Chemical modification of the naphthoyl 3-position of JWH-015: in search of a fluorescent probe to the cannabinoid CB 2 receptor

AS Yates, SW Doughty, DA Kendall, B Kellam

Index: Yates, Andrew S.; Doughty, Stephen W.; Kendall, David A.; Kellam, Barrie Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 16 p. 3758 - 3762

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Citation Number: 24

Abstract

In silico modelling was used to guide the positioning of the fluorescent dye NBD-F on the cannabinoid CB2 receptor agonist JWH-015. While the ultimate fluorescent conjugate lost extensive binding affinity to the cannabinoid CB2 receptor, affinity and efficacy studies on the naphthoyl 3-position modified precursor molecules have provided new insight into structure–activity relationships associated with this position.