Involvement of the long-chain fatty acid receptor GPR40 as a novel pain regulatory system

Nakamoto, Kazuo; Nishinaka, Takashi; Matsumoto, Kengo; Kasuya, Fumiyo; Mankura, Mitsumasa; Kōyama, Yutaka; Tokuyama, Shogo

doi:10.1016/j.brainres.2011.11.012

Cited by 120 publications

(86 citation statements)

References 45 publications

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“…The doses of GW9508, DHA, and GW1100 were chosen based upon our previous reports (Nakamoto et al, 2012.…”

Section: Drugsmentioning

confidence: 99%

“…We recently reported that DHA and/or GW9508, a GPR40 agonist, have suppressive effects on pain behavior elicited by formalin, acetic acid and a complete Freund's adjuvant. These effects appear to be mediated through the release of β-endorphin, an endogenous opioid peptide, which is stimulated by GPR40 signaling in the supraspinal region (Nakamoto et al, 2010(Nakamoto et al, , 2011(Nakamoto et al, , 2012. GPR40 is a member of the large family of seven-transmembrane receptors referred to as G-proteincoupled receptors, and is known to be activated by long-chain fatty acids such as DHA and eicosapentaenoic acid (EPA) (Hirasawa et al, 2008).…”

Section: Introductionmentioning

confidence: 98%

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Involvement of GPR40, a long-chain free fatty acid receptor, in the production of central post-stroke pain after global cerebral ischemia

Harada

Haruna

Aizawa

et al. 2014

European Journal of Pharmacology

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“…The doses of GW9508, DHA, and GW1100 were chosen based upon our previous reports (Nakamoto et al, 2012.…”

Section: Drugsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 98%

Involvement of GPR40, a long-chain free fatty acid receptor, in the production of central post-stroke pain after global cerebral ischemia

Harada

Haruna

Aizawa

et al. 2014

European Journal of Pharmacology

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“…6,34) The sections were then incubated in specific antibodies against PtdIns(4,5) P2 (1 : 100 dilution), ezrin ( Statistical Analysis Data are expressed as the mean± S.E.M. Statistical significance was assessed using the unpaired Student's t-test or one-way ANOVA, followed by Scheffé's test for single or multiple comparisons, respectively.…”

Section: )mentioning

confidence: 99%

Changes in PtdIns(4,5)P2 Induced by Etoposide Treatment Modulates Small Intestinal P-Glycoprotein <i>via</i> Radixin

Kobori

Harada

Nakamoto

et al. 2014

Biological & Pharmaceutical Bulletin

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Previously, we reported that repeated oral administration of etoposide (ETP) increases P-glycoprotein (P-gp) expression in association with activation of ezrin/radixin/moesin (ERM) via Ras homolog gene family member A (RhoA)/Rho-associated coiled-coil containing protein kinase (ROCK) signaling in the small intestine. However, the detailed mechanisms of this pathway have yet to be fully elucidated. Recently, phosphatidylinositol 4,5-bisphosphate [PtdIns(4,5)P2], one of the most abundant phosphoinositides in the plasma membrane, has attracted attention regarding its involvement in the plasma membrane localization of various membrane proteins. PtdIns(4,5)P2 is an essential factor in the dissociation and subsequent membrane translocation (activation) of ERM, and its synthetic pathway is known to be highly regulated by RhoA/ROCK signaling. Here, we examined the involvement of PtdIns(4,5)P2 in the mechanism by which ETP treatment increases small intestinal P-gp levels, and we determined which protein within ERM contributes to this phenomenon. Key words P-glycoprotein; radixin; phosphatidylinositol 4,5-bisphosphate (PtdIns(4,5)P2); Ras homolog gene family member A (RhoA); Rho-associated coiled-coil containing protein kinase (ROCK); small intestine We previously reported that repeated oral treatment with etoposide (ETP), an anticancer drug that is a substrate for Pglycoprotein (P-gp), 1) activates ezrin/radixin/moesin (ERM), which are scaffold proteins for P-gp in the small intestine. 2,3)Activated ERM may in turn increase P-gp expression in the plasma membrane of the small intestine under ETP treatment.2,3) ERM activation is regulated by Ras homolog gene family member A (RhoA) and Rho-associated coiled-coil containing protein kinase (ROCK) signaling, as demonstrated in our previous studies 2,3) and others. 4,5) In our reports we proposed the possibility that of the ERM proteins, radixin may contribute to the above phenomena more than ezrin or moesin 6)

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“…of β-endorphin, mediated (at least in part) through GPR40 signaling, and finally the stimulation of μ-and δ-opioid receptors induced antinociception [120]. Analgesic action of the epoxidized metabolites derived from omega-3 PUFAs DHA (epoxydocosapentaenoic 2.…”

Section: Omega-3 Fatty Acids Combined With Morphinementioning

confidence: 99%

Innovations in Pain Management: Morphine Combined with Omega-3 Fatty Acids

Laino¹

2017

TOPROCJ

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Abstract:The treatment of acute and chronic severe pain remains a common major challenge faced by clinicians working with the general population, and even after the application of recent advances to treatments, there may still continue to be manifestations of adverse effects.Chronic pain affects the personal and social life of the patient, and often also their families. In some cases, after an acute pain the patient continues to experience chronic pain, which can be a result of diseases such as cancer.Morphine is recommended as the first choice opioid in the treatment of moderate to severe acute and chronic pain. However, the development of adverse effects and tolerance to the analgesic effects of morphine often leads to treatment discontinuation. The present work reviews the different pharmaceutical innovations reported concerning the use of morphine. First, its utilization as the first medication for the treatment of moderate to severe cancer pain and non-cancer pain in patients is evaluated, taking into account the most common complications and adverse effects. Next, strategies utilized to manage these side effects are considered, and we also summarize results using omega-3 fatty acids (eicosapentaenoic acid and docosahexaenoic acid) as a monotherapy or as an adjunct to morphine in the treatment of pain.

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Involvement of the long-chain fatty acid receptor GPR40 as a novel pain regulatory system

Cited by 120 publications

References 45 publications

Involvement of GPR40, a long-chain free fatty acid receptor, in the production of central post-stroke pain after global cerebral ischemia

Involvement of GPR40, a long-chain free fatty acid receptor, in the production of central post-stroke pain after global cerebral ischemia

Changes in PtdIns(4,5)P2 Induced by Etoposide Treatment Modulates Small Intestinal P-Glycoprotein <i>via</i> Radixin

Innovations in Pain Management: Morphine Combined with Omega-3 Fatty Acids

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