Metabolism of LY654322, a Growth Hormone Secretagogue, to an Unusual Diimidazopyridine Metabolite

• Published in: Drug metabolism and disposition Vol. 39; no. 5; pp. 740 - 749
• Main Authors: BOREL, Anthony G, JONES, Timothy M, BARBUCH, Robert J, JACKSON, David A, KULANTHAIVEL, Palaniappan, MATTIUZ, Edward, KLIMKOWSKI, Valentine J, WHEELER, William J, RENER, Gregory A
• Format: Journal Article
• Language: English
• Published: Bethesda, MD American Society for Pharmacology and Experimental Therapeutics 01.05.2011
• Subjects: Animals; Biological and medical sciences; Dipeptides - blood; Dipeptides - chemistry; Dipeptides - metabolism; Dipeptides - pharmacokinetics; Dipeptides - pharmacology; Dogs; Female; Heterocyclic Compounds, 3-Ring - analysis; Heterocyclic Compounds, 3-Ring - chemistry; Human Growth Hormone - metabolism; Imidazoles - blood; Imidazoles - chemistry; Imidazoles - metabolism; Imidazoles - pharmacokinetics; Imidazoles - pharmacology; Male; Medical sciences; Pharmacology. Drug treatments; Pyridines - analysis; Pyridines - chemistry; Rats; Rats, Inbred F344; Receptors, Ghrelin - agonists; Receptors, Ghrelin - metabolism; Somatotropin; Somatropin; Adenohypophyseal hormone; Metabolite; Neurohypophyseal hormone; Exploration; Pharmacokinetics; Metabolism; Quantitative analysis

2-Methylalanyl-N-{1-[(1R)-1-(4-fluorophenyl)-1-methyl-2-oxo-2-pyrrolidin-1-ylethyl]-1H-imidazol-4-yl}-5-phenyl-D-norvalinamide (LY654322) was rapidly cleared in rats and dogs by renal excretion of parent and metabolism (oxidative and hydrolytic). Among the metabolites identified in the urine of rats...