Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0030193 (pain)
 261,466 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The opioid nature of kentsin (Thr-Pro-Arg-Lys) and its ability to alter pain perception and intestinal transit were examined. Kentsin (30,000 nM) did not inhibit electrically stimulated contractions of the guinea pig ileum (GPI) or mouse vas deferens (MVD), nor did it cause a rightward displacement of the inhibitory concentration-response curves of the mu-selective opioid agonist PL017 in the GPI or the delta-selective agonist DPDPE in the MVD. Kentsin (10,000 nM) did not displace [3H] naloxone from rat brain homogenates. These results indicate that kentsin lacks opioid agonist and mu and delta opioid antagonist properties and does not bind to opioid receptors. In vivo, kentsin produced dose-dependent analgesia in both the hotplate and abdominal stretch tests when administered intracerebroventricularly (ICV) and intrathecally but not intravenously. The central analgesic effect of kentsin was partially antagonized by the opioid antagonist naloxone. Kentsin inhibited intestinal transit in a dose-dependent manner after ICV administration only. The intestinal antitransit effect of kentsin was not blocked by pretreatment with naloxone. These results suggest that kentsin acts centrally to produce both opioid and non-opioid effects. Further, the opioid-mediated analgesic effects of kentsin involve mechanisms other than direct interaction with opioid receptors.
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PMID:Kentsin: tetrapeptide from hamster embryos produces naloxone-sensitive effects without binding to opioid receptors. 281 32

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 antinociceptive effects obtained in arthritic rats with morphine, the opioid mu-agonist DAGO [D-Ala2,MePhe4,Gly-ol5]enkephalin, the delta-selective agonist DTLET [D-Thr2, Leu5]enkephalyl-Thr, and the kappa-agonist U-50,488H were compared to their corresponding effects in normal animals and morphine-pretreated arthritic rats, respectively, using a paw pressure test. The effects of the mu- and kappa-agonists were increased in arthritic rats. While morphine-treated rats were cross-tolerant to the mu- and kappa-agonists, no tolerance to the delta-selective agonist was found. The possibility that the potent action of morphine in this model for chronic inflammatory pain is mediated partly through kappa-mechanisms is discussed.
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PMID:Opioid receptor types and antinociceptive activity in chronic inflammation: both kappa- and mu-opiate agonistic effects are enhanced in arthritic rats. 302 2

Local endometrial blood flow was measured by a thermistor technique and myometrial activity by intrauterine pressure recording in 10 women before and during menstruation. The effect of lysine vasopressin infusion (1 pmol/kg body-weight per min) and of bolus injection of a synthetic oxytocin analogue, 1-deamino-2-D-Tyr(OEt)-4-Thr-8-Orn-oxytocin (10 nmol/kg body-weight), were studied. Spontaneous variations in blood flow were seen synchronous with clearly demarcated uterine contractions, the myometrial activity being significantly increased in early (day -1 to day +2) compared with late (day +3 to day +5) menstrual phase. The vasopressin infusion decreased blood flow, stimulated uterine activity and caused slight to moderate dysmenorrhoea-like pain. These effects were completely inhibited by the injection of the oxytocin analogue. In-vitro studies on uterine arteries confirmed that the analogue also inhibited the vasopressin-induced constriction of the uterine arteries. This antagonist was more effective than two other analogues, 1-deamino-2-D-Tyr(OEt)-4-Val-8-Orn-oxytocin and 1-deamino-2-Tyr(OEt)-oxytocin. The counteracting effect of 1-deamino-2-D-Tyr(OEt)-4-Thr-8-Orn-oxytocin on the vasopressin-induced decrease of blood flow and increase of contractions supports the therapeutic value of the drug in primary dysmenorrhoea and preterm labour.
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PMID:Uterine blood flow and myometrial activity at menstruation, and the action of vasopressin and a synthetic antagonist. 319 Oct 63

In order to study the etiological role of vasopressin in primary dysmenorrhea the therapeutic effect of an antagonist of vasopressin action on the uterus (1-deamino-2-D-Tyr(OEt)-4-Thr-8-Orn-oxytocin) was investigated in 14 patients with moderate to severe symptoms. The women participated in the study at two menstruations and each time one intravenous bolus injection of the analogue (10 micrograms/kg body weight) and one of the placebo (saline) were given, randomized and double-blind with at least a 2 hour interval. The effect was monitored by overall ratings and by pain diagrams described by the patients. In the former parameter the vasopressin antagonist was significantly more effective (p less than 0.01). In the pain diagrams, however, a significant reduction of symptoms occurred both after the analogue administrations and after placebo given as second injection. The results support a causative role of vasopressin in primary dysmenorrhea, but further studies with higher doses and/or other routes of administration or delivery systems are required in order to delineate the therapeutic value of vasopressin antagonists in the condition.
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PMID:Can primary dysmenorrhea be alleviated by a vasopressin antagonist? Results of a pilot study. 332 65

Acrylic-fixed total hip and surface replacement arthroplasty have been very effective in affording immediate relief of pain and providing improved function. Complications have been reduced by improvements in design, materials, and especially technique. They are now very low in the elderly, and the stem type acrylic-fixed design remains the procedure of choice. The failure rates in youthful patients and those with bone-stock deficiencies have been high in both THR and surface types, although the latter had the advantage of preserving femoral stock. On the femoral side, the new "macro" femoral designs from Europe and "micro" femoral porous designs have shown promise, but thigh pain, incomplete and difficult to predict bone ingrowth patterns, coupled with removal problems have influenced design and technique changes. Both press-fit stem types and porous surface replacements have produced promising initial results with less potential downside risks. On the acetabular side, both the cementless hemispherical with screw-type adjuvant fixation, or the chamfered cylinder designs, used primarily with the UCLA porous surface replacements, but also with stem-type devices, appear to achieve best short-term results, while the entire variety of screw rings are disappointing. The future will bring further refinements in technique and specific indications for certain types of replacement stem in specific types of bone stock deficiencies. The all ceramic-ceramic and ceramic-polyethylene bearings show promise of reducing wear and, hence, should improve longevity of implant fixation.
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PMID:Hip arthroplasty today and tomorrow. 332 84

A study of 141 total hip replacements with the Lubinus prosthesis is presented. The complications in the total patient group and the results in 129 hips with follow-up times from 5 to 7 years are described. Three prostheses (2.1%) have been reoperated because of loosening. There were radiographic signs of definitive loosening in 2.3%. Varus positioning was associated with an increased loosening rate. No infections have been encountered, and none of the hips have undergone excision arthroplasty. Ninety-two percent of the hips were free from significant pain and 78% had a total range of motion exceeding 160 degrees. THR was performed, without subsequent infections, in a conventional operating room using prophylactic penicillin and gentamicin cement. We propose that the surgical technique of exposure and the cement injection technique with a partial vacuum in the medullary canal may be responsible for the low incidence of femoral prosthesis loosening (0.7%).
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PMID:Total hip replacement ad modum Lubinus: five- to seven-year follow-up. 356 3

Hundreds of total hip replacements in dogs have been performed at the Ohio State University of Veterinary Medicine since August 1976. Dogs with disabling diseases or conditions of the hip are candidates for the THR. The technique provides the dog with a pain free, mechanically sound ball and socket joint. The most commonly encountered complication is dislocation, while the most disastrous complication is infection. Complications can be minimized through adherence to detail during the procedure. By following strict aseptic principles, surgical technique and postoperative care, successful hip function has been achieved in 94.7% of the cases.
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PMID:[Replacement of the hip joint in the dog]. 376 84

A randomized, double-blind, placebo-controlled trial was carried out in 22 patients with hypostatic leg ulceration. Patients were treated topically with either a cream containing the amino acids l-cysteine, glycine and dl-threonine or the cream base alone (placebo). Most patients had their leg ulcers treated and dressed 3-times per week for 12 weeks. Clinical assessments were conducted at weekly intervals and data from 21 of the 22 patients were available for statistical analysis. The results revealed that the degree of healing and decrease of pain were significantly better in the group of patients receiving the amino acid combination. It would appear from this study that l-cysteine, glycine and dl-threonine in combination are of value in promoting would healing in hypostatic leg ulceration.
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PMID:L-cysteine, glycine and dl-threonine in the treatment of hypostatic leg ulceration: a placebo-controlled study. 393 19

Bone marrow cells of various animal species and men produce a group of bioregulatory peptides called myelopeptides (MPs). A highly purified MP fraction and some individual molecules have been isolated from the supernatant of porcine bone marrow cell cultures by reverse phase chromatography. MPs have a wide spectrum of functional activities: immunoregulatory, differentiating and opiate-like. They evoke 2.5-fold stimulation of antibody production to various antigens. They correct some immune defects in MRL/lpr mice with spontaneous autoimmune disorders that results in 2-fold prolongation of the life span of these mice. MPs influence the differentiation of bone marrow and peripheral blood cells derived from healthy and leukemic donors. They induce terminal differentiation in the leukemic human HL-60 cell line. MPs also show an effect on pain sensitivity. A new immunocorrective drug Myelopid has been developed on the basis of MP mixtures. This drug is effectively used in Russia both in medicine and veterinary practice for prophylaxis and treatment of diseases accompanied by immunodeficiency. Two individual MPs were isolated and identified: Phe-Leu-Gly-Phe-Pro-Thr (MP-1) and Leu-Val-Val-Tyr-Pro-Trp (MP-2). MP-1 displays immunoregulatory activity; MP-2 abolishes the inhibitory effect of leukemic cells on T-lymphocyte functional activity. MPs seem to provide not only immunoregulation but also to participate in complex interactions between different systems in the organism.
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PMID:Myelopeptides: bone marrow regulatory mediators. 764 88


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