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- W2599696978 abstract "Opioids are a mainstay for treatment of acute and chronic pain. However, chronic use leads to a host of adverse events including tolerance and opioid-induced hyperalgesia (OIH), complicating pain management and diminishing patient compliance. OIH has been described in patient populations with high usage of opioids, where patients paradoxically experience exaggerated nociceptive responses instead of pain reduction. Here, we describe the pharmacological properties of TRV9101, a novel μ receptor G protein Pathway Selective (μ-GPS) modulator—a close analog of oliceridine (TRV130)—that activates G proteins while causing low β-arrestin recruitment to the μ receptor. OIH was evaluated via mechanical allodynia over 7 days in mice administered with a chronic infusion of vehicle, TRV9101, fentanyl, morphine, or oxycodone using doses that elicit similar analgesic efficacy. Analgesia was evaluated in a parallel thermal hot plate assay using the same mice. Reversal of morphine-induced hyperalgesia was evaluated via the following: mice were dosed twice daily (s.c.) with vehicle or morphine for 4 days (20mg/kg); on day 5, morphine-treated mice were reassigned and dose twice daily (s.c.) to vehicle, morphine or TRV9101 for 8 additional days. While continuous infusion of morphine, fentanyl and oxycodone promoted significant and sustained hyper-responsiveness to innocuous mechanical stimuli beginning day 2, TRV9101 did not induce allodynia, similar to vehicle, throughout the same dosing paradigm (p<0.001 for morphine, oxycodone, fentanyl versus vehicle). After a single dose, TRV9101 promoted acute reversal of morphine-induced hyperalgesia and provided sustained reversal after 7 days of repeat dosing. In the hot plate assay, TRV9101 displayed similar analgesic efficacy to morphine, fentanyl and oxycodone. These results suggest that long term use of a μ-GPS modulator such as TRV9101 may provide maintenance of analgesia with reduced risk of opioid-induced hyperalgesia. This study was supported by Trevena, Inc." @default.
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- W2599696978 date "2017-04-01" @default.
- W2599696978 modified "2023-09-27" @default.
- W2599696978 title "(224) Assessment of Nociceptive Sensitization with TRV9101, a Novel μ Receptor G Protein Pathway Selective Modulator (μ-GPS), versus Fentanyl, Morphine, and Oxycodone" @default.
- W2599696978 doi "https://doi.org/10.1016/j.jpain.2017.02.116" @default.
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