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Pharmacological characterization of AC-262536, a novel selective androgen receptor modulator

Piu, Fabrice ; Gardell, Luis R. ; Son, Thomas ; Schlienger, Nathalie ; Lund, Birgitte W. ; Schiffer, Hans H. ; Vanover, Kim E. ; Davis, Robert E. ; Olsson, Roger LU and Bradley, Stefania Risso (2008) In Journal of Steroid Biochemistry and Molecular Biology 109(1-2). p.129-137
Abstract

Because of the limitations and liabilities of current testosterone therapies, non-steroidal tissue-selective androgen receptor modulators may provide a clinically meaningful advance in therapy. Using a functional cell-based assay AC-262536 was identified as a potent and selective AR ligand, with partial agonist activity relative to the natural androgen testosterone. A 2-week chronic study in castrated male rats indicated that AC-262536 significantly improves anabolic parameters in these animals, especially in stimulating the growth of the levator ani and in suppressing elevated LH levels. In sharp contrast to testosterone, AC-262536 has weak androgenic effects, as measured by prostate and seminal vesicle weights. Thus, AC-262536... (More)

Because of the limitations and liabilities of current testosterone therapies, non-steroidal tissue-selective androgen receptor modulators may provide a clinically meaningful advance in therapy. Using a functional cell-based assay AC-262536 was identified as a potent and selective AR ligand, with partial agonist activity relative to the natural androgen testosterone. A 2-week chronic study in castrated male rats indicated that AC-262536 significantly improves anabolic parameters in these animals, especially in stimulating the growth of the levator ani and in suppressing elevated LH levels. In sharp contrast to testosterone, AC-262536 has weak androgenic effects, as measured by prostate and seminal vesicle weights. Thus, AC-262536 represents a novel class of selective androgen receptor modulators (SARMs) with beneficial anabolic effects.

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author
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publishing date
type
Contribution to journal
publication status
published
subject
keywords
Non-steroidal, Selective androgen receptor modulator
in
Journal of Steroid Biochemistry and Molecular Biology
volume
109
issue
1-2
pages
9 pages
publisher
Elsevier
external identifiers
  • scopus:40849102688
  • pmid:18164613
ISSN
0960-0760
DOI
10.1016/j.jsbmb.2007.11.001
language
English
LU publication?
no
id
170e5956-7c77-4acc-86c8-d3a37f1111bc
date added to LUP
2019-10-02 10:24:52
date last changed
2020-01-13 02:26:14
@article{170e5956-7c77-4acc-86c8-d3a37f1111bc,
  abstract     = {<p>Because of the limitations and liabilities of current testosterone therapies, non-steroidal tissue-selective androgen receptor modulators may provide a clinically meaningful advance in therapy. Using a functional cell-based assay AC-262536 was identified as a potent and selective AR ligand, with partial agonist activity relative to the natural androgen testosterone. A 2-week chronic study in castrated male rats indicated that AC-262536 significantly improves anabolic parameters in these animals, especially in stimulating the growth of the levator ani and in suppressing elevated LH levels. In sharp contrast to testosterone, AC-262536 has weak androgenic effects, as measured by prostate and seminal vesicle weights. Thus, AC-262536 represents a novel class of selective androgen receptor modulators (SARMs) with beneficial anabolic effects.</p>},
  author       = {Piu, Fabrice and Gardell, Luis R. and Son, Thomas and Schlienger, Nathalie and Lund, Birgitte W. and Schiffer, Hans H. and Vanover, Kim E. and Davis, Robert E. and Olsson, Roger and Bradley, Stefania Risso},
  issn         = {0960-0760},
  language     = {eng},
  month        = {03},
  number       = {1-2},
  pages        = {129--137},
  publisher    = {Elsevier},
  series       = {Journal of Steroid Biochemistry and Molecular Biology},
  title        = {Pharmacological characterization of AC-262536, a novel selective androgen receptor modulator},
  url          = {http://dx.doi.org/10.1016/j.jsbmb.2007.11.001},
  doi          = {10.1016/j.jsbmb.2007.11.001},
  volume       = {109},
  year         = {2008},
}