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Binding of [3H] methyltrienolone (R 1881) in rat prostate and human benign prostatic hypertrophy (BPH).
Authors:J Asselin  F Labrie  Y Gourdeau  C Bonne  J P Raynaud
Institution:Medical Research Council Group in Molecular Endocrinology, Le Centre Hospitalier de l''Université Laval, Québec, G1V 4G2, Canada, L''Hôpital de l''Enfant-Jésus, Québec, and Centre de Recherches Roussel-UCLAF, 93230 Romainville, France
Abstract:Methyltrienolone (R 1881 - 17beta-hydroxy-17alpha-methyl-estra-4, 9, 11-trien-3-one) binding to rat ventral prostate cytosol has a specificity typical of an androgen receptor. In human benign prostatic hypertrophy (BPH) tissue, the specificity of 3H] R 1881 binding is different from that measured in rat prostate: progesterone and R 5020 (17, 21-dimethyl-19-nor-4, 9-pregnadiene-3, 20-dione) being more potent while 19-nortestosterone is less potent competitor. Moreover, the synthetic progestin 3H] R 5020 binds to BPH tissue with a similar specificity. These data suggest the presence of progestin binding components or of an atypical androgen receptor in human BPH cytosol.
Keywords:R 1881  methyl trienolone  17β-hydroxy-17α-methyl-estra-4  9  11-trien-3-one  DHT  androstanolone  5α-dihydrotestosterone = 17β-hydroxy-5α-androstan-3-ne  T  testosterone  17β-hydroxy-4-androsten-3-one  epitestosterone  17α-hydroxy-4-androsten-3-one  androstenedione  4-androstene-3  17-dione  progesterone  4-pregnene-3  20-dione  cyproterone acetate  6-chloro-17α-acetoxy-1  2α-methylene-4  6-pregnadiene-3  20-dione  estradiol  1  3  5 (10)-estratriene-3  17β-diol  19-nortestosterone  17β-hydroxy-4-estren-3-one  androstanediol  5α-androstane-3α  17β-diol  R 5020  17  21-dimethyl-19-nor-4  9-pregnadiene-3  20-dione
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