PMID: 9533642Apr 9, 1998Paper

The neuropeptide Y Y1 antagonist, 1229U91, a potent agonist for the human pancreatic polypeptide-preferring (NPY Y4) receptor

Peptides
D A SchoberD R Gehlert

Abstract

Recently, a novel high-affinity peptide antagonist, 1229U91, was published as a selective neuropeptide Y Y1 antagonist. The selectivity of 1229U91 was evaluated in the human NPY Y1 receptor containing cell line, SK-N-MC, and cells containing the cloned human NPY Y2, the pancreatic polypeptide-preferring (NPY Y4), and the NPY Y5 receptors. 1229U91 potently displaced [125I]-peptide YY (PYY) binding to human NPY Y1 receptors (IC50 = 0.245+/-0.004 nM, n = 4). but displayed little affinity for the human NPY Y2 and Y5 receptors (IC50 > 1000 nM). Interestingly, 1229U91 displaced [125I]-PYY with even greater affinity at the human NPY Y4 receptor (IC50 = 0.081+/-0.009 nM, n = 4). Using a cyclic AMP accumulation assay, 1229U91 blocked NPY inhibition of forskolin-induced adenylate cyclase activity in NPY Y1 receptor containing SK-N-MC cells. In the human NPY Y4 receptor expressing cell line, 1229U91 did not block pancreatic polypeptide (PP) inhibition of forskolin stimulated adenylate cyclase. However, in the absence of PP, 1229U91 was able to inhibit forskolin stimulated cyclic AMP accumulation (IC50 = 7.16+/-2.8 nM, n = 4). We conclude that 1229U91 binds non-selectively with high affinity to both human NPY Y1 and Y4 receptors. Furthermo...Continue Reading

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Citations

Apr 12, 2000·Journal of Peptide Science : an Official Publication of the European Peptide Society·C Cabrele, A G Beck-Sickinger
Nov 6, 2002·Clinica Chimica Acta; International Journal of Clinical Chemistry·Antonio P SilvaEric Grouzmann
May 5, 2000·European Journal of Pharmacology·D E MullinsE M Parker
Jul 11, 2002·European Journal of Pharmacology·Rickard E Malmström
Oct 3, 2002·European Journal of Pharmacology·Michael S ParkerSteven L Parker
May 30, 2002·Neuroscience and Biobehavioral Reviews·Ants KaskRémi Quirion
Apr 5, 2001·Peptides·T L HorvathS P Kalra
Feb 5, 2002·Peptides·Goro KatsuuraAkio Inui
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Mar 22, 2000·British Journal of Pharmacology·Y DumontR Quirion
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May 10, 2002·Genes & Development·Amanda SainsburyHerbert Herzog
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Jul 20, 1999·Journal of Medicinal Chemistry·Y MurakamiM Fujimoto

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