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

摘要

New compounds are prepared having the formula: wherein (1) X1 is Cl, R<2> is oxygen and R<1> is -(CH2)n-OH or -(CH2)n-O-(CO)m(CH2)pCOZ or -O-(CH2)pCOZ or -O-(CH2)pCOOR11 or is a radioisotope or (2) X1 is Cl, R<1> is H and R<2> is = N.O(CH2)qCOZ or (3) X1 is a radioisotope, R2 is oxygen and R1 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 R7 is OH. Various methods for their preparation are described. The unlabelled compounds in which R1 and R2 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 radio-immunoassay contains antisera, radioactive labelled compound I and optionally bupropion.