Abstract
Aiming at molecular tools for the neuropeptide Y Y-1 receptor (Y1R), three types of derivatives of the argininamide-type Y1R antagonist BIBO3304 were prepared by (i) propionylation at the guanidine group (3), (ii) substitution at the urea moiety with a propionamidobutyl residue (4), and (iii) replacement of ureidomethyl by a propionylaminomethyl group (5). With K-i and K-b values in the range of ...
Abstract
Aiming at molecular tools for the neuropeptide Y Y-1 receptor (Y1R), three types of derivatives of the argininamide-type Y1R antagonist BIBO3304 were prepared by (i) propionylation at the guanidine group (3), (ii) substitution at the urea moiety with a propionamidobutyl residue (4), and (iii) replacement of ureidomethyl by a propionylaminomethyl group (5). With K-i and K-b values in the range of 1.5-4.3nM, determined in binding and functional assays, and high selectivity for the Y1R over the Y2R, Y4R, and Y5R, compounds 4 and 5 were identified as promising candidates for radiolabeling by [H-3]propionylation according to established protocols.