Mildronate dihydrate

Description

Meldonium is a zwitterionic compound that was developed in Latvia in 1970 as an anti-ischemia drug. AS Grindeks, a Latvian pharmaceutical company, markets small quantities of it in Eastern Europe.
But meldonium is better known as a doping drug that athletes use to enhance performance. At the beginning of this year, the World Anti-Doping Agency added meldonium to its list of banned substances. Soon thereafter, tennis star Maria Sharapova became the first prominent athlete to have been affected by this ban.
After failing a drug test at the Australian Open, Sharapova announced that she had taken the drug for many years and was not aware of the ban. The International Tennis Federation suspended her for 2 years, but Sharapova appealed the ban. The Court of Arbitration for Sport will likely consider the appeal later this month.

Description

Mildronate is an inhibitor of biosynthesis of L-carnitine by gamma-butyrobetaine (GBB) hydroxylase and as a competitive inhibitor of renal carnitine reabsorption.Mildronate (40 μM) inhibits the reaction of γ-butyrobetaine hydroxylase with γ-butyrobetaine with Km and Vmax of 36.8 μM and 0.08 nmol/min/mg protein, respectively.

The Uses of Mildronate dihydrate

Meldonium dihydrate has been used as an anti-ischemic agent to evaluate its protective effects on Ischemia-reperfusion (I/R) in chick embryos.

Biochem/physiol Actions

Meldonium is an Inhibitor of γ-butyrobetaine hydroxylase (BBOX) a key enzyme in the synthesis of carnitine.