Biological Activity
Pomaglumetad methionil hydrochloride (LY2140023 hydrochloride) is an orally active, methionine prodrug of the selective mGlu2/3 receptor agonist LY404039. Pomaglumetad methionil hydrochloride has the potential for schizophrenia research[1][2].
Pomaglumetad methionil (LY2140023) is a high-affinity peptide transporter 1 (PEPT1) substrate with a Km value of ~30 μM[2].LY2140023 is active against [14C]Gly-Sar with an IC50 value of 0.018 mM[2].
Pomaglumetad methionil (LY2140023; orally; 3-300 mg/kg; once daily for 7 days) dose-dependent increases the levels of the dopamine metabolites dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA) [1].
References
[1]. Lowe S, et al. Effects of a novel mGlu?/? receptor agonist prodrug, LY2140023 monohydrate, on central monoamine turnover as determined in human and rat cerebrospinal fluid. Psychopharmacology (Berl). 2012 Feb;219(4):959-70. [2]. Y Anne Pak, et al. In Vitro and Clinical Evaluations of the Drug-Drug Interaction Potential of a Metabotropic Glutamate 2/3 Receptor Agonist Prodrug with Intestinal Peptide Transporter 1. Drug Metab Dispos. 2017 Feb;45(2):137-144.
