Glutamate Transporter Boosting Medications
Propentofylline increases the statement of both the GLT-1 and GLAST glutamate transporters squeezing out in vitro, and significantly enhanced glutamate uptake in astrocytes. 1 2 Propentofylline spoken bioavailability is only 4%. Propentofylline moiety life of 15 – 45 minutes. Molecular power: 306.
Note that the study used powerfully concentrations of propentofylline (100 microM), what one. would equate to very high human parole dosages of 30 grams of propentofylline (agitation into account the low 4% bioavailability). Transdermal petition of propentofylline would be the best idea, as this avoids the primary-pass metabolism, but the very dark dosage of 30 grams probably makes propentofylline unusable as antidote to practical purposes for enhancing glutamate uptake.
Riluzole (a physic for ALS) at a dose of 160 mg elevates GLT-1 glutamate transporter general tone and activity. 1 2 Riluzole bioavailability is 60%. Riluzole half-life is 12 hours. Molecular make heavy: 234. Riluzole costs around $1.50 as being a 50 mg tablet.
Ceftriaxone (Rocephin) ~y antibiotic that increases GLT-1 glutamate transporter suitable feeling and execution 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 significance: 555. A single 500 mg ceftriaxone injection costs around $14.
Citicoline (a cognitive enhancing add to) at a dose of 2000 mg increases glutamate uptake and increases the modulation of the GLT-1 glutamate transporter in cultured rat astrocytes. 1 Citicoline bioavailability is to all intents and purposes 100%. Citicoline half life is 3.5 hours. Molecular gravity: 489.
Valproic acid at a drench of 8 grams increased the utterance of glutamate transporter GLT-1 on the model of stroke. 1
Alpha lipoic acid at dose of around 270 mg to 1370 mg increases glutamate uptake ~ means of 20%. 1 Alpha lipoic acid bioavailability is in a circle 30%. Half life is around 30 minutes. Molecular gravity: 206.
Pyroglutamate stimulates glutamate transporter exercise. 1 2 Pyroglutamic acid is to be availed of as a supplement. Arginine pyroglutamate is besides 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 force potentially explain why some ME/CFS patients actual trial major improvements in their symptoms the in the days subsequent taking opioid pain killers, but not for the time of the opioid treatment. See this fibre for more info of this pleasing opioid effect).
Glutamate Transporter Nomenclature
Glutamate transporter (GLT-1) is moreover called the excitatory amino acid transporter 2 (EAAT2). Glutamate aspartate transporter (GLAST) is in addition called the excitatory amino acid transporter 1 (EAAT1). GLT-1 plays the prevailing role in regulating extracellular glutamate; it is amenable for clearing 90% of the glutamate from the brain.
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