or naloxone also reduced defeat-induced feeding. These results indicate that FMRFamide (or FMRFamide-like neuropeptides) may function as endogenous opioid antagonists.
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PMID:FMRFamide, a putative endogenous opiate antagonist: evidence from suppression of defeat-induced analgesia and feeding in mice. 408 Jan 10

Analgesia, opiate receptor binding, and neurochemical effects of kyotorphin (tyrosine-arginine) were studied in the rat. It was found that while kyotorphin, in vivo, causes naloxone reversible analgesia, and affects dopamine metabolism and acetylcholine turnover in the same manner as do morphine and other opiate agents, the dipeptide does not bind to mu, delta or kappa opiate receptors in vitro. Taken together, these data support the concept that there is an indirect action of kyotorphin on opiate receptors.
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PMID:Kyotorphin (tyrosine-arginine): further evidence for indirect opiate receptor activation. 628 89

The analgesic actions of some synthetically prepared peptides having the Tyr-D-Arg unit at the N terminal portion of met- and leu-enkephalin were measured by the intra-cisternal injection method in mice. Among them, Tyr-D-Arg-Gly-Phe (DR-4) induced the most potent naloxone-reversible analgesia and was also effective by s.c. injection. DR-4 showed the good affinity to mu-receptor, and the resistance to the enzymatic degradation.
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PMID:Morphine-like analgesic actions of enkephalin-like peptides containing the Tyr-Arg unit. 629 21

The pharmacological activity of eight analogues of enkephalin containing L-Arg or D-Arg in position 2 were examined. All peptides showed weaker inhibitory effects than those of naturally-occurring enkephalins on the isolated guinea-pig ileal longitudinal muscle and the mouse vas deferens. On the contrary, these eight peptides were more potent than enkephalins in the analgesic test involving intracisternal administration to mice. By the intravenous route, only D- Arg2 -Met5-enkephalin, which induced a most potent analgesia by intracisternal injection, was effective. D- Arg2 -Met5-enkephalin showed a similar binding affinity to that of Met5-enkephalin in the opioid mu-receptor binding assay, but had a lower delta-receptor binding affinity than did Leu5-enkephalin. Administration of thiorphan , an enkephalin dipeptidyl carboxypeptidase inhibitor, did not potentiate the analgesic effect of D- Arg2 -Met5-enkephalin, whereas it dramatically enhanced the effect of D-Ala2-Met5-enkephalin, when both drugs were administered concomitantly into the cisterna magna of mice.
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PMID:Opioid activity of enkephalin analogues containing the kyotorphin-related structure in the N-terminus. 632 51


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