Abstract
New, short-linker BODIPY 630/650™ fluorescent conjugates of the adenosine receptor ligand N-ethylcarboxamido-adenosine (NECA) have been synthesised and pharmacologically evaluated. These novel conjugates confirm that short linkers between the N6-amino group of NECA and the fluorophore are preferred with the best ligand (15b, aminopropyl linker) displaying the greatest potency (Log IC50 (Gi) = −9.31) at the human adenosine A1-receptor. Imaging studies with this compound confirmed it can be employed to selectively label the human adenosine A1-receptor in single living cells, with receptor-associated binding prevented by preincubation with the nonfluorescent antagonist DPCPX.
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
