Allosteric modulation of G protein-coupled receptors (GPCR) is a rapidly advancing area of drug discovery with considerable therapeutic potential. In this study, we used various bioluminescence resonance energy transfer (BRET) assay configurations to investigate the differential activity of LY3154207, a dopamine D1 rec...
Anh Minh Nguyen, Hayato Umaoka, Hideaki Yano· bioRxiv· 0 citations
Dopamine D1 receptors (D1R) and muscarinic M4 receptors (M4R) regulate overlapping functions in the cortex and the striatum, but the cellular relationship between D1R- and M4R-associated populations across brain regions remains incompletely defined. Using D1R-tdTomato/M4R-EGFP double-reporter mice, we quantified tdToma...
Rian Garland, Maya Dickson, Alice J. Lee et al.· bioRxiv· 0 citations
The full efficacy range of ligands at CB1 and CB2 (i.e., inverse agonists, neutral agonists, partial agonists, full agonists, and high-efficacy agonists) has been reported collectively across numerous laboratories and assay platforms. Canonical Gi/o and β-arrestin signaling have each been suggested to shape physiologic...
Soo Jung Oh, Christopher Lucaj, Kiera Truong et al.· bioRxiv· 0 citations
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