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• W2788126937 endingPage "2103" @default.
• W2788126937 startingPage "2087" @default.
• W2788126937 abstract "The adenosine A1 receptor (A1AR) is a potential novel therapeutic target for myocardial ischemia-reperfusion injury. However, to date, clinical translation of prototypical A1AR agonists has been hindered due to dose limiting adverse effects. Recently, we demonstrated that the biased bitopic agonist 1, consisting of an adenosine pharmacophore linked to an allosteric moiety, could stimulate cardioprotective A1AR signaling in the absence of unwanted bradycardia. Therefore, this study aimed to investigate the structure–activity relationship of compound 1 biased agonism. A series of novel derivatives of 1 were synthesized and pharmacologically profiled. Modifications were made to the orthosteric adenosine pharmacophore, linker, and allosteric 2-amino-3-benzoylthiophene pharmacophore to probe the structure–activity relationships, particularly in terms of biased signaling, as well as A1AR activity and subtype selectivity. Collectively, our findings demonstrate that the allosteric moiety, particularly the 4-(trifluoromethyl)phenyl substituent of the thiophene scaffold, is important in conferring bitopic ligand bias at the A1AR." @default.
• W2788126937 created "2018-03-06" @default.
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• W2788126937 date "2018-02-15" @default.
• W2788126937 modified "2023-09-29" @default.
• W2788126937 title "A Structure–Activity Relationship Study of Bitopic <i>N</i>⁶-Substituted Adenosine Derivatives as Biased Adenosine A₁ Receptor Agonists" @default.
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• W2788126937 doi "https://doi.org/10.1021/acs.jmedchem.8b00047" @default.
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• W2788126937 hasPublicationYear "2018" @default.
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