Monocarboxylate blood-brain barrier

Ackley, D. C. and R. A. Yokel. Aluminum dtrate is transported from brain into blood via the monocarboxylic acid transporter located at the blood-brain barrier. Toxicology 1997, 120, 89-97. 

Endothelial cells of the blood-brain barrier and brain cells have specific transporters for the uptake of glucose and monocarboxylic acids 533... 

Pellerin, L, and Pierre, K, (2005) Monocarboxylate transporters and their dual role in efflux and influx across the blood-brain barrier and beyond, in Effiux Transporters and the Blood-Brain Barrier (ed. F.M. Taylor), Nova Science Publishers, Inc., New York. 

Kang, Y,S Terasaki, T and Tsuji, A. (1990) Acidic dmg transport in vivo through die blood-brain barrier a role of the fansport carrier for monocarboxylic acids. Journal of Pharmaeobio-Dynamics, 13, 158-163,... 

Kido, Y., Tamai, 1.. Okamoto, M, Suzuki, F.. and Tsuji, A, (2000) Functional clarification of MCTl-mediated transport of monocarboxylic add at die blood—brain barrier using in vitro cultured cells and in vivo BUI studies. Pharmaceutical Research, 17. 55-62,... 

The mean oral bioavailability of finasteride is 65%, as shown in Table 45.4, and is not affected by food (99). Approximately 90% of circulating finasteride is bound to plasma proteins. Finasteride has been found to cross the blood-brain barrier, but levels in semen were undetectable (<0.2 ng/mL). Finasteride is extensively metabolized in the liver, primarily via CYP3A4 to two major metabolites monohydroxylation of the t-butyl side chain, which is further metabolized via an aldehyde intermediate to the second metabolite, a monocarboxylic acid (Fig. 45.15). The metabolites show approximately 20% the inhibition of finasteride for 5a-reductase. The mean terminal half-life is approximately 5 to 6 hours in men between 18 and 60 years of age and 8 hours in men older than 70 years of age. Following an oral dose of finasteride, approximately 40% of the dose was excreted in the urine as metabolites and approximately 57% in the feces. Even though the elimination rate of finasteride is decreased in the elderly, no dosage adjustment is necessary. No dosage adjustment is necessary in patients with renal insufficiency. A decrease in the urinary excretion of metabolites was observed in patients with renal impairment, but this was compensated for by... 

The following substrates were used to assess blood-brain barrier transport systems L-lysine and L-histidine (basic and neutral amino acid systems, respectively), adenine (purine base), thiamine (vitamin), choline (amine), pyruvate (monocarboxylic acid) and 3-hydroxybutyrate (ketone body). Tracer levels of the C-labelled substrates (Amersham International pic) were added to the perfusate at 0.3-1.2 /iCi/ml together with pH]inulin at l.OjUCi/ml as intravascular marker. Following a net perfusion time of 18.5 s, the animal was decapitated. The brain was rapidly removed, sliced into 2 mm coronal sections and quick-frozen on solid CO2. Each slice was dissected on a freezing... 

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