(Z)-17 beta-hydroxy-17 alpha-(2-[125I]iodovinyl)-4-estren-3-one: a new specific gamma-emitting ligand for determination of progesterone receptor.
An iodine-125 labeled ligand for progesterone receptor determination was synthesized: (Z)-17 beta-hydroxy-17 alpha-(2-[125I]iodovinyl)-4-estren-3-one ([125I]SH-D 510). The ligand is stable chemically as well as under the conditions of a receptor assay. The relative binding affinity of the nonradioactive compound towards human uterine progesterone receptor was 7.0 for the Z-isomer (promegestone (R5020) 1.0) and 0.95 for the E-isomer. 4 S and 8 S receptor forms were obtained on sucrose density gradient analysis. Progesterone receptors were assayed in 103 human mammary tumour cytosols, using either [3H]promegestone or [125I]SH-D 510. The coefficient of correlation was r = 0.951.
D000818:Animals; D003600:Cytosol / Q000032:analysis; D005260:Female; D006801:Humans; D066298:In Vitro Techniques; D008297:Male; D008325:Mammary Neoplasms, Experimental / Q000032:analysis; D009277:Nandrolone / Q000031:analogs & derivatives* / Q000138:chemical synthesis; D011467:Prostate / Q000032:analysis; D011869:Radioligand Assay; D051381:Rats; D011944:Receptors, Androgen / Q000032:analysis; D011980:Receptors, Progesterone / Q000032:analysis*; D014599:Uterus / Q000032:analysis
D011944:Receptors, Androgen; D011980:Receptors, Progesterone; D009277:Nandrolone; C049157:(2-iodovinyl)-19-nortestosterone