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OwnerHartmut Glossmaninventor
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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.
A radioactively labelled 1,4-dihydropyridine derivative of the formula ##STR10## in which R.sup.1 and R.sup.2 are the same or different and R.sup.1 is a ##STR11## group, in which A and Y are a straight chain or branched alkyl group with 1-6 carbon atoms and R.sup.x is a phenyl radical substituted in the p-position, but not with halogen, or an imidazole radical attached to the 4-position, and if R.sup.1 is not the same as R.sup.2, then R.sup.2 denotes NO.sub.2, nitrile or alkoxy with 1-4 carbon atoms, R.sup.3 and R.sup.4 are the same or different and denote H, NH.sub.2 or straight-chain or branched alkyl radicals with 1-4 carbon atoms, R.sup.5 denotes an aryl radical which is unsubstituted or is substituted by 1 to 2 identical or different substituents from the group consisting of alkyl, alkoxy, phenyl, halogen, nitro, cyano, trifluoromethyl and alkylmercapto, and in which the radical R.sup.x is also singly or doubly substituted by .sup.125 I and has a specific activity of about 2200 to about 8800 Ci/mMole.
A radioactively labelled 1,4-dihydroquinoline derivative of the formula ##STR13## in which R.sup.1 and R.sup.2 are the same or different and R.sup.1 is a ##STR14## group, in which A and Y are a straight chain or branched alkyl group with 1-6 carbon atoms and R.sup.x is a phenyl radical substituted in the p-position, but not with halogen, or an imidazole radical attached to the 4-position, R.sup.3 is H, NH.sub.2 or straight-chain or branched alkyl radicals with 1-4 carbon atoms, R.sup.5 denotes an unsubstituted aryl radical or an aryl radical substituted by 1 or 2 identical or different substituents from the group consisting of alkyl, alkoxy, phenyl, halogen, nitro, cyano, trifluoromethyl and alkyl-mercapto, R.sup.6 denotes H, halogen, alkyl or alkoxy radical, and in which the radical R.sup.x is also singly or doubly substituted by .sup.125 I and has a specific activity of about 2200 to about 8800 Ci/mMole.
Dependencies are inferred from the claim text.