Hobe G, Reddersen G, Wesemann R, Hübner M, Menzenbach B, Wagner H, Römer J, Frankenberg G, Schubert K
Pharmazie. 1986 Sep;41(9):627-30.
In order to develop a radioimmunoassay for the new progestagen dienogest (STS 557, 17 alpha-cyanomethyl-17 beta-hydroxy-estra-4,9-dien-3-one), bovine serum albumin (BSA) conjugates of STS 557-3-carboxymethyloxime and of STS 557-11-hemisuccinate were synthesized as antigens for the production of antisera. It was proved that an excess of isobutylchlorocarbonate in the coupling reaction using the "mixed anhydride method" results in an acylation of free NH2-groups in the BSA. By the immunization of rabbits with the STS 557-antigen-antisera of high specificity and affinity to STS 557 were produced. Endogenous steroids show no cross reaction with the STS 557-antisera. Steroids with a 17 alpha-CH2CN-group, being obtained by chemical synthesis or microbial transformation, compete with STS 557 for the binding positions of the antibodies to a different extent.
为开发针对新型孕激素地诺孕素(STS 557,17α-氰甲基-17β-羟基-雌甾-4,9-二烯-3-酮)的放射免疫分析方法,合成了STS 557-3-羧甲基肟和STS 557-11-半琥珀酸酯的牛血清白蛋白(BSA)缀合物作为抗原以制备抗血清。已证明,在使用“混合酸酐法”的偶联反应中过量的异丁基氯甲酸酯会导致BSA中游离NH2基团的酰化。通过用STS 557抗原免疫兔子,产生了对STS 557具有高特异性和亲和力的抗血清。内源性类固醇与STS 557抗血清无交叉反应。通过化学合成或微生物转化获得的具有17α-CH2CN基团的类固醇,在不同程度上与STS 557竞争抗体的结合位点。