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.
(Less)
- author
- 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
- publishing date
- 2008-03-01
- 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
-
- pmid:18164613
- scopus:40849102688
- 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
- 2024-01-01 21:27:53
@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}},
keywords = {{Non-steroidal; Selective androgen receptor modulator}},
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}},
}