Local administration of mu or kappa opioid agonists attenuates capsaicin-induced thermal hyperalgesia via peripheral opioid receptors in rats

Ko, Mei‐Chuan; Tuchman, Jessica; Johnson, Mark D.; Wiesenauer, K.; Woods, James H.

doi:10.1007/s002130050040

Cited by 22 publications

(19 citation statements)

References 33 publications

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“…To ensure an active dose of opioid drug was being administered in the forced swim assay, some groups of rats were subjected to the rat warm water tail withdrawal assay (Ko et al 2000) to measure antinociception with SNC80, morphine and CI977. The warm water tail withdrawal assay was performed one week before the forced swim assay was commenced.…”

Section: Warm Water Tail Withdrawal Assaymentioning

confidence: 99%

Nonpeptidic δ-opioid Receptor Agonists Reduce Immobility in the Forced Swim Assay in Rats

Broom

Jutkiewicz

Folk³

et al. 2002

Neuropsychopharmacology

166

122

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The present study examined the effect of opioid receptor agonists in the rat forced swim assay. The ␦ -opioid receptor agonists SNC80 (( ϩ )-4-[( ␣ R)-␣ -((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]-N,Ndiethylbenzamide) and ( 7 ␣ ,5]classes of compounds have also been investigated and have potential antidepressant activity. One such class of agents is the opioids. Studies have been performed using a variety of different opioid system-enhancing agents that suggest an antidepressant role for opioid agonists. Such studies have demonstrated antidepressant activity with the opioid ligand cyclazocine (Fink et al. 1970; open, placebo-controlled study) and with the opioid peptide ␤ -endorphin (Kline et al. 1977; open study). Interestingly, the enkephalinase inhibitors RB101 and BL-2401 exert an antidepressant-like action in a learned helplessness assay in rats, presumably by inhibiting the degradation of endogenous opioids (Baamonde et al. 1992;Kita et al. 1997). The effect of RB101 was reversed by the ␦ -opioid receptor antagonist nal-

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Section: Warm Water Tail Withdrawal Assaymentioning

confidence: 99%

Nonpeptidic δ-opioid Receptor Agonists Reduce Immobility in the Forced Swim Assay in Rats

Broom

Jutkiewicz

Folk³

et al. 2002

Neuropsychopharmacology

166

122

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“…To this end, capsaicin was injected into the distal portion of the rat's tail, and hyperalgesia was quantified by measuring the tail-withdrawal latency from 45°C water (Ko et al, 2000). A second purpose was to compare the ability of the -opioids morphine, buprenorphine and dezocine to reverse this hyperalgesia in male and female rats.…”

mentioning

confidence: 99%

Capsaicin-Induced Hyperalgesia and μ-Opioid-Induced Antihyperalgesia in Male and Female Fischer 344 Rats

Barrett¹,

Smith²,

Picker³

2003

J Pharmacol Exp Ther

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The influence of sex in determining responses to opioid analgesics has been well established in rodents and monkeys in assays of short-lasting, phasic pain. The purpose of this investigation was to use a capsaicin model of tonic pain to evaluate sex differences in hyperalgesia and -opioid-induced antihyperalgesia in Fischer 344 (F344) rats. Capsaicin injected into the tail produced a dose-dependent thermal hyperalgesia in males and females, with the dose required to produce a comparable level of hyperalgesia being 3.0-fold higher in males than in females. These sex differences were modulated by gonadal hormones, inasmuch as gonadectomy increased the potency of capsaicin in males and decreased its potency in females. Morphine, buprenorphine, and dezocine administered by various routes [systemic (s.c.), local (in the tail), and central (i.c.v.)] generally produced marked antihyperalgesic effects in males and females. Although in most instances these opioids were equally potent and effective in males and females, selected doses of local and i.c.v. administered buprenorphine produced greater effects in females. When administered locally, the antihyperalgesic effects of morphine were mediated by peripheral opioid receptors in both males and females, since this effect was not reversed by i.c.v. naloxone methiodide. These data contrast with the finding that -opioids are more potent in male rodents in assays of phasic pain, thus suggesting that distinct mechanisms underlie male and female sensitivity to opioid antinociception in phasic and tonic pain models. These findings emphasize the need to test male and female rodents in tonic pain assays that may have greater relevance for human pain conditions.

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“…With the [ 35 S]GTPγS binding assay, a classical functional measurement for receptor activation that can be used to determine the potencies and efficacies of opioid ligands at opioid receptors [25] , we found that MB- It have been well demonstrated that κ-agonists produce potent antinociception in different animal pain models [9,[11][12][13] . Our findings were similar to these studies in that we found that MB-1C-OH produced a significant antinociceptive effect in the acetic acid-induced writhing test via κ-but not µ-or δ-opioid receptors.…”

Section: Discussionmentioning

confidence: 99%

“…The precise mechanisms of MB-1C-OH-induced antinociception are of great interest and need to be elucidated in future studies. Many recent studies have shown that κ-opioid agonists produced analgesic effect via peripheral κ-opioid receptor [9][10][11][12][13] without producing undesirable side effects.…”

Section: Discussionmentioning

confidence: 99%

“…Increasing evidence from a wide variety of visceral pain models, inflammatory pain models and thermal hyperalgesia induced by capsaicin show that κ-opioid agonists could produce their analgesic effects via peripheral targeting [9][10][11][12][13] . Thus, peripherally acting κ-opioid agonists may be more promising candidate pharmacotherapies for pain relief because they do not cause central nervous system side effects.…”

Section: Introductionmentioning

confidence: 99%

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Novel κ-opioid receptor agonist MB-1C-OH produces potent analgesia with less depression and sedation

et al. 2015

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Aim: To characterize the pharmacological profiles of a novel κ-opioid receptor agonist MB-1C-OH. Methods: [ 3 H]diprenorphine binding and [ 35 S]GTPγS binding assays were performed to determine the agonistic properties of MB-1C-OH. Hot plate, tail flick, acetic acid-induced writhing, and formalin tests were conducted in mice to evaluate the antinociceptive actions. Forced swimming and rotarod tests of mice were used to assess the sedation and depression actions. Results: In [ 3 H]diprenorphine binding assay, MB-1C-OH did not bind to μ-and δ-opioid receptors at the concentration of 100 μmol/L, but showed a high affinity for κ-opioid receptor (K i =35 nmol/L). In [ 35 S]GTPγS binding assay, the compound had an E max of 98% and an EC 50 of 16.7 nmol/L for κ-opioid receptor. Subcutaneous injection of MB-1C-OH had no effects in both hot plate and tail flick tests, but produced potent antinociception in the acetic acid-induced writhing test (ED 50 =0.39 mg/kg), which was antagonized by pretreatment with a selective κ-opioid receptor antagonist Nor-BNI. In the formalin test, subcutaneous injection of MB-1C-OH did not affect the flinching behavior in the first phase, but significantly inhibited that in the second phase (ED 50 =0.87 mg/kg). In addition, the sedation or depression actions of MB-1C-OH were about 3-fold weaker than those of the classical κ agonist (-)U50,488H. Conclusion: MB-1C-OH is a novel κ-opioid receptor agonist that produces potent antinociception causing less sedation and depression.

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Local administration of mu or kappa opioid agonists attenuates capsaicin-induced thermal hyperalgesia via peripheral opioid receptors in rats

Cited by 22 publications

References 33 publications

Nonpeptidic δ-opioid Receptor Agonists Reduce Immobility in the Forced Swim Assay in Rats

Nonpeptidic δ-opioid Receptor Agonists Reduce Immobility in the Forced Swim Assay in Rats

Capsaicin-Induced Hyperalgesia and μ-Opioid-Induced Antihyperalgesia in Male and Female Fischer 344 Rats

Novel κ-opioid receptor agonist MB-1C-OH produces potent analgesia with less depression and sedation

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