ArticleBioorganic & medicinal chemistry2025
Indazole partial agonists targeting peripheral cannabinoid receptors.
Article in Bioorganic & medicinal chemistry, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Authors and funding
9 authors.
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Abstract
Considerable efforts have been made to produce full agonists of cannabinoid receptors (CBRs), but there has been limited reports on partial agonists and the associated structure activity relationship (SAR) studies. Partial agonists of peripheral CBRs may have unique pharmacological profiles that provide prolonged efficacy through delayed or limited development of tolerance, absent or limited psychiatric effects, and good therapeutic index. Some potential therapeutic applications include inflammatory diseases, gastrointestinal (GI) disorders and pain. In this report, we show the SAR developed in the conversion of indazole full agonists to peripheral partial agonists. Compound 45 is a partial agonist of CBRs with 50% Effective Concentration (EC
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