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Central control of feeding behavior by neuropeptide Y.
The effects of NPY on the regulation of food intake and energy expenditure is reviewed and the pharmacological and molecular evidence as to which NPY receptor(s) mediate this effect is discussed.
Pharmacological characterization and appetite suppressive properties of BMS-193885, a novel and selective neuropeptide Y(1) receptor antagonist.
Supporting evidence that BMS-193885 reduces food intake and body weight via inhibition of the central neuropeptide Y(1) receptor is provided, as well as testing the compound in a panel of 70 G-protein coupled receptors and ion channels, which shows good systemic bioavailability and brain penetration.
NPY‐Ergic agents for the treatment of obesity
This review summarizes the role of NPY in energy homeostasis, the reported evidence for the involvement of different receptors in NPY’s action, and the advancement of pharmacological tools for these receptors which might lead to useful treatments of human obesity.
Highly Reactive Magnesium for the Preparation of Grignard Reagents: 1‐Norbornanecarboxylic Acid
Highly reactive magnesium for the preparation of Grignard reagents: 1-norbornanecarboxylic acid intermediate: 2,2-dichloronorbornane intermediate: 1-chloronorbornane product:
Dihydropyridine neuropeptide Y Y1 receptor antagonists 2. bioisosteric urea replacements.
The cyanoguanidine moiety was identified as an effective urea replacement in a series of dihydropyridine NPY Y(1) receptor antagonists and demonstrated improved permeability properties in Caco-2 cells in comparison to urea 4a.
Dihydropyridine neuropeptide Y Y(1) receptor antagonists.
Structural-activity studies around certain portions of the dihydropyridine chemotype identified BMS-193885 (6e) as a potent and selective Y(1) receptor antagonist.
Synthesis and evaluation of 5,5-diphenylimidazolones as potent human neuropeptide Y5 receptor antagonists.
A series of novel 5,5-diphenylimidazolones was synthesized and evaluated for activity against the human neuropeptide Y5 receptor. The 3-pyridyl analog 46 demonstrated an IC(50) of 8.3 nM with a