Glufimet Explained

Glufimet (developmental code name RGPU-238), also known as dimethyl 3-phenylglutamate hydrochloride, is a derivative of glutamic acid (glutamate) which was developed in Russia and is related to the γ-aminobutyric acid (GABA) derivative phenibut (3-phenyl-GABA).[1] [2] [3] [4] It contains phenibut and glycine fragments in its chemical structure, has been described, as a "GABA precursor", and is said to modulate the GABA and nitric oxide (NO) systems and to have antioxidant activity. It has been suggested that metabotropic glutamate receptors may also play a role in the mechanism of action of glufimet. Stress-protective effects have been described for glufimet in animals.

Notes and References

  1. Tyurenkov IN, Perfilova VN, Sadikova NV, Berestovitskaya VM, Vasil'eva OS . Effects of a New Glutamic Acid Derivative on Myocardial Contractility of Stressed Animals under Conditions of Nitric Oxide Synthesis Blockade . Bull. Exp. Biol. Med. . 159 . 3 . 384–6 . July 2015 . 26205724 . 10.1007/s10517-015-2969-7 . 666113 .
  2. Perfilova VN, Popova TA, Prokofiev II, Mokrousov IS, Ostrovskii OV, Tyurenkov IN . Effect of Phenibut and Glufimet, a Novel Glutamic Acid Derivative, on Respiration of Heart and Brain Mitochondria from Animals Exposed to Stress against the Background of Inducible NO-Synthase Blockade . Bull. Exp. Biol. Med. . 163 . 2 . 226–229 . June 2017 . 28726197 . 10.1007/s10517-017-3772-4 . 4907409 .
  3. Perfilova VN, Sadikova NV, Prokofiev II, Inozemtsev OV, Tyurenkov IN . [Cardioprotective effect of the new derivative of glutamic acid - glufimet in acute immobilization-painful stress in animals of different ages] . ru . Adv Gerontol . 29 . 1 . 116–122 . 2016 . 28423256 . 10.1134/S2079057016030073 . 78111848 .
  4. Borisov AV, Prokofiev II, Mokrousov IS, Perfilova VN, Tyurenkov IN . Inhibition of the Expression of Inducible NO Synthase by Neuroactive Amino Acid Derivatives Phenibut and Glufimet In Vitro and Ex Vivo . Bull. Exp. Biol. Med. . 164 . 2 . 177–180 . December 2017 . 29181662 . 10.1007/s10517-017-3952-2 . 90334012 .

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