The influence of divalent cations on the analgesic effect of opioid and non-opioid drugs

Assi, Abdel-Azim

doi:10.1006/phrs.2001.0811

Cited by 14 publications

(8 citation statements)

References 37 publications

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“…Aspirin and levetiracetam-aspirin combination produced high antinociceptive efficacy in diabetic mice in both tests compared to weak efficacy (tail-flick test), and no effect (von Frey test) in nondiabetic mice. The general lack of antinociception of individually applied drugs in non-diabetic mice is in line with previous studies which showed no effect of levetiracetam [6,7], ibuprofen [36], aspirin [37,38] and paracetamol [39] in healthy mice/rats in thermal/mechanical pain tests. Therefore, we could hypothesize that the determined antinociceptive effects of levetiracetam, analgesics and levetiracetam-analgesic combinations in diabetic mice are dependent on neuropathic changes caused by diabetes.…”

Section: Discussionsupporting

confidence: 88%

Levetiracetam synergises with common analgesics in producing antinociception in a mouse model of painful diabetic neuropathy

Micov

Tomić

Pecikoza

et al. 2015

Pharmacological Research

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Section: Discussionsupporting

confidence: 88%

Levetiracetam synergises with common analgesics in producing antinociception in a mouse model of painful diabetic neuropathy

Micov

Tomić

Pecikoza

et al. 2015

Pharmacological Research

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“…Literature data show that MS at a dose of 2.5 mg/kg (0.5 mg of elementary magnesium, i.p.) had no analgesic effect (Assi et al, 2001) and magnesium oxide at doses of 5 and 10 mg/kg (3.02 and 6.03 mg of elementary magnesium, i.p.) had analgesic effect (Jahangiri et al, 2013) in acetic acid-induced writhing test in mice.…”

Section: Discussionmentioning

confidence: 95%

“…Additionally, magnesium acts as an antagonist at the glutamate subtype of NMDA receptors and blocks NMDA-induced currents in a voltage-dependent manner by blocking the receptor channel effects (Fawcett et al, 1999). Several lines of evidence indicate that magnesium enhances the analgesic effects of opioids, general, and local anesthetics in different animal models of pain (Assi, 2001;Liu et al, 2001;Nechifor, 2011). As a sole drug, magnesium demonstrated analgesic efficacy against neuropathic pain (Begon et al, 2000;Rondón et al, 2010).…”

Section: Introductionmentioning

confidence: 99%

The antinociceptive effects of magnesium sulfate and MK-801 in visceral inflammatory pain model: The role of NO/cGMP/K⁺ATP pathway

Vučković

Srebro

Vujović

et al. 2015

Pharmaceutical Biology

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Context: Magnesium and MK-801 (dizocilpine), antagonists of N-methyl-D-aspartate receptors, are involved in the processing of pain. Objective: This study determines whether magnesium sulfate (MS) and MK-801 affects visceral inflammatory pain and determines a possible mechanism of action. Materials and methods: Analgesic activity was assessed using the acetic acid-induced writhing test in rats. MS (1-45 mg/kg) or MK-801 (0.005-0.03 mg/kg) was administrated subcutaneously (s.c.). To assess possible mechanisms of action, we examined the effects of L-NAME (10 mg/kg, intraperitoneal), methylene blue (0.5 mg/kg, s.c.), and glibenclamide (3 mg/kg, s.c.) on the effect of MS or MK-801. Results: MS and MK-801 showed biphasic and linear dose-response pattern, respectively. MS reduces the number of writhing on the dose of 1, 5, and 15 mg/kg by 60, 50, and 78%, respectively, while it has no effects on the doses of 30 and 45 mg/kg. MK-801 (0.005-0.03 mg/kg) showed decrease in the number of writhing by 33-79%. The mean effective doses of MS and MK-801 were 6.6 (first phase) and 0.009 mg/kg, respectively. Both drugs did not impair the rotarod performance. L-NAME, methylene blue, and glybenclamide reduced the effect of MK-801 by 100, 43, and 64%, respectively, but not the effect of MS. Conclusions:The results suggest that MS and MK-801 may be useful analgesics in the management of visceral inflammatory pain, at doses that do not induce motor impairment. The modulation of NO/cGMP/K+ATP pathway plays an important role in the antinociceptive mechanism of MK-801, but does not contribute to the antinociceptive effect of MS.

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“…In the tail-flick 21 or hot plate 22 assays in mice, neither 5a (doses up to 3010 lmol/kg) nor APAP (doses up to 6620 lmol/kg) was effective (data not shown), a finding that is consistent with previous studies that have demonstrated no or weak analgesic activity of APAP in these assay. 23 Moreover, neither 5a nor APAP was found to possess anti-inflammatory properties in a model of carrageenan-induced paw edema 24 (Fig. 4).…”

Section: Resultsmentioning

confidence: 98%

“…Carrageenan-induced paw edema. 24 Under halothane anesthesia male CD-1 mice were injected with lambda-carrageenan (50 lL, 1% in saline; Sigma) via the plantar surface of one hind paw 30 min after drug administration. Inflammation (paw volume: model 520 paw volume meter; IITC Life Sciences, Inc., Woodland Hills, CA.)…”

Section: 34mentioning

confidence: 99%

Synthesis and in vivo evaluation of non-hepatotoxic acetaminophen analogs

Vaccarino

Paúl

Mukherjee

et al. 2007

Bioorganic & Medicinal Chemistry

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Abstract-A series of acetaminophen (APAP) analogs, 2-(1,1-dioxido-3-oxo-1,2-benzisothiazol-2(3H)-yl)-N-(4-hydroxyphenyl)alkanecarboxamides, bearing a heterocyclic moiety linked to the p-acylaminophenol fragment, were prepared in a general project to develop APAP analogs with modulated pharmacokinetic profiles. Unexpectedly, the products described maintained the in vivo analgesic profile, while the characteristic hepatotoxicity of APAP was consistently reduced. One of the products, 5a, was studied in vivo in comparison with APAP. Compound 5a displayed an analgesic efficacy comparable to that of APAP. A relatively high acute oral dose of 5a (6 mmol/kg) produced no measurable toxicity, whereas the equimolar dose of APAP increased transaminase activity, depleted hepatic and renal glutathione, and resulted in mortality. In human hepatocytes (HEPG-2) and in human primary cultures of normal liver cells, APAP, but not 5a, was associated with apoptotic cell death, Fas-ligand up-regulation, and CAR (constitutive androstane receptor) activation, contributing to a favorable safety profile of 5a as an orally delivered analgesic.

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The influence of divalent cations on the analgesic effect of opioid and non-opioid drugs

Cited by 14 publications

References 37 publications

Levetiracetam synergises with common analgesics in producing antinociception in a mouse model of painful diabetic neuropathy

Levetiracetam synergises with common analgesics in producing antinociception in a mouse model of painful diabetic neuropathy

The antinociceptive effects of magnesium sulfate and MK-801 in visceral inflammatory pain model: The role of NO/cGMP/K⁺ATP pathway

Synthesis and in vivo evaluation of non-hepatotoxic acetaminophen analogs

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The influence of divalent cations on the analgesic effect of opioid and non-opioid drugs

Cited by 14 publications

References 37 publications

Levetiracetam synergises with common analgesics in producing antinociception in a mouse model of painful diabetic neuropathy

Levetiracetam synergises with common analgesics in producing antinociception in a mouse model of painful diabetic neuropathy

The antinociceptive effects of magnesium sulfate and MK-801 in visceral inflammatory pain model: The role of NO/cGMP/K+ATP pathway

Synthesis and in vivo evaluation of non-hepatotoxic acetaminophen analogs

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Product

Resources

About

The antinociceptive effects of magnesium sulfate and MK-801 in visceral inflammatory pain model: The role of NO/cGMP/K⁺ATP pathway