Study of the involvement of K+ channels in the peripheral antinociception of the κ-opioid receptor agonist bremazocine

Amarante, Luiz H; Alves, Daniela Pereira; Duarte, Igor Dimitri Gama

doi:10.1016/j.ejphar.2004.05.009

Cited by 15 publications

(13 citation statements)

References 27 publications

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“…Therefore, we further corroborate recent findings in various pain models that local activation or blockade of KATPs modulates the anti-hyperalgesic effects induced by peripheral opioid receptors (Amarante et al, 2004; Granados-Soto et al, 2002; Pacheco and Duarte 2005; Picolo et al, 2003; Rodrigues et al, 2000). …”

Section: Discussionsupporting

confidence: 90%

“…Activation or blockade of the KATP in sensory neurons modulates the anti-hyperalgesic responses induced by all three subtypes of ORs in the spinal system (Amarante et al, 2004; Pacheco and Duarte 2005). While both pore-forming and regulatory subunits of KATP are expressed in trigeminal sensory neurons (Niu et al, 2011) the functional interaction between KATP and ORs in the orofacial model has not been demonstrated.…”

Section: Introductionmentioning

confidence: 99%

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Activation of peripheral delta-opioid receptors leads to anti-hyperalgesic responses in the masseter muscle of male and female rats

Saloman

Niu

2011

Neuroscience

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In this project, we examined peripheral δ-opioid receptor (DOR)-mediated anti-hyperalgesic responses in the context of an acute orofacial muscle pain condition in both male and female rats. We also investigated whether the ATP-sensitive K+ channel (KATP), a downstream target of OR signaling, contributes to DOR-mediated anti-hyperalgesic responses. Local pretreatment of the masseter with a DOR agonist, DPDPE, dose-dependently attenuated capsaicin-induced mechanical hypersensitivity in both male and female rats. However, there were sex differences in the potency of local DPDPE in that a 10 fold higher dose of DPDPE was required in female rats to produce the level of anti-hyperalgesia achieved in male rats. The sex differences in the DPDPE effect may not be fully explained by DOR expression level since there was no significant sex difference in DOR mRNA levels in trigeminal ganglia (TG). Finally, pretreatment of the masseter with the KATP antagonist, glibenclamide significantly blocked the effects of DPDPE in male rats suggesting that the peripheral DOR effect is mediated by the KATP. These studies revealed novel information about sex differences with regards to peripherally localized DOR-mediated anti-hyperalgesia under an orofacial muscle pain condition.

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Section: Discussionsupporting

confidence: 90%

Section: Introductionmentioning

confidence: 99%

Activation of peripheral delta-opioid receptors leads to anti-hyperalgesic responses in the masseter muscle of male and female rats

Saloman

Niu

2011

Neuroscience

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“…Previous studies that utilized inflammatory agents such as carrageenan, capsaicin, or formalin examined the anti-hyperalgesic effects of KOR agonists under pain conditions that are resolved in a relatively shorter duration and during the development phase of inflammatory pain [1,8,20,21]. Our data is particularly interesting in that U50, 488 was anti-hyperalgesic 3 days after the induction of inflammation, a time point at which the hyperalgesia was fully developed.…”

mentioning

confidence: 81%

Effects of peripheral κ opioid receptor activation on inflammatory mechanical hyperalgesia in male and female rats

Auh

2012

Neuroscience Letters

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Activation of peripheral κ opioid receptors (KOR) effectively relieves pain and hyperalgesia in preclinical and clinical models of pain. Although centrally located KOR activation results in sexually dimorphic effects, it is unclear whether peripheral KOR also produces sex dependent effects in persistent inflammatory pain conditions. In this study, we investigated whether local administration of a specific KOR agonist, U50, 488 relieve mechanical hyperalgesia induced by the injection of complete Freund’s adjuvant (CFA) in the rat hindpaw, and whether there are sex differences. The effects of U50, 488 were assessed three days after the induction of CFA-induced inflammation, a time point at which mechanical hyperalgesia was most prominent. There were no sex differences in baseline and CFA-induced changes in mechanical thresholds between male and female rats. Local treatment of U50, 488 produced moderate, but significant, anti-hyperalgesia in both male and female rats. However, U50, 488 was significantly more effective in male rats at the highest dose of U50, 488. We confirmed that the highest dose of U50, 488 used in this study did not produce systemic effects, and that the drug effect is receptor specific. On the basis of these results, we suggest that local KOR agonists are effective in mitigating mechanical hyperalgesia under a persistent inflammatory pain condition and that sex differences in anti-hyperalgesic effects become more evident at high doses.

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“…Furthermore, all sulfonylureas tested to date, when administered by the intracerebroventricular or intrathecal route, dose dependently antagonized the antinociception induced by systemic administration of fentanyl (4,37), suggesting that opening of ATPsensitive K + channels in neurons of the central nervous system underlies the antinociceptive effect of fentanyl. Interestingly, peripheral antinociception of bremazocine, a κ-opioid, is not due to K + channel activation (38).…”

Section: Discussionmentioning

confidence: 99%

Participation of ATP-sensitive K+ channels in the peripheral antinociceptive effect of fentanyl in rats

Rodrigues

Castro

Francischi

et al. 2005

Braz J Med Biol Res

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We examined the effect of several K + channel blockers such as glibenclamide, tolbutamide, charybdotoxin (ChTX), apamin, tetraethylammonium chloride (TEA), 4-aminopyridine (4-AP), and cesium on the ability of fentanyl, a clinically used selective µ-opioid receptor agonist, to promote peripheral antinociception. Antinociception was measured by the paw pressure test in male Wistar rats weighing 180-250 g (N = 5 animals per group). Carrageenan (250 µg/ paw) decreased the threshold of responsiveness to noxious pressure (∆ = 188.1 ± 5.3 g). This mechanical hyperalgesia was reduced by fentanyl (0.5, 1.5 and 3 µg/paw) in a peripherally mediated and dosedependent fashion (17.3, 45.3 and 62.6%, respectively). The selective blockers of ATP-sensitive K + channels glibenclamide (40, 80 and 160 µg/paw) and tolbutamide (80, 160 and 240 µg/paw) dose dependently antagonized the antinociception induced by fentanyl (1.5 µg/paw). In contrast, the effect of fentanyl was unaffected by the large conductance Ca 2+ -activated K + channel blocker ChTX (2 µg/paw), the small conductance Ca 2+ -activated K + channel blocker apamin (10 µg/paw), or the non-specific K + channel blocker TEA (150 µg/paw), 4-AP (50 µg/paw), and cesium (250 µg/paw). These results extend previously reported data on the peripheral analgesic effect of morphine and fentanyl, suggesting for the first time that the peripheral µ-opioid receptor-mediated antinociceptive effect of fentanyl depends on activation of ATP-sensitive, but not other, K + channels.

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Study of the involvement of K+ channels in the peripheral antinociception of the κ-opioid receptor agonist bremazocine

Cited by 15 publications

References 27 publications

Activation of peripheral delta-opioid receptors leads to anti-hyperalgesic responses in the masseter muscle of male and female rats

Activation of peripheral delta-opioid receptors leads to anti-hyperalgesic responses in the masseter muscle of male and female rats

Effects of peripheral κ opioid receptor activation on inflammatory mechanical hyperalgesia in male and female rats

Participation of ATP-sensitive K+ channels in the peripheral antinociceptive effect of fentanyl in rats

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