Common animal models for spasticity and pain

Eaton, Mary J.

doi:10.1682/jrrd.2003.08.0041

Cited by 36 publications

(28 citation statements)

References 150 publications

(165 reference statements)

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“…Therefore, antinociceptive activity of Bupredermi was evaluated using chemical and thermal models of acute pain, acetic acid-induced writhing test and the tail flick test. Such thermal tail-flick tests are most widely and reliably used for revealing the potency of opioid analgesics, useful for predicting analgesic effects in humans (69)(70).…”

Section: Discussionmentioning

confidence: 99%

Buprederm™, a New Transdermal Delivery System of Buprenorphine: Pharmacokinetic, Efficacy and Skin Irritancy Studies

Park¹,

Kim²,

Song³

et al. 2008

Pharm Res

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Section: Discussionmentioning

confidence: 99%

Buprederm™, a New Transdermal Delivery System of Buprenorphine: Pharmacokinetic, Efficacy and Skin Irritancy Studies

Park¹,

Kim²,

Song³

et al. 2008

Pharm Res

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“…The writhing test can predict effective analgesic doses for agents that can be used in humans (Dubinsky et al, 1987;Eaton, 2003). The mediators involved in the genesis of the nociception observed in the writhing test are the eicosanoids and sympathomimetic amines, the release of which is preceded by the release of the nociceptive cytokines TNF-a, IL-1b, and IL-8 (Duarte et al, 1988;Ribeiro et al, 2000a;Thomazzi et al, 1997).…”

Section: Discussionmentioning

confidence: 99%

Analgesic activity ofEugenia jambolanaleave constituent: A dikaempferol rhamnopyranoside from ethyl acetate soluble fraction

Lingaraju

Anand

Balaganur

et al. 2014

Pharmaceutical Biology

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Context: Eugenia jambolana Lam. (Myrtaceae) is a medicinal plant used in folk medicine for the treatment of diabetes, inflammation, and pain. Objective: We investigated the antinociceptive effect of kaempferol-, isolated from the E. jambolana leaves. Materials and methods: EJ-01 (3, 10, and 30 mg kg À1 , orally) was assessed for peripheral (formalin-nociception and acetic acid-writhing) and central (hot plate and tail flick test) analgesic activity in mice and the in vitro anti-inflammatory activity (25, 50, and 100 mg mL ) levels were observed in EJ-01-treated medium (25, 50, and 100 mg mL À1 ) as compared with vehicle-treated control values (788.67 and 161.77 pg mL À1 ), respectively. Significant reduction in total nitrite plus nitrate (NO x ) levels (70.80 nmol) was observed in the EJ-01-treated medium (100 mg mL À1

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“…Because DiPOA has a higher selectivity for mu over kappa, as compared with morphine, this may contribute to the lack of efficacy in the PSN model. Secondly, both the CCI and SNL models involve a more substantial inflammatory component as compared with the PSN model (Lindenlaub and Sommer, 2000;Eaton, 2003), which may account for the efficacy of peripherally applied opioid agonists observed using these models. Finally, the time point in these studies was 14 days postsurgery or less; at this time, there may be a significant inflammatory component due to the surgery.…”

Section: Discussionmentioning

confidence: 99%

DiPOA ([8-(3,3-Diphenyl-propyl)-4-oxo-1-phenyl-1,3,8-triazaspiro[4.5]dec-3-yl]-acetic Acid), a Novel, Systemically Available, and Peripherally Restricted Mu Opioid Agonist with Antihyperalgesic Activity: II. In Vivo Pharmacological Characterization in the Rat

Whiteside¹,

Harrison²,

Pearson³

et al. 2004

J Pharmacol Exp Ther

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Mu opioid receptors are expressed throughout the central and peripheral nervous systems. Peripheral inflammation leads to an increase in mu receptor present on the peripheral terminals of primary sensory neurons. Activation of peripheral mu receptors produces potent antihyperalgesic effects in both humans and animals. Here, we describe the in vivo pharmacological properties of the structurally novel, highly potent, systemically available yet peripherally restricted mu opioid agonist, [8-(3,3-diphenyl-propyl)-4-oxo-1-phenyl-1,3,8-triaza-spiro[4.5]dec-3-yl]-acetic acid (DiPOA). DiPOA administered i.p. produced naltrexone-sensitive, dose-dependent reversal of Freund's complete adjuvant-induced inflammatory mechanical hyperalgesia (1-10 mg/kg). Maximum percent reversal (67%) was seen 1 h postadministration at 10 mg/kg (the highest dose studied). DiPOA also proved antihyperalgesic in a model of postsurgical pain with a maximum percent reversal of 85% 1 h postadministration at 30 mg/kg i.p. (the highest dose studied). DiPOA administered i.p. had no effect in the tail flick assay of acute pain (0.1-10 mg/kg), produced no ataxia as measured by latency to fall from an accelerating rotarod (3-30 mg/kg), and was not antihyperalgesic in the Seltzer model of neuropathic pain (1-10 mg/kg). This is the first report of a peripherally restricted, small-molecule mu opioid agonist that is nonsedating, antihyperalgesic, and effective against inflammatory and postsurgical pain when administered systemically.To date, four members of the opioid receptor family have been cloned and characterized, and include the mu, kappa, delta, and opioid receptor-like 1 (ORL-1) receptors (Pleuvry, 2003). All are G-protein-coupled receptors and mediate inhibition of adenylate cyclase through activation of GTP-binding proteins. In addition, opioid receptor agonism results in the opening of receptor-operated potassium channels and suppression of voltage-gated calcium currents (Duggan and North, 1983). Several classes of endogenous peptidic ligands have been identified for the opioid receptors, including the enkephalins, dynorphins, endorphins, and nociceptin (Terenius, 2000). These ligands are distributed throughout the central and peripheral nervous system (CNS and PNS) as well as in peripheral tissues.Opioid receptors are also expressed throughout the CNS, and their activation results in potent analgesia via inhibition of ascending excitatory nociceptive transmissions and activation of descending inhibitory systems (Fields and Basbaum, 1999;Yaksh, 1999). Activation of CNS opioid receptors also results in diminished responsiveness of the brainstem respiratory centers to carbon dioxide (Gutstein and Akil, 2001) and stimulation of dopaminergic pathways, particularly the Article, publication date, and citation information can be found at

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Common animal models for spasticity and pain

Cited by 36 publications

References 150 publications

Buprederm™, a New Transdermal Delivery System of Buprenorphine: Pharmacokinetic, Efficacy and Skin Irritancy Studies

Buprederm™, a New Transdermal Delivery System of Buprenorphine: Pharmacokinetic, Efficacy and Skin Irritancy Studies

Analgesic activity ofEugenia jambolanaleave constituent: A dikaempferol rhamnopyranoside from ethyl acetate soluble fraction

DiPOA ([8-(3,3-Diphenyl-propyl)-4-oxo-1-phenyl-1,3,8-triazaspiro[4.5]dec-3-yl]-acetic Acid), a Novel, Systemically Available, and Peripherally Restricted Mu Opioid Agonist with Antihyperalgesic Activity: II. In Vivo Pharmacological Characterization in the Rat

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