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Readable research linked to original sources
Browse normalized, publication-ready research with direct links to its evidence and source.
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Readable research linked to original sources
Browse normalized, publication-ready research with direct links to its evidence and source.
3 articles
Newest firstCannabinoid receptor type 2 (CB2R) is a prominent class A G protein-coupled receptor (GPCR) and is a therapeutic target of interest for inflammatory diseases, pain management, and neurodegenerative disorders. We report the development of ligands based on HU-308 that share a single central scaffold but bear diverse sidechains, enabling controlled modulation of GPCR activation. Structural modifications at a single p…
Open article record in new tab ↗Purpose The monoacylglycerol lipase (MAGL) plays a pivotal role in modulating the endocannabinoid system and is considered an attractive therapeutic target for diseases in both the central nervous system and periphery. The current study aimed to develop and evaluate a suitable carbon-11 labeled tracer for imaging MAGL in preclinical studies. Methods (R)-YH168 was synthesized via a multi-step pathway and its half-m…
We report a blueprint for the rational design of G protein coupled receptor (GPCR) ligands with a tailored functional response. The present study discloses the structure-based design of cannabinoid receptor type 2 (CB2R) selective inverse agonists (S)-1 and (R)-1, which were derived from privileged agonist HU-308 by introduction of a phenyl group at the gem-dimethylheptyl side chain. Epimer (R)-1 exhibits high aff…
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