Kennedy, Nicole M. published the artcileOptimization of a Series of Mu Opioid Receptor (MOR) Agonists with High G Protein Signaling Bias, Category: piperidines, the publication is Journal of Medicinal Chemistry (2018), 61(19), 8895-8907, database is CAplus and MEDLINE.
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, MOR agonists that induce minimal βarrestin-mediated signaling were extensively investigated because MOR agonist-treated βarrestin2 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. It was recently shown that, within a chem. series, the degree of bias correlates linearly with the magnitude of the respiratory safety index. Herein, the synthesis and optimization of (piperidinyl)benzimidazolone MOR agonists I (R1 = H, 4-Cl, 5-Me, 5-CN, 5,6-Cl2, etc.; R2 = H, Me; R3 = Ph, 2-ClC6H4, 2-F-4-BrC6H3, etc.) and analogs that display a wide range of bias (G/βarr2) is described. The structural features affecting potency and maximizing bias were identified and many compounds were shown to have desirable properties, such as long half-lives and high brain penetration.
Journal of Medicinal Chemistry published new progress about 39546-32-2. 39546-32-2 belongs to piperidines, auxiliary class Piperidine,Amine,Amide, name is Piperidine-4-carboxamide, and the molecular formula is C6H12N2O, Category: piperidines.
Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem