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Radioreceptor and High‐Performance Liquid Chromatographic Assays for the Calcium Channel Antagonist Nitrendipine in Serum
Author(s) -
JANIS RONALD A.,
KROL GEORGE J.,
NOE ANSON J.,
PAN MARY
Publication year - 1983
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1002/j.1552-4604.1983.tb02734.x
Subject(s) - nitrendipine , high performance liquid chromatography , chromatography , chemistry , radioligand assay , pharmacokinetics , metabolite , quantitative analysis (chemistry) , active metabolite , pharmacology , calcium , in vitro , biochemistry , biology , organic chemistry
Radioreceptor and high‐performance liquid chromatographic (HPLC) assays for nitrendipine were developed and applied to the analysis of serum samples. The HPLC assay required both extraction and concentration of the serum samples, whereas the radioreceptor assay involved only direct dilution of the serum. The HPLC assay, in contrast to the radioreceptor assay, can be used for detection and quantitative analysis of biologically inactive metabolites. The radioreceptor assay is based on the competition between nitrendipine in serum and [ 3 H]nitrendipine for high‐affinity binding sites on cardiac membranes. Forty‐two serum samples were obtained from five volunteers, and the HPLC and radioreceptor assay results were compared. A correlation coefficient of 0.98 was found between the results of the two assays within the nitrendipine serum concentration range of 1 to 20 ng/ml. No significant levels of active metabolites or any other interferences were found. The radioreceptor assay provides a specific and sensitive alternative to HPLC; it is rapid and inexpensive and with minor modifications may be applicable to most presently available Ca 2+ channel antagonists.