Abstract
Aiming at molecular tools for the neuropeptide Y Y1 receptor (Y1R), three types of derivatives of the argininamide-type Y1R antagonist BIBO3304 were prepared by (1) propionylation at the guanidine group (3), (2) substitution at the urea moiety with a propionamidobutyl residue (4) and (3) replacement of ureidomethyl by a propionylaminomethyl group (5). With Ki and Kb values in the range of 1.5-4.3 ...
Abstract
Aiming at molecular tools for the neuropeptide Y Y1 receptor (Y1R), three types of derivatives of the argininamide-type Y1R antagonist BIBO3304 were prepared by (1) propionylation at the guanidine group (3), (2) substitution at the urea moiety with a propionamidobutyl residue (4) and (3) replacement of ureidomethyl by a propionylaminomethyl group (5). With Ki and Kb values in the range of 1.5-4.3 nM, 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 [3H]propionylation according to established protocols.
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