| 词条 | Glufimet |
| 释义 |
| Verifiedfields = | Watchedfields = | verifiedrevid = | IUPAC_name = dimethyl 2-amino-3-phenylpentanedioate;hydrochloride | image = Glufimet.svg | width = 200px | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = | class = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = | CAS_number = 651321-95-8 | CAS_supplemental = | ATC_prefix = | ATC_suffix = | ATC_supplemental = | PubChem = 78064435 | IUPHAR_ligand = | DrugBank_Ref = | DrugBank = | ChemSpiderID_Ref = | ChemSpiderID = 9646572 | UNII = | KEGG = | ChEBI = | ChEMBL = | synonyms = RGPU-238; Dimethyl 3-phenylglutamic acid hydrochloride; Dimethyl 3-phenylglutamate hydrochloride; 1,5-Dimethyl (2S)-2-amino-3-phenylpentanedioate hydrochloride | C=13 | H=18 | Cl=1 | N=1 | O=4 | molecular_weight = 287.74 g/mol | SMILES = COC(=O)CC(C1=CC=CC=C1)C(C(=O)OC)N.Cl | StdInChI_Ref = | StdInChI = 1S/C13H17NO4.ClH/c1-17-11(15)8-10(12(14)13(16)18-2)9-6-4-3-5-7-9;/h3-7,10,12H,8,14H2,1-2H3;1H | StdInChIKey_Ref = | StdInChIKey = YYGZEJCVUMTAMY-UHFFFAOYSA-N }}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.[1][2][3][4] It has been suggested that metabotropic glutamate receptors may also play a role in the mechanism of action of glufimet.[4] Stress-protective effects have been described for glufimet in animals.[1][2][3] References1. ^1 2 {{cite journal | vauthors = Tyurenkov IN, Perfilova VN, Sadikova NV, Berestovitskaya VM, Vasil'eva OS | title = Effects of a New Glutamic Acid Derivative on Myocardial Contractility of Stressed Animals under Conditions of Nitric Oxide Synthesis Blockade | journal = Bull. Exp. Biol. Med. | volume = 159 | issue = 3 | pages = 384–6 | date = July 2015 | pmid = 26205724 | doi = 10.1007/s10517-015-2969-7 | url = }} {{GABA receptor modulators}}{{Glutamate receptor modulators}}{{Nitric oxide signaling modulators}}{{Nervous-system-drug-stub}}2. ^1 2 {{cite journal | vauthors = Perfilova VN, Popova TA, Prokofiev II, Mokrousov IS, Ostrovskii OV, Tyurenkov IN | title = 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 | journal = Bull. Exp. Biol. Med. | volume = 163 | issue = 2 | pages = 226–229 | date = June 2017 | pmid = 28726197 | doi = 10.1007/s10517-017-3772-4 | url = }} 3. ^1 2 {{cite journal | vauthors = Perfilova VN, Sadikova NV, Prokofiev II, Inozemtsev OV, Tyurenkov IN | title = [Cardioprotective effect of the new derivative of glutamic acid - glufimet in acute immobilization-painful stress in animals of different ages] | language = Russian | journal = Adv Gerontol | volume = 29 | issue = 1 | pages = 116–122 | date = 2016 | pmid = 28423256 | doi = 10.1134/S2079057016030073 | url = }} 4. ^1 2 {{cite journal | vauthors = Borisov AV, Prokofiev II, Mokrousov IS, Perfilova VN, Tyurenkov IN | title = Inhibition of the Expression of Inducible NO Synthase by Neuroactive Amino Acid Derivatives Phenibut and Glufimet In Vitro and Ex Vivo | journal = Bull. Exp. Biol. Med. | volume = 164 | issue = 2 | pages = 177–180 | date = December 2017 | pmid = 29181662 | doi = 10.1007/s10517-017-3952-2 | url = }} 7 : Amino acids|Dicarboxylic acids|Drugs with unknown mechanisms of action|Experimental drugs|GABA analogues|Glutamates|Russian drugs |
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