Literature DB >> 7568074

High-affinity neuropeptide Y receptor antagonists.

A J Daniels1, J E Matthews, R J Slepetis, M Jansen, O H Viveros, A Tadepalli, W Harrington, D Heyer, A Landavazo, J J Leban, A Spaltenstein.   

Abstract

Neuropeptide Y (NPY) is one of the most abundant peptide transmitters in the mammalian brain. In the periphery it is costored and coreleased with norepinephrine from sympathetic nerve terminals. However, the physiological functions of this peptide remain unclear because of the absence of specific high-affinity receptor antagonists. Three potent NPY receptor antagonists were synthesized and tested for their biological activity in in vitro, ex vivo, and in vivo functional assays. We describe here the effects of these antagonists inhibiting specific radiolabeled NPY binding at Y1 and Y2 receptors and antagonizing the effects of NPY in human erythroleukemia cell intracellular calcium mobilization perfusion pressure in the isolated rat kidney, and mean arterial blood pressure in anesthetized rats.

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Year:  1995        PMID: 7568074      PMCID: PMC40925          DOI: 10.1073/pnas.92.20.9067

Source DB:  PubMed          Journal:  Proc Natl Acad Sci U S A        ISSN: 0027-8424            Impact factor:   11.205


  22 in total

1.  The first highly potent and selective non-peptide neuropeptide Y Y1 receptor antagonist: BIBP3226.

Authors:  K Rudolf; W Eberlein; W Engel; H A Wieland; K D Willim; M Entzeroth; W Wienen; A G Beck-Sickinger; H N Doods
Journal:  Eur J Pharmacol       Date:  1994-12-27       Impact factor: 4.432

Review 2.  Structure-activity relationships of neuropeptide Y analogues with respect to Y1 and Y2 receptors.

Authors:  A G Beck-Sickinger; G Jung
Journal:  Biopolymers       Date:  1995       Impact factor: 2.505

3.  Neuropeptide Y--a novel brain peptide with structural similarities to peptide YY and pancreatic polypeptide.

Authors:  K Tatemoto; M Carlquist; V Mutt
Journal:  Nature       Date:  1982-04-15       Impact factor: 49.962

Review 4.  Neuropeptide Y: anatomical distribution and possible function in mammalian nervous system.

Authors:  T S Gray; J E Morley
Journal:  Life Sci       Date:  1986-02-03       Impact factor: 5.037

5.  Evidence for different pre-and post-junctional receptors for neuropeptide Y and related peptides.

Authors:  C Wahlestedt; N Yanaihara; R Håkanson
Journal:  Regul Pept       Date:  1986-02

6.  [Leu31, Pro34]neuropeptide Y: a specific Y1 receptor agonist.

Authors:  J Fuhlendorff; U Gether; L Aakerlund; N Langeland-Johansen; H Thøgersen; S G Melberg; U B Olsen; O Thastrup; T W Schwartz
Journal:  Proc Natl Acad Sci U S A       Date:  1990-01       Impact factor: 11.205

7.  Characterization of functional neuropeptide Y receptors in a human neuroblastoma cell line.

Authors:  E A Gordon; T A Kohout; P H Fishman
Journal:  J Neurochem       Date:  1990-08       Impact factor: 5.372

8.  Neuropeptide Y mobilizes intracellular Ca2+ and increases inositol phosphate production in human erythroleukemia cells.

Authors:  A J Daniels; E R Lazarowski; J E Matthews; E G Lapetina
Journal:  Biochem Biophys Res Commun       Date:  1989-12-29       Impact factor: 3.575

9.  Comparative immunohistochemical and biochemical analysis of pancreatic polypeptide-like peptides with special reference to presence of neuropeptide Y in central and peripheral neurons.

Authors:  J M Lundberg; L Terenius; T Hökfelt; K Tatemoto
Journal:  J Neurosci       Date:  1984-09       Impact factor: 6.167

10.  Neuropeptide Y distribution in human brain.

Authors:  T E Adrian; J M Allen; S R Bloom; M A Ghatei; M N Rossor; G W Roberts; T J Crow; K Tatemoto; J M Polak
Journal:  Nature       Date:  1983 Dec 8-14       Impact factor: 49.962

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  13 in total

1.  [(125)I]-GR231118: a high affinity radioligand to investigate neuropeptide Y Y(1) and Y(4) receptors.

Authors:  Y Dumont; R Quirion
Journal:  Br J Pharmacol       Date:  2000-01       Impact factor: 8.739

2.  BIIE0246, a potent and highly selective non-peptide neuropeptide Y Y(2) receptor antagonist.

Authors:  Y Dumont; A Cadieux; H Doods; L H Pheng; R Abounader; E Hamel; D Jacques; D Regoli; R Quirion
Journal:  Br J Pharmacol       Date:  2000-03       Impact factor: 8.739

3.  Constitutive neuropeptide Y Y(4) receptor expression in human colonic adenocarcinoma cell lines.

Authors:  H M Cox; I R Tough; D W Zandvliet; N D Holliday
Journal:  Br J Pharmacol       Date:  2001-01       Impact factor: 8.739

4.  In Vitro Mouse and Human Serum Stability of a Heterobivalent Dual-Target Probe That Has Strong Affinity to Gastrin-Releasing Peptide and Neuropeptide Y1 Receptors on Tumor Cells.

Authors:  Arijit Ghosh; Natarajan Raju; Michael Tweedle; Krishan Kumar
Journal:  Cancer Biother Radiopharm       Date:  2017-02       Impact factor: 3.099

5.  Discrimination between neuropeptide Y and peptide YY in the rat tail artery by the neuropeptide Y1-selective antagonist, BIBP 3226.

Authors:  H Gicquiaux; M Tschöpl; H N Doods; B Bucher
Journal:  Br J Pharmacol       Date:  1996-12       Impact factor: 8.739

6.  Development and characterization of a highly selective neuropeptide Y Y5 receptor agonist radioligand: [125I][hPP1-17, Ala31, Aib32]NPY.

Authors:  Yvan Dumont; Mira Thakur; Annette Beck-Sickinger; Alain Fournier; Rémi Quirion
Journal:  Br J Pharmacol       Date:  2003-08       Impact factor: 8.739

Review 7.  Neuropeptide Y: a physiological orexigen modulated by the feedback action of ghrelin and leptin.

Authors:  Satya P Kalra; Pushpa S Kalra
Journal:  Endocrine       Date:  2003-10       Impact factor: 3.633

8.  Synthesis and characterization of a selective peptide antagonist of neuropeptide Y vascular postsynaptic receptors.

Authors:  M J Lew; R Murphy; J A Angus
Journal:  Br J Pharmacol       Date:  1996-04       Impact factor: 8.739

9.  Expression and characterization of the neuropeptide Y Y5 receptor subtype in the rat brain.

Authors:  Y Dumont; A Fournier; R Quirion
Journal:  J Neurosci       Date:  1998-08-01       Impact factor: 6.167

10.  Neuropeptide Y: A hypothalamic brake restraining the onset of puberty in primates.

Authors:  M El Majdoubi; A Sahu; S Ramaswamy; T M Plant
Journal:  Proc Natl Acad Sci U S A       Date:  2000-05-23       Impact factor: 11.205

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