What question did this study set out to answer?

To establish whether neutral amino acids share a single competitive transport site across the blood-brain barrier and to formulate a predictive model of brain amino acid influx.

January 1, 1977Journal of Neurochemistry

Kinetics of Competitive Inhibition of Neutral Amino Acid Transport Across the Blood‐brain Barrier

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Authors

WPWilliam M. PardridgeBoston University

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Implication

Pharmacokinetic study demonstrates competitive inhibition of neutral amino acid transport across the blood-brain barrier in rats, indicating plasma levels govern brain influx.

Key Points

To establish whether neutral amino acids share a single competitive transport site across the blood-brain barrier and to formulate a predictive model of brain amino acid influx.
Measured the inhibition of [14C]tryptophan transport across the blood-brain barrier by phenylalanine, leucine, methionine, valine, and alpha-methyl tyrosine in barbiturate-anesthetized rats.
Used a single-injection tissue-sampling method to measure uptake saturation and derive Ki and Km values.
Formulated competitive inhibition transport equations to calculate apparent Km values from known plasma amino acid concentrations.
Inhibition constants (Ki) determined from cross-inhibition matched Michaelis constants (Km) from auto-inhibition, confirming all tested neutral amino acids compete for a single transport carrier.
Calculated apparent Km values enable accurate qualitative and mathematical prediction of in vivo brain influx rates based directly on circulating plasma amino acid concentrations.

Cite This Study

William M. Pardridge (1977) studied this question.

synapsesocial.com/papers/6a6e1df731a3df8243273ae3 https://doi.org/10.1111/j.1471-4159.1977.tb07714.x

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Implication

Pharmacokinetic study demonstrates competitive inhibition of neutral amino acid transport across the blood-brain barrier in rats, indicating plasma levels govern brain influx.

Kinetics of Competitive Inhibition of Neutral Amino Acid Transport Across the Blood‐brain Barrier

Discussion

Member takes

Implication

Key Points

Cite This Study

Kinetics of Competitive Inhibition of Neutral Amino Acid Transport Across the Blood‐brain Barrier

Discussion

Member takes

Implication

Key Points

Cite This Study

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