Binding of 17-alpha-methyltestosterone in vitro to human sex hormone binding globulin and rat ventral prostate androgen receptors

We measured the relative binding affinity (RBA) of 17-alpha-methyltestosterone (MET) for the rat prostate androgen receptor and human sex hormone-binding globulin (SHBG) in vitro. The reference compound in both instances was dihydrotestosterone (DHT), the RBA of which was set at 100%. The RBA of met...

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Bibliographic Details
Published inTherapeutic drug monitoring Vol. 17; no. 4; p. 377
Main Authors Wiita, B, Artis, A, Ackerman, D M, Longcope, C
Format Journal Article
LanguageEnglish
Published United States 01.08.1995
Subjects
Animals
Dihydrotestosterone - metabolism
Female
Humans
Male
Methyltestosterone - metabolism
Prostate - metabolism
Protein Binding
Rats
Receptors, Androgen - metabolism
Sex Hormone-Binding Globulin - metabolism
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Summary:We measured the relative binding affinity (RBA) of 17-alpha-methyltestosterone (MET) for the rat prostate androgen receptor and human sex hormone-binding globulin (SHBG) in vitro. The reference compound in both instances was dihydrotestosterone (DHT), the RBA of which was set at 100%. The RBA of methyltestosterone was 44% for the androgen receptor, but 11% for SHBG. The androgen receptor, therefore, would appear to recognize a different part of an androgen compared to the recognition site on SHBG. The difference in RBAs may amplify the biologic action of methyltestosterone.
ISSN:0163-4356
DOI:10.1097/00007691-199508000-00011