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- W3102805119 endingPage "13637" @default.
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- W3102805119 abstract "In this work, we studied a series of carfentanyl amide-based opioid derivatives targeting the mu opioid receptor (μOR) and the delta opioid receptor (δOR) heteromer as a credible novel target in pain management therapy. We identified a lead compound named MP135 that exhibits high G-protein activity at μ-δ heteromers compared to the homomeric δOR or μOR and low β-arrestin2 recruitment activity at all three. Furthermore, MP135 exhibits distinct signaling profile, as compared to the previously identified agonist targeting μ-δ heteromers, CYM51010. Pharmacological characterization of MP135 supports the utility of this compound as a molecule that could be developed as an antinociceptive agent similar to morphine in rodents. In vivo characterization reveals that MP135 maintains untoward side effects such as respiratory depression and reward behavior; together, these results suggest that optimization of MP135 is necessary for the development of therapeutics that suppress the classical side effects associated with conventional clinical opioids." @default.
- W3102805119 created "2020-11-23" @default.
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- W3102805119 date "2020-11-10" @default.
- W3102805119 modified "2023-10-16" @default.
- W3102805119 title "Synthesis and Pharmacology of a Novel μ–δ Opioid Receptor Heteromer-Selective Agonist Based on the Carfentanyl Template" @default.
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- W3102805119 cites W1879282201 @default.
- W3102805119 cites W1902885317 @default.
- W3102805119 cites W1914290984 @default.
- W3102805119 cites W1969179176 @default.
- W3102805119 cites W1977014151 @default.
- W3102805119 cites W1979572916 @default.
- W3102805119 cites W1998878665 @default.
- W3102805119 cites W2003737145 @default.
- W3102805119 cites W2005970620 @default.
- W3102805119 cites W2007476630 @default.
- W3102805119 cites W2009421550 @default.
- W3102805119 cites W2013087295 @default.
- W3102805119 cites W2013107372 @default.
- W3102805119 cites W2015214417 @default.
- W3102805119 cites W2027591014 @default.
- W3102805119 cites W2053216532 @default.
- W3102805119 cites W2054982830 @default.
- W3102805119 cites W2056353612 @default.
- W3102805119 cites W2056384403 @default.
- W3102805119 cites W2063923754 @default.
- W3102805119 cites W2066729230 @default.
- W3102805119 cites W2067086630 @default.
- W3102805119 cites W2073771628 @default.
- W3102805119 cites W2079975546 @default.
- W3102805119 cites W2082645963 @default.
- W3102805119 cites W2083492614 @default.
- W3102805119 cites W2086196752 @default.
- W3102805119 cites W2086618906 @default.
- W3102805119 cites W2086995969 @default.
- W3102805119 cites W2094109627 @default.
- W3102805119 cites W2112698036 @default.
- W3102805119 cites W2122307483 @default.
- W3102805119 cites W2122484765 @default.
- W3102805119 cites W2137585418 @default.
- W3102805119 cites W2138295551 @default.
- W3102805119 cites W2165408834 @default.
- W3102805119 cites W2165671231 @default.
- W3102805119 cites W2218709607 @default.
- W3102805119 cites W2235632662 @default.
- W3102805119 cites W2284011329 @default.
- W3102805119 cites W2344110116 @default.
- W3102805119 cites W2407606194 @default.
- W3102805119 cites W2469589171 @default.
- W3102805119 cites W2507665026 @default.
- W3102805119 cites W2507900361 @default.
- W3102805119 cites W2512819857 @default.
- W3102805119 cites W253726848 @default.
- W3102805119 cites W2584321011 @default.
- W3102805119 cites W2591997013 @default.
- W3102805119 cites W2608001712 @default.
- W3102805119 cites W2751679915 @default.
- W3102805119 cites W2752512915 @default.
- W3102805119 cites W2770319189 @default.
- W3102805119 cites W2793380501 @default.
- W3102805119 cites W2793807943 @default.
- W3102805119 cites W2808792445 @default.
- W3102805119 cites W2810414063 @default.
- W3102805119 cites W2889071092 @default.
- W3102805119 cites W2895856094 @default.
- W3102805119 cites W2900192128 @default.
- W3102805119 cites W2902898515 @default.
- W3102805119 cites W2906251908 @default.
- W3102805119 cites W2914129570 @default.
- W3102805119 cites W2921247428 @default.
- W3102805119 cites W2937061546 @default.
- W3102805119 cites W2948408185 @default.
- W3102805119 cites W2987572976 @default.
- W3102805119 cites W2995508272 @default.
- W3102805119 cites W3085621672 @default.
- W3102805119 cites W3087313941 @default.
- W3102805119 cites W761736724 @default.
- W3102805119 doi "https://doi.org/10.1021/acs.jmedchem.0c00901" @default.
- W3102805119 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/7745089" @default.
- W3102805119 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/33170687" @default.
- W3102805119 hasPublicationYear "2020" @default.