NMP-7 inhibits chronic inflammatory and neuropathic pain via block of Cav3.2 T-type calcium channels and activation of CB2 receptors.
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Additional excerpts
...2 channels (Berger et al., 2014)....
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Cites background from "NMP-7 inhibits chronic inflammatory..."
...More recently, a series of novel DHP derivatives with a condensed hexahydroquinoline 1,4-DHP ring system were identified (Bladen et al., 2014)....
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Cites background from "NMP-7 inhibits chronic inflammatory..."
...2 blocker SNI model analgesic effect (Berger et al., 2014) Suramin and the flavonoid gossypetin USP5-Cav3....
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...2 T-type channel blocker, was shown to mediate a significant analgesic effect in the model of neuropathic pain (Berger et al. , 2014)....
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References
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"NMP-7 inhibits chronic inflammatory..." refers background in this paper
...produce analgesia in mice with peripheral nerve injuries, altogether indicating that both T-type calcium channels and CB2 receptors are important targets for treating neuropathic pain [28]....
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"NMP-7 inhibits chronic inflammatory..." refers methods in this paper
...To investigate the extent of CB2 receptor involvement, the CB2 antagonist AM630 was delivered 15 minutes prior to NMP-7 treatment or URB597 treatment, which was used as a positive control....
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...%) and PBS. Selective CB1 antagonist AM281, irreversible inhibitor of monoacylglycerol lipase JZL184 [32,33], selective CB2 antagonist AM630, and the irreversible inhibitor of fatty acid amide hydrolase URB597 [34] were provided by Cayman Chemical, and dissolved in phosphate buffered saline (PBS) and dimethyl sulfoxide (DMSO) to 5%....
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...AM630 also reversed the analgesic effect of URB597 (10 mg/kg, i.p., an inhibitor of fatty acid amide hydrolase, the primary degradatory enzyme for the endocannabinoid anandamide), which was used as positive control (Two-way ANOVA, p 0.01) (Figure 6A)....
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...Selective CB1 antagonist AM281, irreversible inhibitor of monoacylglycerol lipase JZL184 [32,33], selective CB2 antagonist AM630, and the irreversible inhibitor of fatty acid amide hydrolase URB597 [34] were provided by Cayman Chemical, and dissolved in phosphate buffered saline (PBS) and dimethyl sulfoxide (DMSO) to 5%....
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"NMP-7 inhibits chronic inflammatory..." refers background in this paper
...knockdown [7,8] or inhibition of the T-type calcium channel by T-type channel modulators produce significant antinociceptive effects in vivo [9-13]....
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...Inhibition of T-type channels or in vivo antisense-mediated knockdown produces antinociception in these and other models of chronic pain [7-16]....
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107 citations