Identification of Arginine Analogues as Antagonists and Agonists for the Melanocortin-4 Receptor
نویسندگان
چکیده
منابع مشابه
Melanocortin-4 receptor agonists for the treatment of obesity.
The identification of a highly efficacious anti-obesity agent remains an illusive goal. While many avenues of investigation have been pursued, none of the existing compounds claim much more than a 10% reduction in weight in humans (over a one year period with diet and exercise). Nonetheless, the potential reward for fulfilling this unmet medical need has kept interest levels high in the researc...
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The effects of caerulin, a CCK receptor agonist, and proglumide, a receptor antagonist, on hyperalgesia induced by sciatic nerve ligation, was studied in mice. Tolerance to the morphine response was obtained 3,7, 14,21 and 28 days after unilateral sciatic nerve ligation. Maximum hyperalgesia was found 14 days after nerve ligation. Caerulin increased morphine antinociception in nerve-ligated ani...
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Evidence from animal studies suggests corticotrophin and melanocortin systems have regulatory role in feeding system in avian, but there is no evidence for their interaction. In this survey three experiments designed to investigate the role of corticotrophin receptors on food intake using melanocortin receptors agonist M3 and M4 in neonatal chicken (each experiment includes 4 groups and 11 bird...
متن کاملAntibodies against the melanocortin-4 receptor act as inverse agonists in vitro and in vivo.
Functionally active antibodies (Abs) against central G-protein-coupled receptors have not yet been reported. We selected the hypothalamic melanocortin-4 receptor (MC4-R) as a target because of its crucial role in the regulation of energy homeostasis. A 15 amino acid sequence of the N-terminal (NT) domain was used as an antigen. This peptide showed functional activity in surface plasmon resonanc...
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ژورنال
عنوان ژورنال: Chemical and Pharmaceutical Bulletin
سال: 2007
ISSN: 0009-2363,1347-5223
DOI: 10.1248/cpb.55.1232