Journal of medicinal chemistry, 2003-02, Vol.46 (5), p.670-673
2003
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Details
- Autor(en) / Beteiligte
- Titel
- In vitro and in vivo characterization of 3-[2-[6-(2-tert-butoxyethoxy)pyridin-3-yl]-1H-imidazol-4-yl]benzonitrile hydrochloride salt, a potent and selective NPY5 receptor antagonist
- Ist Teil von
- Journal of medicinal chemistry, 2003-02, Vol.46 (5), p.670-673
- Ort / Verlag
- United States
- Erscheinungsjahr
- 2003
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- To investigate the anorectic potential of NPY5 receptor antagonists, we have profiled the in vitro and in vivo properties of 3-[2-[6-(2-tert-butoxyethoxy)pyridin-3-yl]-1H-imidazol-4-yl]benzonitrile hydrochloride salt (1). This compound was found to have excellent NPY5 receptor affinity and selectivity, potent functional antagonism, and good peripheral and central nervous system exposure in rats. This compound attenuated bovine pancreatic polypeptide induced food intake in rats but failed to demonstrate anorectic activity in rodent natural feeding models.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0022-2623eISSN: 1520-4804DOI: 10.1021/jm025584pTitel-ID: cdi_proquest_miscellaneous_73037630
- Format
- –
- Schlagworte
- Animals, Brain - metabolism, Calcium - metabolism, Cattle, Cerebrospinal Fluid - metabolism, Eating - drug effects, Humans, Imidazoles - chemical synthesis, Imidazoles - pharmacokinetics, Imidazoles - pharmacology, In Vitro Techniques, Male, Nitriles - chemical synthesis, Nitriles - pharmacokinetics, Nitriles - pharmacology, Pancreatic Polypeptide - pharmacology, Rats, Rats, Sprague-Dawley, Rats, Wistar, Receptors, Neuropeptide Y - antagonists & inhibitors, Receptors, Neuropeptide Y - metabolism, Tissue Distribution, Tumor Cells, Cultured