In‐vitro Evidence for Carrier‐mediated Uptake of Acidic Drugs by Isolated Bovine Brain Capillaries

TETSUYA TERASAKI; YOUNG SOOK KANG; TOSHIMASA OHNISHI; AKIRA TSUJI

doi:10.1111/j.2042-7158.1991.tb06660.x

In‐vitro Evidence for Carrier‐mediated Uptake of Acidic Drugs by Isolated Bovine Brain Capillaries

TETSUYA TERASAKI, YOUNG SOOK KANG, TOSHIMASA OHNISHI, AKIRA TSUJI

Research output: Contribution to journal › Article › peer-review

20 Citations (Scopus)

Abstract

Abstract— [³H]Acetic acid was taken up into the isolated brain capillaries in a temperature and concentration dependent manner. The initial uptake rates were pH dependent over the range 5.0–7.4. An increase of the uptake rate with decrease in medium pH was not seen in the presence of unlabelled acetic acid (10 mM). The uptake of [³H]acetic acid was significantly reduced in the presence of several drugs having a monocarboxylic group. The initial uptake of [¹⁴C]salicylic acid was also pH dependent and was inhibited by acetic acid and acidic drugs. A mutually competitive inhibition was observed for the uptake of acetic acid and salicylic acid. The present study demonstrates that acidic drugs having a monocarboxylic group are transported by a common carrier‐mediated system into the brain capillaries. 1991 Royal Pharmaceutical Society of Great Britain

Original language	English
Pages (from-to)	172-176
Number of pages	5
Journal	Journal of Pharmacy and Pharmacology
Volume	43
Issue number	3
DOIs	https://doi.org/10.1111/j.2042-7158.1991.tb06660.x
Publication status	Published - 1991 Mar
Externally published	Yes

ASJC Scopus subject areas

Pharmacology
Pharmaceutical Science

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10.1111/j.2042-7158.1991.tb06660.x

Cite this

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title = "In‐vitro Evidence for Carrier‐mediated Uptake of Acidic Drugs by Isolated Bovine Brain Capillaries",

abstract = "Abstract— [3H]Acetic acid was taken up into the isolated brain capillaries in a temperature and concentration dependent manner. The initial uptake rates were pH dependent over the range 5.0–7.4. An increase of the uptake rate with decrease in medium pH was not seen in the presence of unlabelled acetic acid (10 mM). The uptake of [3H]acetic acid was significantly reduced in the presence of several drugs having a monocarboxylic group. The initial uptake of [14C]salicylic acid was also pH dependent and was inhibited by acetic acid and acidic drugs. A mutually competitive inhibition was observed for the uptake of acetic acid and salicylic acid. The present study demonstrates that acidic drugs having a monocarboxylic group are transported by a common carrier‐mediated system into the brain capillaries. 1991 Royal Pharmaceutical Society of Great Britain",

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AU - KANG, YOUNG SOOK

AU - OHNISHI, TOSHIMASA

AU - TSUJI, AKIRA

PY - 1991/3

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N2 - Abstract— [3H]Acetic acid was taken up into the isolated brain capillaries in a temperature and concentration dependent manner. The initial uptake rates were pH dependent over the range 5.0–7.4. An increase of the uptake rate with decrease in medium pH was not seen in the presence of unlabelled acetic acid (10 mM). The uptake of [3H]acetic acid was significantly reduced in the presence of several drugs having a monocarboxylic group. The initial uptake of [14C]salicylic acid was also pH dependent and was inhibited by acetic acid and acidic drugs. A mutually competitive inhibition was observed for the uptake of acetic acid and salicylic acid. The present study demonstrates that acidic drugs having a monocarboxylic group are transported by a common carrier‐mediated system into the brain capillaries. 1991 Royal Pharmaceutical Society of Great Britain

AB - Abstract— [3H]Acetic acid was taken up into the isolated brain capillaries in a temperature and concentration dependent manner. The initial uptake rates were pH dependent over the range 5.0–7.4. An increase of the uptake rate with decrease in medium pH was not seen in the presence of unlabelled acetic acid (10 mM). The uptake of [3H]acetic acid was significantly reduced in the presence of several drugs having a monocarboxylic group. The initial uptake of [14C]salicylic acid was also pH dependent and was inhibited by acetic acid and acidic drugs. A mutually competitive inhibition was observed for the uptake of acetic acid and salicylic acid. The present study demonstrates that acidic drugs having a monocarboxylic group are transported by a common carrier‐mediated system into the brain capillaries. 1991 Royal Pharmaceutical Society of Great Britain

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In‐vitro Evidence for Carrier‐mediated Uptake of Acidic Drugs by Isolated Bovine Brain Capillaries

Abstract

ASJC Scopus subject areas

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