Central Administration of BIBP3226, Neuropeptide Y (NPY) Y1 Receptor Antagonist, does not Inhibit Fasting- and NPY-Induced Food Intake in Neonatal Chicks

2001 ◽  
Vol 38 (4) ◽  
pp. 259-265 ◽  
Author(s):  
Shin-ichi Kawakami ◽  
Ryuichi Ando ◽  
Takashi Bungo ◽  
Atsushi Ohgushi ◽  
Tetsuya Tachibana ◽  
...  
Keyword(s):  
Food Intake ◽  
Neuropeptide Y ◽  
Receptor Antagonist ◽  
Central Administration ◽  
Y1 Receptor ◽  
Neonatal Chicks

scholarly journals Peripheral and Central Administration of a Selective Neuropeptide Y Y1 Receptor Antagonist Suppresses Ethanol Intake by C57BL/6J Mice

2004 ◽  
Vol 28 (9) ◽  
pp. 1324-1330 ◽  
Author(s):  
Dennis R. Sparta ◽  
Jon R. Fee ◽  
Dayna M. Hayes ◽  
Darin J. Knapp ◽  
Douglas J. MacNeil ◽  
...  
Keyword(s):  
Neuropeptide Y ◽  
Receptor Antagonist ◽  
Ethanol Intake ◽  
Central Administration ◽  
Y1 Receptor

scholarly journals Potent neuropeptide Y Y1 receptor antagonist, 1229U91: blockade of neuropeptide Y-induced and physiological food intake.

Endocrinology ◽  
1996 ◽  
Vol 137 (8) ◽  
pp. 3177-3182 ◽  
Author(s):  
A Kanatani ◽  
A Ishihara ◽  
S Asahi ◽  
T Tanaka ◽  
S Ozaki ◽  
...  
Keyword(s):  
Food Intake ◽  
Neuropeptide Y ◽  
Receptor Antagonist ◽  
Y1 Receptor

Orexigenic effect of the melanocortin MC4 receptor antagonist HS014 is inhibited only partially by neuropeptide Y Y1 receptor selective antagonists

2000 ◽  
Vol 78 (2) ◽  
pp. 143-149 ◽  
Author(s):  
Ants Kask ◽  
Helgi B Schiöth ◽  
Jaanus Harro ◽  
Jarl ES Wikberg ◽  
Lembit Rägo
Keyword(s):  
Food Intake ◽  
Neuropeptide Y ◽  
Receptor Antagonist ◽  
Male Rats ◽  
Receptor Antagonists ◽  
Y1 Receptor ◽  
Npy Receptor ◽  
Inhibit Food Intake ◽  
In Vitro Data

Neuropeptide Y (NPY) and melanocortin (MC) peptides have opposite effects on food intake: NPY-like peptides and MC receptor antagonists stimulate feeding and increase body weight, whereas melanocortins and NPY antagonists inhibit food intake. In this study we tested whether the orexigenic effect of the selective MC4 receptor antagonist HS014 (1 nmol) could be inhibited by three different NPY antagonists, (R)-N2-(diphenylacetyl)-N-[(4-hydroxy-phenyl)methyl]- D-argininamide (BIBP3226), (R)-N-[[4-(aminocarbonylaminomethyl)-phenyl]methyl]-N2-(diphenylacetyl)-argininamide-trifluoroacetate (BIBO3304), and decapeptide [D-Tyr27,36D-Thr32]NPY27-36, after icv administration in freely feeding male rats. All three NPY receptor antagonists inhibited the orexigenic effects of HS014 partially and with markedly different potency. [D-Tyr27,36D-Thr32]NPY27-36 was active only in subconvulsive dose. The NPY Y1 selective antagonist BIBP3226 was more effective in inhibiting the effect of HS014 than BIBO3304 despite in vitro data indicating that BIBP3226 is about 10 times less potent than BIBO3304 at NPY Y1 receptor. An enantiomer of BIBO3304, BIBO3457, failed to inhibit HS014-induced feeding, indicating that the effects of BIBO3304 were stereoselective. These results suggest that stimulation of food intake caused by weakening of melanocortinergic tone at the MC4 receptor is partially but not exclusively related to NPY Y1 receptor activation.Key words: neuropeptide Y, NPY Y1 receptor antagonist, BIBO3304, BIBP3226, [D-Tyr27,36D-Thr32]NPY(27-36), 1229U91, food intake, MC4 receptor antagonist, HS014.

scholarly journals Evidence That the Inhibition of Luteinizing Hormone Secretion Exerted by Central Administration of Neuropeptide Y (NPY) in the Rat Is Predominantly Mediated by the NPY-Y5 Receptor Subtype1

Endocrinology ◽  
1999 ◽  
Vol 140 (9) ◽  
pp. 4046-4055 ◽  
Author(s):  
Paula D. Raposinho ◽  
Pierre Broqua ◽  
Dominique D. Pierroz ◽  
Amanda Hayward ◽  
Yvan Dumont ◽  
...  
Keyword(s):  
Food Intake ◽  
Neuropeptide Y ◽  
Receptor Antagonist ◽  
Pancreatic Polypeptide ◽  
Inhibitory Action ◽  
Receptor Subtypes ◽  
Y1 Receptor ◽  
Npy Receptor ◽  
Gonadotropic Axis ◽  
Lh Secretion

Abstract A number of studies have indicated that neuropeptide Y (NPY) is a central regulator of the gonadotropic axis, and the Y1 receptor was initially suggested to be implicated. As at least five different NPY receptor subtypes have now been characterized, the aim of the present study was to reinvestigate the pharmacological profile of the receptor(s) mediating the inhibitory action of NPY on LH secretion by using a panel of NPY analogs with different selectivity toward the five NPY receptor subtypes. When given intracerebroventricularly (icv) to castrated rats, a bolus injection of native NPY (0.7–2.3 nmol) dose-dependently decreased plasma LH. Peptide YY (PYY; 2.3 nmol) was as potent as NPY, suggesting that the Y3 receptor is not implicated. Confirming previous data, the mixed Y1, Y4, and Y5 agonist[ Leu31,Pro34]NPY (0.7–2.3 nmol) inhibited LH release with potency and efficacy equal to those of NPY. Neither the selective Y2 agonist C2-NPY (2.3 nmol) nor the selective Y4 agonist rat pancreatic polypeptide affected plasma LH, excluding Y2 and Y4 subtypes for the action of NPY on LH secretion. The mixed Y4-Y5 agonist human pancreatic polypeptide (0.7–7 nmol) as well as the mixed Y2-Y5 agonist PYY3–36 (0.7–7 nmol) that displayed very low affinity for the Y1 receptor, thus practically representing selective Y5 agonists in this system, decreased plasma LH with potency and efficacy similar to those of NPY, indicating that the Y5 receptor is mainly involved in this inhibitory action of NPY on LH secretion.[ d-Trp32]NPY, a selective, but weak, Y5 agonist, also inhibited plasma LH at a dose of 7 nmol. Furthermore, the inhibitory action of NPY (0.7 nmol) on LH secretion could be fully prevented, in a dose-dependent manner (6–100 μg, icv), by a nonpeptidic Y5 receptor antagonist. This antagonist (60 μg, icv) also inhibited the stimulatory action of NPY (0.7 nmol) on food intake. The selectivity of PYY3–36, human PP,[ d-Trp32]NPY, and the Y5 antagonist for the Y5 receptor subtype was further confirmed by their ability to inhibit the specific[ 125I][Leu31,Pro34]PYY binding to rat brain membrane homogenates in the presence of the Y1 receptor antagonist BIBP3226, a binding assay system that was described as being highly specific for Y5-like receptors. With the exception of[ d-Trp32]NPY, all analogs able to inhibit LH secretion were also able to stimulate food intake. Taken together, these results indicate that the Y5 receptor is involved in the negative control by NPY of the gonadotropic axis.

Regulation of food intake by neuropeptide Y in goldfish

2000 ◽  
Vol 279 (3) ◽  
pp. R1025-R1034 ◽  
Author(s):  
Yuwaraj K. Narnaware ◽  
Pierre P. Peyon ◽  
Xinwei Lin ◽  
Richard E. Peter
Keyword(s):  
Food Intake ◽  
Neuropeptide Y ◽  
Mrna Levels ◽  
Food Ration ◽  
Y1 Receptor ◽  
Daily Food ◽  
Daily Food Ration ◽  
Brain Ventricle ◽  
Dose Dependent Increase ◽  
Dose Dependent

In mammals, neuropeptide Y (NPY) is a potent orexigenic factor. In the present study, third brain ventricle (intracerebroventricular) injection of goldfish NPY (gNPY) caused a dose-dependent increase in food intake in goldfish, and intracerebroventricular administration of NPY Y1-receptor antagonist BIBP-3226 decreased food intake; the actions of gNPY were blocked by simultaneous injection of BIBP-3226. Goldfish maintained on a daily scheduled feeding regimen display an increase in NPY mRNA levels in the telencephalon-preoptic area and hypothalamus shortly before feeding; however, a decrease occured in optic tectum-thalamus. In both fed and unfed fish, brain NPY mRNA levels decreased after scheduled feeding. Restriction in daily food ration intake for 1 wk or food deprivation for 72 h resulted in increased brain NPY mRNA levels. Results from these studies demonstrate that NPY is a physiological brain signal involved in feeding behavior in goldfish, mediating its effects, at least in part, through Y1-like receptors in the brain.

scholarly journals A potent Neuropeptide Y (NPY) receptor antagonist 1229U91 suppresses spontaneous food intake in Zucker fatty rats

1997 ◽  
Vol 73 ◽  
pp. 180
Author(s):  
A. Ishihara ◽  
A. Kanatani ◽  
S. Asahi ◽  
T. Tanaka ◽  
M. Hidaka ◽  
...  
Keyword(s):  
Food Intake ◽  
Neuropeptide Y ◽  
Receptor Antagonist ◽  
Npy Receptor

Structure-affinity studies of C-terminally modified analogs of neuropeptide Y led to a novel class of peptidic Y1 receptor antagonist

1996 ◽  
Vol 65 (1) ◽  
pp. 61-70 ◽  
Author(s):  
Susanne Hoffmann ◽  
Beate Rist ◽  
Georgi Videnov ◽  
Günther Jung ◽  
Annette G. Beck-Sickinger
Keyword(s):  
Neuropeptide Y ◽  
Receptor Antagonist ◽  
Y1 Receptor
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