Participation of K<sub>ATP</sub> Channels in the Antinociceptive Effect of Pregabalin in Rat Formalin Test

Kweon, Tae Dong; Kim, Ji Young; Kwon, Il; Choi, Jong Bum; Lee, Youn Woo

doi:10.3344/kjp.2011.24.3.131

Cited by 13 publications

(10 citation statements)

References 23 publications

(26 reference statements)

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“…Intrathecal administration of pregabalin, through catheterization of spinal subarachnoid space, was shown to decrease formalin-induced frequency of flinching in a dose dependent manner. However, administration of glibenclamide reversed the analgesic effect of pregabalin suggesting that the anti-nociceptive effect of pregabalin in the rat formalin test may be associated with activation of K ATP channels [ 114 ]. Earlier studies had shown that application of pregabalin to the intracellular surface of the excised patches activates K ATP channels in the differentiated hippocampal neuron-derived H19-7 cells, suggesting that its binding side could be primarily on the intracellular site [ 115 ].…”

Section: Mechanism Of Actionmentioning

confidence: 99%

Pregabalin in Neuropathic Pain: Evidences and Possible Mechanisms

Verma¹,

Singh²,

Jaggi

2014

157

119

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Pregabalin is an antagonist of voltage gated Ca2+ channels and specifically binds to alpha-2-delta subunit to produce antiepileptic and analgesic actions. It successfully alleviates the symptoms of various types of neuropathic pain and presents itself as a first line therapeutic agent with remarkable safety and efficacy. Preclinical studies in various animal models of neuropathic pain have shown its effectiveness in treating the symptoms like allodynia and hyperalgesia. Clinical studies in different age groups and in different types of neuropathic pain (peripheral diabetic neuropathy, fibromyalgia, post-herpetic neuralgia, cancer chemotherapy-induced neuropathic pain) have projected it as the most effective agent either as monotherapy or in combined regimens in terms of cost effectiveness, tolerability and overall improvement in neuropathic pain states. Preclinical studies employing pregabalin in different neuropathic pain models have explored various molecular targets and the signaling systems including Ca2+ channel-mediated neurotransmitter release, activation of excitatory amino acid transporters (EAATs), potassium channels and inhibition of pathways involving inflammatory mediators. The present review summarizes the important aspects of pregabalin as analgesic in preclinical and clinical studies as well as focuses on the possible mechanisms.

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Section: Mechanism Of Actionmentioning

confidence: 99%

Pregabalin in Neuropathic Pain: Evidences and Possible Mechanisms

Verma¹,

Singh²,

Jaggi

2014

157

119

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“…There is evidence that the opening of K ATP channels participates in the analgesic effect of the non-steroidal anti-inflammatory drugs ketorolac [ 16 ] and diclofenac [ 17 , 18 ], but not in that of indomethacin [ 17 ]. There is also evidence that K ATP channels play a role in the analgesic effect of a variety of agents such as morphine [ 19 ], clonidine [ 20 ] and 5-HT1 agonists [ 21 ], atrial natriuretic peptide (ANP) [ 17 ], and pregabalin [ 22 ]. Therefore, it appears that the opening of K ATP channels is a common mechanism of antinociception.…”

Section: Introductionmentioning

confidence: 99%

Evidence for the Participation of ATP-sensitive Potassium Channels in the Antinociceptive Effect of Curcumin

et al. 2012

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BackgroundIt has been reported that curcumin, the main active compound of Curcuma longa, also known as turmeric, exhibits antinociceptive properties. The aim of this study was to examine the participation of ATP-sensitive potassium channels (KATP channels) and, in particular, that of the L-arginine-nitric oxide-cyclic GMP-KATP channel pathway, in the antinociceptive effect of curcumin.MethodsPain was induced by the intraplantar injection of 1% formalin in the right hind paw of Wistar rats. Formalin-induced flinching behavior was interpreted as an expression of nociception. The antinociceptive effect of oral curcumin was explored in the presence and absence of local pretreatment with L-NAME, an inhibitor of nitric oxide synthase, ODQ, an inhibitor of soluble guanylyl cyclase, and glibenclamide, a blocker of KATP channels.ResultsOral curcumin produced a dose-dependent antinociceptive effect in the 1% formalin test. Curcumin-induced antinociception was not altered by local L-NAME or ODQ, but was significantly impaired by glibenclamide.ConclusionsOur results confirm that curcumin is an effective antinociceptive agent. Curcumin-induced antinociception appears to involve the participation of KATP channels at the peripheral level, as local injection of glibenclamide prevented its effect. Activation of KATP channels, however, does not occur by activation of the L-arginine-nitric oxide-cGMP-KATP channel pathway.

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“…This result is consistent with the results of our study in which we found that pregabalin 100 mg/kg decreased the number of writings in acetic acidinduced writhing test in mice. Furthermore, other investigators examined the antinociceptive effect of pregabalin in rat formalin pain model [25]. They found that intratechal pregabalin exhibited antinociceptive effect.…”

Section: Discussionmentioning

confidence: 98%