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Abstract

SKF 525A displaces drugs from serum alpha 1-acid glycoprotein binding sites.

F M Belpaire, B Chindavijak and M G Bogaert
Journal of Pharmacology and Experimental Therapeutics February 1987, 240 (2) 628-630;
F M Belpaire
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B Chindavijak
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M G Bogaert
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Abstract

In vivo treatment of rats with beta-diethylaminoethyl-diphenylpropylacetate hydrochloride (SKF 525A), an inhibitor of hepatic monooxygenases, decreases the serum binding of oxprenolol and propranolol, which bind mainly to alpha 1-acid glycoprotein, but not that of phenytoin, which is bound to albumin. The effect was maximal 40 min after treatment and had disappeared after 6 hr, when enzyme inhibition was still present. A displacing effect was also observed when SKF 525A was added in vitro to serum of rats, dogs and humans and to human alpha 1-acid glycoprotein, whereas binding to human serum albumin was not affected. SKF 525A was found to be equipotent with tris(2-butoxyethyl)phosphate, a known displacer of binding of drugs from alpha 1-acid glycoprotein. When studying the pharmacokinetics or the effects of drugs after SKF 525A pretreatment, the possibility that altered protein binding may influence the findings should be considered.

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Journal of Pharmacology and Experimental Therapeutics
Vol. 240, Issue 2
1 Feb 1987
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Abstract

SKF 525A displaces drugs from serum alpha 1-acid glycoprotein binding sites.

F M Belpaire, B Chindavijak and M G Bogaert
Journal of Pharmacology and Experimental Therapeutics February 1, 1987, 240 (2) 628-630;

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Abstract

SKF 525A displaces drugs from serum alpha 1-acid glycoprotein binding sites.

F M Belpaire, B Chindavijak and M G Bogaert
Journal of Pharmacology and Experimental Therapeutics February 1, 1987, 240 (2) 628-630;
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