High affinity agonists of the neuropeptide Y (NPY) Y4 receptor derived from the C-terminal pentapeptide of human pancreatic polypeptide (hPP): synthesis, stereochemical discrimination and radiolabeling

Kuhn, Kilian K., Ertl, Thomas, Dukorn, Stefanie, Keller, Max, Bernhardt, Günther, Reiser, Oliver und Buschauer, Armin (2016) High affinity agonists of the neuropeptide Y (NPY) Y4 receptor derived from the C-terminal pentapeptide of human pancreatic polypeptide (hPP): synthesis, stereochemical discrimination and radiolabeling. Journal of Medicinal Chemistry 59 (13), S. 6045-6058.

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Zusammenfassung

The diastereomeric mixture of D/L-2,7-diaminooctanedioyl-bis(YRLRY-NH2) (BVD-74D, 2) was described in the literature as a high affinity Y4 receptor agonist. Here we report on the synthesis and pharmacological characterization of the pure diastereomers (2R,7R)- and (2S,7S)-2 and a series of homo- and heterodimeric analogues in which octanedioic acid was used as an achiral linker. To investigate ...

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