mk-0557 and Disease-Models--Animal

mk-0557 has been researched along with Disease-Models--Animal* in 1 studies

Other Studies

1 other study(ies) available for mk-0557 and Disease-Models--Animal

Article	Year
Discovery and evaluation of spirocyclic derivatives as antagonists of the neuropeptide Y5 receptor. Bioorganic & medicinal chemistry letters, 2012, Apr-15, Volume: 22, Issue:8 A novel series of spirocyclic derivatives was synthesized and evaluated as NPY Y5R antagonists for the treatment of obesity. Cis and trans analogs 7a and 8a were equipotent in a Y5R binding assay (K(i)'s ≤ 1 nM) and displayed good stability in human and rat liver microsome preparations. Compound 7a failed to demonstrate weight loss activity in a diet-induced obese (DIO) rat model at unbound drug levels in the brain that exceeded the Y5R K(i) value by 25-fold over a 24-h time-period. Topics: Animals; Anti-Obesity Agents; Cyclohexanes; Disease Models, Animal; Drug Discovery; Drug Stability; Humans; Microsomes, Liver; Molecular Structure; Protein Binding; Pyrazoles; Rats; Receptors, Neuropeptide Y; Spiro Compounds	2012

Article

Year

Discovery and evaluation of spirocyclic derivatives as antagonists of the neuropeptide Y5 receptor.

Bioorganic & medicinal chemistry letters, 2012, Apr-15, Volume: 22, Issue:8

A novel series of spirocyclic derivatives was synthesized and evaluated as NPY Y5R antagonists for the treatment of obesity. Cis and trans analogs 7a and 8a were equipotent in a Y5R binding assay (K(i)'s ≤ 1 nM) and displayed good stability in human and rat liver microsome preparations. Compound 7a failed to demonstrate weight loss activity in a diet-induced obese (DIO) rat model at unbound drug levels in the brain that exceeded the Y5R K(i) value by 25-fold over a 24-h time-period.

Topics: Animals; Anti-Obesity Agents; Cyclohexanes; Disease Models, Animal; Drug Discovery; Drug Stability; Humans; Microsomes, Liver; Molecular Structure; Protein Binding; Pyrazoles; Rats; Receptors, Neuropeptide Y; Spiro Compounds

2012