T-0632, a proven reverse agonist to several Class B G-protein coupled receptors including CCKA, CCKB, and GLP-1R, can be modified to provide deeper insight into the binding sites of said GPCRs. By incorporating a photolabile azido moiety into the structure of T-0632, binding between the small molecule and the receptor binding site is possible upon exposure to ultraviolet light. This covalent interaction can provide details of the T-0632 binding in GPCRs. Synthesis of the azido T-0632 analog will be presented.

Synthesis towards a reverse agonist photolabile ligand

245th National Meeting (2013)

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