Glutamate Transporter Boosting Medications
Propentofylline increases the cast of countenance of both the GLT-1 and GLAST glutamate transporters lively representation in vitro, and significantly enhanced glutamate uptake in astrocytes. 1 2 Propentofylline vocal bioavailability is only 4%. Propentofylline moiety life of 15 – 45 minutes. Molecular power: 306.
Note that the study used vainglorious concentrations of propentofylline (100 microM), that would equate to very high human verbal dosages of 30 grams of propentofylline (alluring into account the low 4% bioavailability). Transdermal assiduity of propentofylline would be the in the highest degree idea, as this avoids the chief-pass metabolism, but the very capital dosage of 30 grams probably makes propentofylline unusable by reason of practical purposes for enhancing glutamate uptake.
Riluzole (a deaden with narcotics for ALS) at a dose of 160 mg elevates GLT-1 glutamate transporter form of words and activity. 1 2 Riluzole bioavailability is 60%. Riluzole half-life is 12 hours. Molecular import: 234. Riluzole costs around $1.50 with regard to a 50 mg tablet.
Ceftriaxone (Rocephin) ~y antibiotic that increases GLT-1 glutamate transporter term and activity by a factor of 3, what one. is a huge increase.1 2 3 4 5 Ceftriaxone half life is around 7 hours. Molecular consequence: 555. A single 500 mg ceftriaxone clyster costs around $14.
Citicoline (a cognitive enhancing addition ) at a dose of 2000 mg increases glutamate uptake and increases the utterance of the GLT-1 glutamate transporter in cultured rat astrocytes. 1 Citicoline bioavailability is potentially 100%. Citicoline half life is 3.5 hours. Molecular efficacy: 489.
Valproic acid at a dose of 8 grams increased the statement of glutamate transporter GLT-1 back stroke. 1
Alpha lipoic acid at prescribed portion of around 270 mg to 1370 mg increases glutamate uptake ~ means of 20%. 1 Alpha lipoic acid bioavailability is surrounding 30%. Half life is around 30 minutes. Molecular ponderousness: 206.
Pyroglutamate stimulates glutamate transporter etc.. 1 2 Pyroglutamic acid is useful as a supplement. Arginine pyroglutamate is in addition available as a supplement.
Morphine retirement increases glutamate uptake, and increases the modulation of the glutamate transporter GLT-1 in the hippocampus. 1
Glutamate Transporter Nomenclature
Glutamate transporter (GLT-1) is likewise called the excitatory amino acid transporter 2 (EAAT2). Glutamate aspartate transporter (GLAST) is besides called the excitatory amino acid transporter 1 (EAAT1). GLT-1 plays the prevalent role in regulating extracellular glutamate; it is responsible for clearing 90% of the glutamate from the brain.
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