1,4-dihydropyridine derivatives and 1,4-dihydroquinoline derivat

Details 1,4-dihydropyridine derivatives and 1,4-dihydroquinoline derivat 1,4-dihydropyridine derivatives and 1,4-dihydroquinoline derivat

1984-11-19

1988-11-15

Marantz, Sidney

Chemistry: analytical and immunological testing

Biospecific ligand binding assay

Utilizing isolate of tissue or organ as binding agent

436804, 546174, 546278, 546283, 546284, 546321, C07D21355, C07D21516, C07D40312, G01N 33534

Patent

active

047849584

ABSTRACT:
A simple method for preparing highly radioactive 1,4-dihydropyridine and 1,4-dihydroquinoline derivatives labelled with .sup.125 I enables a specific radioactivity of approx. 2200 to 8800 Ci/m Mole to be achieved. In this way high sensitivity in medicament screening with the aid of radioreceptor assays and in determining plasma levels of 1,4-dihydropyridines, 1,4-dihydroquinolines and other substances that inter-react with receptors for 1,4-dihydropyridines and 1,4-dihydroquinolines is achieved, with the result that a substantially shorter exposure time in the auto-radiographic identification of the receptors for these substances is required. For this purpose an amino derivative of a 1,4-dihydropyridine or 1,4-dihydroquinoline is reacted with an acylating reagent radiactively labelled with .sup.125 I (2200-4400 Ci/mMole), and the .sup.125 I-substituted 1,4-dihydropyridine or 1,4-dihydroquinoline derivative possessing the specific radioactivity of the acylating reagent is isolated by conventional known separation methods.

REFERENCES:
Journal Lab. Clin. Med., 89, pp. 902 to 909 (1977), (Chem. Abs. 86, 185436P (1977).
J. E. T. Corrie et al., Meth. Enzymol, 73 Part B, 79-112, 1981.
R. Quirion, Neurosci. Lett., 36, 267-271, 1983.
FEMS, Microbiological Letter 10, pp. 107-109 (1981), (Chem. Abstracts 94, 170508e (1981).
Journal Immunoassay 4, pp. 83-98 (1983) (Chem. Abstracts 98, 172409e (1983).
Chemical Abstracts, vol. 84, No. 15, Jun. 24th, 1976, p. 17, reference No. 173596m.

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