A novel neuropeptide Y analog, N-acetyl [Leu28, Leu31]neuropeptide Y-(24–36), with functional specificity for the presynaptic (Y2) receptor

作者: Erica K. Potter , Julian A. Barden , Matthew J.D. McCloskey , Lisa A. Selbie , Albert Tseng

DOI: 10.1016/0922-4106(94)90148-1

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摘要: Abstract We have carried out functional and in vitro studies on a novel analog of neuropeptide Y which shows selectivity for the prejunctional or 2 receptor. In anaesthetised rats N -acetyl [Leu 28 , Leu 31 ]neuropeptide Y-(24–36) attenuates cardiac vagal action (a action) has no significant pressor effects (postjunctional 1 action). human neuroblastoma cell line (SMS-KAN) expresses an endogenous -like receptor, competes with peptide YY binding sites IC 50 0.5 ± 0.1 nM. contrast fibroblast Chinese hamster ovary cloned receptor is used to study changes cytosolic calcium evoked by effect), showed activity even at high concentrations. The steric structure this compound been determined using proton nuclear magnetic resonance (NMR) spectroscopy it consistent C-terminal end published structures Y. suggest acetylation amino acid substitutions stabilise molecule allow bind only

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