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)

Intracerebroventricular administration of the synthetic dipeptide derivative Lys-Trp (Nps) (LTN) elicits a potent and naloxone-sensitive antinociceptive effect in mice and in rats using heat and electrical current respectively as the noxious stimuli. LTN does not induce analgesia by directly acting on opioid receptors but the peptidase inhibiting activity of the new compound may account in part for the behavioral effect. LTN produces also a marked decrease in the met-enkephalin content of the periaqueductal gray suggesting a possible enkephalin releasing property. Structure-activity studies with different analogs of LTN indicate that replacement of Lys by other basic amino acids results also in compounds with a potent antinociceptive effect whereas replacement by neutral or acidic amino acids leads to a complete loss of activity.
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PMID:Antinociceptive effects in rodents of the dipeptide Lys-Trp (Nps) and related compounds. 301 88

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

The effects of lysine acetylsalicylate, a new injectable salicylate, on postoperative pain relief and platelet function were studied in ten men who had surgery for peptic ulcer. Four of five patients receiving lysine acetylsalicylate had satisfactory pain relief. One patient required an additional injection of 15 mg of pentazocine. Of the five patients in the control group, an average (+/- SD) dose of 90 +/- 23.7 mg of pentazocine was required to achieve adequate postoperative pain relief. Lysine acetylsalicylate decreased platelet aggregability but without resulting in hemorrhage. We concluded that this new salicylate administered intravenously to patients in the postoperative period provided adequate analgesia while allowing effective hemostasis despite its inhibitory effect on platelet aggregation.
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PMID:Postoperative intravenous administration of lysine acetylsalicylate: effect on pain relief and platelet function. 310 86

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

A series of analogues of the analgesic dipeptide derivative H-Lys-Trp(NPS)-OMe has been designed to determine the influence of the (2-nitrophenyl)sulfenyl (NPS) moiety on the activity. The syntheses and antinociceptive effects of these analogues of general formula H-Lys-Trp(R)-OMe [R = phenylsulfenyl (PS) (9); R = (2-carbomethyoxyphenyl)sulfenyl (CmPS) (10); R = (4-nitrophenyl)sulfenyl (pNPS) (11); R = (2,4-dinitrophenyl)sulfenyl (DNPS) (12); R = [2-(acetylamino)-2-carbomethoxyethyl]sulfenyl (AacCmES) (13); R = [2-(acetylamino)phenyl]sulfenyl (AacPS) (17); R = tert-butylsulfenyl (t-BuS) (23); R = (2-carbomethoxyethyl)sulfenyl (CmES) (24)] are described. Reaction of Z-Lys(Z)-Trp-OMe (3) with PS-, CmPS-, pNPS-, DNPS-, and AacCmES-Cl afforded the corresponding 2-(sulfenyl)tryptophan derivatives, which on treatment with boron-tris(trifluoroacetate)/trifluoroacetic acid or trimethylsilyl iodide in acetonitrile (Me3SiI/CH3CN) provided 9-13, respectively. Sulfenylation of 3 with NPS-Cl gave Z-Lys(Z)-Trp(NPS)-OMe, which, on catalytic hydrogenation of the nitro group using 10% Pd/C followed by acetylation of the resulting amino function and removal of the protecting Z groups, gave 17. Condensation of 2-(tert-butylsulfenyl)- and 2-[(2-carbomethoxyethyl)sulfenyl]tryptophan methyl ester, obtained by reaction of methyl 3a-hydroxy-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indole-2-carboxyla te with the corresponding thiol, with Z-Lys(Z)-OSu afforded Z-Lys(Z)-Trp(t-BuS)-OMe and Z-Lys(Z)-Trp(CmES)-OMe, which on treatment with Me3SiI/CH3CN provided 23 and 24, respectively. Intracerebroventricular administration of 10 elicited a naloxone-reversible antinociceptive effect in mice similar to that of H-Lys-Trp(NPS)-OMe. No analgesia was however found with the phenylsulfenyl or acyclic sulfenyl substituted dipeptides 9, 11, and 17 or 13, 23, and 24. The Trp(DNPS)-containing analogue was neurotoxic. Structure-activity studies indicate that the role of the NPS and CmPS moieties could be related to the adoption of a preferential active conformation.
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PMID:Analgesic dipeptide derivatives. 3. Synthesis and structure-activity relationships of o-nitrophenyl-modified analogues of the analgesic compound H-Lys-Trp(NPS)-OMe. 362 10

The effect of a constant i.v. infusion of lysine acetyl salicylate (LAS) on pain after operation was compared with that of a constant infusion of morphine in 30 patients undergoing unilateral inguinal herniorrhaphy. LAS provided analgesia equivalent to that provided by morphine and was associated with significantly less drowsiness, nausea and vomiting. No patient in either group was noted to suffer from respiratory depression. No untoward side effects were noted during or following the administration of LAS.
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PMID:Comparison of infusions of morphine and lysine acetyl salicylate for the relief of pain after surgery. 391 45

Desglycinamide(9)-lysine vasopressin facilitates development of resistance to the analgesic action of morphine in mice if morphine is administered before the peptide. Desglycinamide(9)-lysine vasopressin is not a morphine antagonist, and does not appear to cause either hyperalgesia or alteration of the response to the technique used for evaluating analgesia.
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PMID:Facilitation of development of resistance to morphine analgesia by desglycinamide9-lysine vasopressin. 452 67

The effects of the ACTH 4-9 analog (Org 2766) and the COOH-terminal tripeptide of Org 2766 (Phe-D-Lys-Phe; PDLP) on retrieval of one-trial learning passive avoidance behavior were compared with those of beta-endorphin, [Met5]-enkephalin, [D-Ala2,Met5]-enkephalin, des-Tyr1-[Met5]-enkephalin and des-enkephalin-gamma-endorphin (DE gamma E). Amounts of intracerebroventricularly administered Org 2766, PDLP, [Met5]-enkephalin, [D-Ala2,Met5]-enkephalin and DE gamma E, which induced a comparable attenuation of passive avoidance behavior were determined. Pretreatment with the opiate antagonist naltrexone prevented the attenuating effect of these peptides on passive avoidance behavior except that of DE gamma E. The attenuating effect of Org 2766 and of [Met5]-enkephalin was reversed to facilitation of passive avoidance behavior in the presence of naltrexone. Subcutaneous treatment with Org 2766 and [D-Phe7]-ACTH 4-10 decreased electrical self-stimulation behavior elicited from the medial septal area. Naltrexone prevented the inhibitory effect of Org 2766 on this behavior, but not that of [D-Phe7]-ACTH 4-10. Although the attenuating effect of PDLP on passive avoidance behavior was not reduced by pretreatment with [Met5]-enkephalin- or beta-endorphin-antiserum, and PDLP induced neither analgesia nor excessive grooming, the data suggest that the inhibitory effect of Org 2766 and PDLP on passive avoidance behavior and electrical self-stimulation are mediated by endorphin systems in the brain.
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PMID:Naltrexone-sensitive behavioral actions of the ACTH 4-9 analog (Org 2766). 630 25

beta-(Tyr9)melanotropin-(9-18), which itself has no analgesic action, as measured by the tail-flick and hot-plate methods, decreased morphine-induced analgesia following intracerebroventricular injection. H-Phe-Ile-Tyr-His-Ser-Tyr-Lys-OH heptapeptide, which has weak CRF-like activity, had no action on analgesia and was not able to modify morphine-induced analgesia. Compared with ACTH1-24, which in a subcutaneous dose of 100 micrograms/rat decreased morphine-induced analgesia, the same dose of H-Phe-Ile-Tyr-His-Ser-Tyr-Lys-OH was ineffective.
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PMID:The effects of beta-(Tyr9)melanotropin-(9-18) and H-Phe-Ile-Tyr-His-Ser-Tyr-Lys-OH on the analgesic action of morphine. 630 43

Intravenous lysine acetylsalicylate (LAS) and oxycodone were compared under double-blind conditions for analgesia after upper abdominal surgery in sixty patients anaesthetized by N2O--O2--halothane--relaxant technique. Either 125 mg/10 kg or 250 mg/10 kg LAS or 0.4 mg/10 kg or 0.8 mg/10 kg oxycodone was randomly administered when the patients complained of moderate or severe postoperative pain. When 30 min had elapsed following the injection of the test drug, oxycodone was given in 4 mg increments on demand until adequate pain relief was achieved. At 15 min postdrug, the lower dose of LAS offered significantly less pain relief than all other test drugs. At 30 min, the effect of the higher dose of LAS reached almost the analgesic level of the higher dose of oxycodone but only the latter provided significantly (P less than 0.05) better analgesia than the low dose of LAS. About 50% less additional narcotic supplementation was demanded following higher doses of both drugs when compared to lower ones. LAS 250 mg/10 kg (c. 1.8 g/70 kg) was found approximately equipotent to oxycodone 0.8 mg/10 kg (c. 6 mg/70 kg). However, LAS had a slower onset of action. Sweating seemed to occur more frequently after LAS than oxycodone, but significant changes in respiratory rate or sedation following LAS-oxycodone combinations when compared to oxycodone alone were not noted. The results show that for analgesia after upper abdominal surgery, 1.8 g of LAS may be substituted for about 6 mg of oxycodone.
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PMID:Comparison of lysine acetylsalicylate and oxycodone in postoperative pain following upper abdominal surgery. 678 30


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