The measurement of free nitrendipine in human serum by an equilibrium dialysis - radioreceptor assay

Howard R. Lee; William R. Roeske; Henry I. Yamamura

doi:10.1016/0024-3205(83)90690-2

The measurement of free nitrendipine in human serum by an equilibrium dialysis - radioreceptor assay

Howard R. Lee, William R. Roeske, Henry I. Yamamura

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

12 Scopus citations

Abstract

A radioreceptor assay using [³H]nitrendipine and rat cerebral cortical membranes, in conjunction with equilibrium dialysis, measures the unbound (free) level of nitrendipine in human sera. The sensitivity of the assay is 0.1-0.2 picomoles/ml and is linear from 4 × 10^-11 to 4 × 10^-9 M nitrendipine. Other dihydropyridine calcium channel antagonists may be measured using this assay if these compounds are used to generate the standard curve. Blank serum interferes with specific [³H]nitrendipine binding (24 percent inhibition per 20 μ1 serum) whereas serum dialysates do not. Total serum nitrendipine levels may be measured, but the sensitivity of the assay is decreased due to interference by serum. Nitrendipine is highly protein bound in serum (93 - 99 percent). This protein binding is essentially unchanged over a serum concentration from 1 to 100 ng/ml. This assay is suitable for pharmacokinetic and pharmacodynamic studies.

Original language	English (US)
Pages (from-to)	1821-1829
Number of pages	9
Journal	Life Sciences
Volume	33
Issue number	18
DOIs	https://doi.org/10.1016/0024-3205(83)90690-2
State	Published - Oct 31 1983

ASJC Scopus subject areas

General Pharmacology, Toxicology and Pharmaceutics
General Biochemistry, Genetics and Molecular Biology

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10.1016/0024-3205(83)90690-2

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title = "The measurement of free nitrendipine in human serum by an equilibrium dialysis - radioreceptor assay",

abstract = "A radioreceptor assay using [3H]nitrendipine and rat cerebral cortical membranes, in conjunction with equilibrium dialysis, measures the unbound (free) level of nitrendipine in human sera. The sensitivity of the assay is 0.1-0.2 picomoles/ml and is linear from 4 × 10-11 to 4 × 10-9 M nitrendipine. Other dihydropyridine calcium channel antagonists may be measured using this assay if these compounds are used to generate the standard curve. Blank serum interferes with specific [3H]nitrendipine binding (24 percent inhibition per 20 μ1 serum) whereas serum dialysates do not. Total serum nitrendipine levels may be measured, but the sensitivity of the assay is decreased due to interference by serum. Nitrendipine is highly protein bound in serum (93 - 99 percent). This protein binding is essentially unchanged over a serum concentration from 1 to 100 ng/ml. This assay is suitable for pharmacokinetic and pharmacodynamic studies.",

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T1 - The measurement of free nitrendipine in human serum by an equilibrium dialysis - radioreceptor assay

AU - Lee, Howard R.

AU - Roeske, William R.

AU - Yamamura, Henry I.

PY - 1983/10/31

Y1 - 1983/10/31

N2 - A radioreceptor assay using [3H]nitrendipine and rat cerebral cortical membranes, in conjunction with equilibrium dialysis, measures the unbound (free) level of nitrendipine in human sera. The sensitivity of the assay is 0.1-0.2 picomoles/ml and is linear from 4 × 10-11 to 4 × 10-9 M nitrendipine. Other dihydropyridine calcium channel antagonists may be measured using this assay if these compounds are used to generate the standard curve. Blank serum interferes with specific [3H]nitrendipine binding (24 percent inhibition per 20 μ1 serum) whereas serum dialysates do not. Total serum nitrendipine levels may be measured, but the sensitivity of the assay is decreased due to interference by serum. Nitrendipine is highly protein bound in serum (93 - 99 percent). This protein binding is essentially unchanged over a serum concentration from 1 to 100 ng/ml. This assay is suitable for pharmacokinetic and pharmacodynamic studies.

AB - A radioreceptor assay using [3H]nitrendipine and rat cerebral cortical membranes, in conjunction with equilibrium dialysis, measures the unbound (free) level of nitrendipine in human sera. The sensitivity of the assay is 0.1-0.2 picomoles/ml and is linear from 4 × 10-11 to 4 × 10-9 M nitrendipine. Other dihydropyridine calcium channel antagonists may be measured using this assay if these compounds are used to generate the standard curve. Blank serum interferes with specific [3H]nitrendipine binding (24 percent inhibition per 20 μ1 serum) whereas serum dialysates do not. Total serum nitrendipine levels may be measured, but the sensitivity of the assay is decreased due to interference by serum. Nitrendipine is highly protein bound in serum (93 - 99 percent). This protein binding is essentially unchanged over a serum concentration from 1 to 100 ng/ml. This assay is suitable for pharmacokinetic and pharmacodynamic studies.

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The measurement of free nitrendipine in human serum by an equilibrium dialysis - radioreceptor assay

Abstract

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