Synthesis and Evaluation of New Arylsulfonamidomethylcyclohexyl Derivatives as Human Neuropeptide Y Y5 Receptor Antagonists for the Treatment of Obesity.

ChemInform ◽  
2004 ◽  
Vol 35 (30) ◽  
Author(s):  
Antonio Moreno ◽  
Silvia Perez ◽  
Silvia Galiano ◽  
Laura Juanenea ◽  
Oihana Erviti ◽  
...  
Keyword(s):  
Neuropeptide Y ◽  
Receptor Antagonists ◽  
Treatment Of Obesity

Synthesis and evaluation of new hydrazide derivatives as neuropeptide Y Y5 receptor antagonists for the treatment of obesity

2004 ◽  
Vol 12 (17) ◽  
pp. 4717-4723 ◽  
Author(s):  
Laura Juanenea ◽  
Silvia Galiano ◽  
Oihana Erviti ◽  
Antonio Moreno ◽  
Silvia Pérez ◽  
...  
Keyword(s):  
Neuropeptide Y ◽  
Receptor Antagonists ◽  
Treatment Of Obesity

Synthesis and evaluation of new arylsulfonamidomethylcyclohexyl derivatives as human neuropeptide Y Y5 receptor antagonists for the treatment of obesity

2004 ◽  
Vol 39 (1) ◽  
pp. 49-58 ◽  
Author(s):  
Antonio Moreno ◽  
Silvia Pérez ◽  
Silvia Galiano ◽  
Laura Juanenea ◽  
Oihana Erviti ◽  
...  
Keyword(s):  
Neuropeptide Y ◽  
Receptor Antagonists ◽  
Treatment Of Obesity

Novel Human Neuropeptide Y Y5 Receptor Antagonists for the Treatment of Obesity

2011 ◽  
Vol 55 (02) ◽  
pp. 81-85
Author(s):  
Silvia Galiano ◽  
Oihana Erviti ◽  
Silvia Pérez ◽  
Antonio Moreno ◽  
Laura Juanenea ◽  
...  
Keyword(s):  
Neuropeptide Y ◽  
Receptor Antagonists ◽  
Treatment Of Obesity

Design, synthesis and evaluation of a novel cyclohexanamine class of neuropeptide Y Y1 receptor antagonists

2009 ◽  
Vol 19 (16) ◽  
pp. 4781-4785 ◽  
Author(s):  
Kaimei Cho ◽  
Makoto Ando ◽  
Kensuke Kobayashi ◽  
Hiroshi Miyazoe ◽  
Toshiaki Tsujino ◽  
...  
Keyword(s):  
Neuropeptide Y ◽  
Receptor Antagonists ◽  
Design Synthesis ◽  
Y1 Receptor

Discovery of neuropeptide Y receptor antagonists

1997 ◽  
pp. 191-201 ◽  
Author(s):  
Alexandr Rabinovich ◽  
Anatoly Mazurov ◽  
Galina Krokhina ◽  
Anthony Ling ◽  
Nurit Livnah ◽  
...  
Keyword(s):  
Neuropeptide Y ◽  
Receptor Antagonists ◽  
Neuropeptide Y Receptor

scholarly journals Neuropeptide Y in normal eating and in genetic and dietary-induced obesity

2006 ◽  
Vol 361 (1471) ◽  
pp. 1159-1185 ◽  
Author(s):  
B Beck
Keyword(s):  
Neuropeptide Y ◽  
Diet Composition ◽  
High Energy ◽  
Glucose Sensing ◽  
Feeding Regulation ◽  
Treatment Of Obesity ◽  
The Brain ◽  
Diet Type

Neuropeptide Y (NPY) is one the most potent orexigenic peptides found in the brain. It stimulates food intake with a preferential effect on carbohydrate intake. It decreases latency to eat, increases motivation to eat and delays satiety by augmenting meal size. The effects on feeding are mediated through at least two receptors, the Y1 and Y5 receptors. The NPY system for feeding regulation is mostly located in the hypothalamus. It is formed of the arcuate nucleus (ARC), where the peptide is synthesized, and the paraventricular (PVN), dorsomedial (DMN) and ventromedial (VMN) nuclei and perifornical area where it is active. This activity is modulated by the hindbrain and limbic structures. It is dependent on energy availability, e.g. upregulation with food deprivation or restriction, and return to baseline with refeeding. It is also sensitive to diet composition with variable effects of carbohydrates and fats. Leptin signalling and glucose sensing which are directly linked to diet type are the most important factors involved in its regulation. Absence of leptin signalling in obesity models due to gene mutation either at the receptor level, as in the Zucker rat, the Koletsky rat or the db / db mouse, or at the peptide level, as in ob / ob mouse, is associated with increased mRNA abundance, peptide content and/or release in the ARC or PVN. Other genetic obesity models, such as the Otsuka–Long–Evans–Tokushima Fatty rat, the agouti mouse or the tubby mouse, are characterized by a diminution in NPY expression in the ARC nucleus and by a significant increase in the DMN. Further studies are necessary to determine the exact role of NPY in these latter models. Long-term exposure to high-fat or high-energy palatable diets leads to the development of adiposity and is associated with a decrease in hypothalamic NPY content or expression, consistent with the existence of a counter-regulatory mechanism to diminish energy intake and limit obesity development. On the other hand, an overactive NPY system (increased mRNA expression in the ARC associated with an upregulation of the receptors) is characteristic of rats or rodent strains sensitive to dietary-induced obesity. Finally, NPY appears to play an important role in body weight and feeding regulation, and while it does not constitute the only target for drug treatment of obesity, it may nevertheless provide a useful target in conjunction with others.

Discovery and SAR of Potent, Orally Available and Brain-Penetrable 5,6-Dihydro-4H-3-thia-1-aza-benzo[e]azulen- and 4,5-Dihydro-6-oxa-3-thia-1-aza-benzo[e]azulen Derivatives as Neuropeptide Y Y5 Receptor Antagonists.

ChemInform ◽  
2004 ◽  
Vol 35 (37) ◽  
Author(s):  
Heinrich Rueeger ◽  
Marc Gerspacher ◽  
Peter Buehlmayer ◽  
Pascal Rigollier ◽  
Yasuchika Yamaguchi ◽  
...  
Keyword(s):  
Neuropeptide Y ◽  
Receptor Antagonists
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