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)

Lappaconitine (LA), isolated from Aconitum sinomontanum Nakai, was characterized as analgesic principle by our laboratory. The analgesic effect of ip LA 6 mg/kg as measured in the rat tail-flick test was reduced by icv CaCl2 or MgCl2 0.1 or 1 mumol/rat. BaCl2 was inactive. The analgesic action induced by LA was potentiated by ethylene glycol tetraacetic acid (EGTA, 0.2 mumol/rat icv) but not by ethylenediamine tetraacetic acid (EDTA, 0.2 or 0.4 mumol/rat icv). The calcium antagonists nifedipine (5 mg/kg ip) and verapamil (1 mumol/rat icv) partially reversed the Ca2+ antagonistic effect on LA analgesia, although nifedipine did not enhance LA analgesic action and only at 15 min after medication did verapamil exhibit enhancement of LA analgesia. The analgesic activity of LA was reduced and augmented by microinjection of CaCl2 0.5 mumol and EGTA 50 nmol to periaqueductal gray (PAG) area, respectively. These results suggest that LA can produce analgesia, possibly through a decrease in cellular calcium availability and PAG may be involved in the Ca2+ antagonistic effect on LA analgesia.
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PMID:[Effects of central Ca2+ on analgesic action of lappaconitine]. 251 40

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

We tested the influence of magnesium, zinc and copper upon the montelukast (MK, antagonist of cysteinyl leukotriene receptor type 1) effect in experimentally-induced thermoalgesia. We worked on 5 groups of 10 adults, each Wistar rats, that received: group I-control; group II: MK (10 mg/kg) unique administration; group III: MgCl2 (1 mM/kg/day) i.p., 3 days and MK (10 mg/kg) unique administration on the 3rd day; group IV: ZnCl2, (0.1 mM/kg/day), i.p., 3 days and MK (10 mg/kg) unique administration on the 3rd day; group V: copper acetate (0.05 mM/kg/day), i.p., 3 days and MK (10 mg/kg) unique administration on the 3rd day. We determined the thermoalgesic sensitivity (TS) using a tail flick analgesia meter, initially, 3 days after daily cation administration and 3 hours after MK administration. Our data show that MK has a statistically significant reduction of TS vs control group (3.76 +/- 1.04 s vs 1.81 +/- 0.98 s, p < 0.05). Copper and magnesium administration do not significantly change the MK effect to decrease TS. The co-administration of zinc and MK statistically significantly increased the TS of the group that received only MK (2.51 +/- 0.21 s vs 3.76 +/- 1.04 s, p < 0.05). Animals that received only cations (in the above mentioned doses) did not significantly change TS.
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PMID:Magnesium and other bivalent cations influence upon sodium montelukast effect in experimental-induced thermoalgesia. 1855 32