首页> 外国专利> New unlabelled and radioactive labelled derivatives of butylamino propiophenone, their preparation, immunogens obtained from the unlabelled derivatives and a process for immunogen preparation, antisera raised using the immunogens and a method for raising antisera, a radioimmunoassay method and a test kit for use in the assay method

New unlabelled and radioactive labelled derivatives of butylamino propiophenone, their preparation, immunogens obtained from the unlabelled derivatives and a process for immunogen preparation, antisera raised using the immunogens and a method for raising antisera, a radioimmunoassay method and a test kit for use in the assay method

机译:丁基氨基苯甲酮的新的未标记和放射性标记的衍生物,它们的制备,从未标记的衍生物获得的免疫原和免疫原的制备方法,使用该免疫原产生的抗血清和产生抗血清的方法,放射免疫测定法和用于该测定的测试试剂盒方法

摘要

New compounds are prepared having the formula:wherein (1) X, is Cl, R2 is oxygen andR1 is -(CH2)n-OHor -(CH2)n-O-(CO)m(CH2)PCOZor -O-(CH2)PCOZor -O-(CH2)pCOOR11or is a radioisotopeor (2) X1 is Cl, R' is Hand R' is = N . O(CH2)qCOZor (3) X, is a radioisotope, R2 is oxygen and R, is OH in the 4-position and wherein n is an integer of 1-5, m is 0 or 1, p is an integer of 1-4, q is an integer of 1-3, R11 is a C1-C3 alkyl group and Z is OH or a group of formula:where s in an integer of 1-4, R6 is a radioactive nuclide and R, is OH.;Various methods for their preparation are described. The unlabelled compounds in which R, and R, contains a free carboxy group can be coupled with an immunogenic carrier to give an immunogen which can be used to raise antisera in host animals e.g. rabbits. This antisera contains antibodies specific to the antidepressant bupropion. This antisera can be used, together with the radioactive labelled compounds I in a radioimmunoassay method for determining bupropion in biological fluids as bupropion and the labelled analogue thereof compete for binding sites in the antisera. A test kit for use in the radioimmunoassay contains antisera, radioactive labelled compound I and optionally bupropion.
机译:制备具有下式的新化合物: <图像文件=“ IMGA0001.GIF” he =“ 35” imgContent =“ chem” imgFormat =“ GIF” inline =“ no” wi =“ 80” /> ,其中(1)X是Cl,R 2 是氧, R 1 是-(CH 2 n -OH 或-(CH 2 n -O-(CO) m (CH 2 P COZ 或-O-(CH 2 P COZ 或- O-(CH 2 p COOR 11 ,或者是放射性同位素 < / ListItem> 或(2)X 1 是Cl,R'是手R'是= N。 O(CH 2 q COZ 或(3)X是放射性同位素,R 2 是氧, R 1是在4-位上的OH,其中n是1-5的整数,m是0或1,p是1-4的整数,q是1-3的整数,R Sub 11 < / Sub>是C 1 -C 3 烷基,Z是OH或下式的基团: <图像文件=“ IMGA0002.GIF” he =“ 21” imgContent =“ chem” imgFormat =“ GIF” inline =“ no” wi =“ 52” /> 其中s在1-4的整数中,R 6 是放射性核素,R是OH。 ;描述了各种制备方法。可以将其中R 1和R 2包含一个游离羧基的未标记化合物与一种免疫原性载体偶联,以产生一种免疫原,该免疫原可以用于提高宿主动物的抗血清,例如兔子。该抗血清含有抗抑郁药安非他酮特异的抗体。当安非他酮与安非他酮及其标记的类似物竞争抗血清中的结合位点时,可以将该抗血清与放射性标记的化合物I一起用于放射免疫测定方法中,以测定生物流体中的安非他酮。用于放射免疫分析的测试试剂盒包含抗血清,放射性标记的化合物I和安非他酮。

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