Glutamate Transporter Boosting Medications
Propentofylline increases the term of both the GLT-1 and GLAST glutamate transporters effective exhibition in vitro, and significantly enhanced glutamate uptake in astrocytes. 1 2 Propentofylline verbal bioavailability is only 4%. Propentofylline half life of 15 – 45 minutes. Molecular ponderousness: 306.
Note that the study used profoundly concentrations of propentofylline (100 microM), what one. would equate to very high human nuncupative dosages of 30 grams of propentofylline (infectious into account the low 4% bioavailability). Transdermal reference to practice of propentofylline would be the most profitably idea, as this avoids the highest-pass metabolism, but the very elevated dosage of 30 grams probably makes propentofylline unusable in spite of practical purposes for enhancing glutamate uptake.
Riluzole (a drug for ALS) at a dose of 160 mg elevates GLT-1 glutamate transporter cast of countenance and activity. 1 2 Riluzole bioavailability is 60%. Riluzole moiety-life is 12 hours. Molecular gravity: 234. Riluzole costs around $1.50 beneficial to a 50 mg tablet.
Ceftriaxone (Rocephin) one antibiotic that increases GLT-1 glutamate transporter statement and activity by a factor of 3, which is a huge increase.1 2 3 4 5 Ceftriaxone half life is around 7 hours. Molecular influence: 555. A single 500 mg ceftriaxone lavement costs around $14.
Citicoline (a cognitive enhancing correlative) at a dose of 2000 mg increases glutamate uptake and increases the effective exhibition of the GLT-1 glutamate transporter in cultured rat astrocytes. 1 Citicoline bioavailability is in effect 100%. Citicoline half life is 3.5 hours. Molecular import: 489.
Valproic acid at a disagreeable lot of 8 grams increased the declaration of glutamate transporter GLT-1 later stroke. 1
Alpha lipoic acid at prescribed portion of around 270 mg to 1370 mg increases glutamate uptake ~ the agency of 20%. 1 Alpha lipoic acid bioavailability is on every side 30%. Half life is around 30 minutes. Molecular measure: 206.
Pyroglutamate stimulates glutamate transporter alertness. 1 2 Pyroglutamic acid is suitable as a supplement. Arginine pyroglutamate is furthermore available as a supplement.
Morphine leave increases glutamate uptake, and increases the squeezing out of the glutamate transporter GLT-1 in the hippocampus. 1 (This puissance potentially explain why some ME/CFS patients actual presentation major improvements in their symptoms the in the days subsequent to taking opioid pain killers, but not during the opioid treatment. See this staple for more info of this interesting opioid effect).
Low-dose naltrexone may enlarge astrocyte glutamate transport. 1
Reactive oxygen collection hydrogen peroxide and peroxynitrite impair glutamate convey into astrocytes. 1
Glutamate Transporter Nomenclature
Glutamate transporter (GLT-1) is moreover called the excitatory amino acid transporter 2 (EAAT2). Glutamate aspartate transporter (GLAST) is furthermore called the excitatory amino acid transporter 1 (EAAT1). GLT-1 plays the predominant role in regulating extracellular glutamate; it is amenable for clearing 90% of the glutamate from the brain.
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