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Dihydropyridine Neuropeptide Y Y1 Receptor Antagonists

Bioorganic & Medicinal Chemistry Letters, 2002
Dihydropyridine 5a was found to be an inhibitor of neuropeptide Y(1) binding in a high throughput (125)I-PYY screening assay. Structure-activity studies around certain portions of the dihydropyridine chemotype identified BMS-193885 (6e) as a potent and selective Y(1) receptor antagonist.
Marc Bruce   +13 more
openaire   +3 more sources

Opposite regulation of hypothalamic orexin and neuropeptide Y receptors and peptide expressions in obese Zucker rats.

Biochemical and Biophysical Research Communications - BBRC, 2001
Many hyothalamic neuropeptides are involved in the regulation of food intake and body weight. The orexins (OX) which are synthesized in the lateral hypothalamus are among the most recently characterized whereas neuropeptide Y (NPY) belongs to a group of "
B. Beck   +3 more
semanticscholar   +1 more source

Neuropeptide Y Receptor in Vascular Smooth Muscle

Journal of Neurochemistry, 1991
Abstract: 125I‐Bolton‐Hunter (125I‐BH) neuropeptide Y (NPY) was used to identify specific high‐affinity NPY binding sites in porcine aortic smooth muscle membrane fractions and to characterize the binding sites in comparison with those in porcine hippocampal membrane fractions.
Yasushi Shigeri   +2 more
openaire   +3 more sources

Multiple neuropeptide Y receptors regulate K+ and Ca2+ channels in acutely isolated neurons from the rat arcuate nucleus.

Journal of Neurophysiology, 1999
We examined the effects of neuropeptide Y (NPY) and related peptides on Ca2+ and K+ currents in acutely isolated neurons from the arcuate nucleus of the rat.
Lihjen Sun, Richard J. Miller
semanticscholar   +1 more source

Neuropeptide Y Y1 receptors in vascular pharmacology

European Journal of Pharmacology, 1998
The existence of neurogenic mediator candidates apart from noradrenaline and acetylcholine involved in the control of vascular tone has attracted enormous attention during the past few decades. One such mediator is neuropeptide Y (NPY), which is co-localized with noradrenaline in sympathetic perivascular nerves.
Jan Liska, Anders Franco-Cereceda
openaire   +2 more sources

Neuropeptide Y as a partial agonist of the Y1 receptor

European Journal of Pharmacology, 2005
In absence of receptor cycling, human/rat neuropeptide Y was found to persistently occupy the guinea pig neuropeptide Y Y1 receptors expressed on the surface of Chinese hamster ovary (CHO) cells (IC50 approximately 8 nM); a lasting occupancy was also evident with active receptor cycling.
Michael S. Parker   +4 more
openaire   +3 more sources

Multiplicity of neuropeptide Y receptors: cloning of a third distinct subtype in the zebrafish.

Biochemical and Biophysical Research Communications - BBRC, 1997
Five different receptor subtypes for neuropeptide Y (NPY) have recently been cloned in mammals. We have discovered three distinct subtypes by PCR in the zebrafish, Danio rerio, and describe here one of these called zYc.
Maria Ringvall   +2 more
semanticscholar   +1 more source

Neuropeptide Y Receptor Subtypes, Y1 and Y2

Annals of the New York Academy of Sciences, 1990
Heterogeneity among NPY (and PYY) receptors was first proposed on the basis of studies on sympathetic neuroeffector junctions, where NPY (and PYY) can exert three types of action: 1) a direct (e.g., vasoconstrictor) response; 2) a postjunctional potentiating effect on NE-evoked vasoconstriction; and 3) a prejunctional suppression of stimulated NE ...
Claes Wahlestedt   +6 more
openaire   +3 more sources

Effect of a selective neuropeptide Y Y2 receptor antagonist, BIIE0246 on neuropeptide Y release

European Journal of Pharmacology, 2000
We have examined the selective neuropeptide Y Y(2) receptor antagonist, (S)-N(2)-[[1-[2-[4-[(R,S)-5,11-dihydro-6(6h)-oxodibenz[b, e]azepin-11-yl]-1-piperazinyl]-2-oxoethyl]cyclopentyl]acetyl ]-N-[2-[1 ,2-dihydro-3,5(4H)-dioxo-1,2-diphenyl-3-H-1,2, 4-triazol-4-yl]ethyl]-argininamid (BIIE0246) on neuropeptide release from rat hypothalamic slices in vitro.
Peter S. Widdowson   +3 more
openaire   +3 more sources

Neuropeptide Y potentiates noradrenaline-induced contraction through the neuropeptide Y Y1 receptor

European Journal of Pharmacology, 1996
To elucidate which neuropeptide Y receptor subtype is responsible for the neuropeptide Y-induced potentiation of the noradrenaline-evoked contraction in human omental arteries we used antisense oligodeoxynucleotide (Antisense), the new selective neuropeptide Y Y1 receptor antagonist, BIBP3226 {(R)-N2-(diphenylacetyl)-N-[(4-hydroxyphenyl) methyl]-D ...
Torun Nilsson   +15 more
openaire   +3 more sources

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