Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner.In a patent, 2879-20-1, name is 1-(2,3-Dihydrobenzo[b][1,4]dioxin-6-yl)ethanone, introducing its new discovery. COA of Formula: C10H10O3
Optimization of a Series of Mu Opioid Receptor (MOR) Agonists with High G Protein Signaling Bias
While mu opioid receptor (MOR) agonists are especially effective as broad-spectrum pain relievers, it has been exceptionally difficult to achieve a clear separation of analgesia from many problematic side effects. Recently, many groups have sought MOR agonists that induce minimal betaarrestin-mediated signaling because MOR agonist-treated betaarrestin2 knockout mice were found to display enhanced antinociceptive effects with significantly less respiratory depression and tachyphylaxis. Substantial data now exists to support the premise that G protein signaling biased MOR agonists can be effective analgesic agents. We recently showed that, within a chemical series, the degree of bias correlates linearly with the magnitude of the respiratory safety index. Herein we describe the synthesis and optimization of piperidine benzimidazolone MOR agonists that together display a wide range of bias (G/betaarr2). We identify structural features affecting potency and maximizing bias and show that many compounds have desirable properties, such as long half-lives and high brain penetration.
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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem