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I'm looking for an inducer that strongly activates the androgen receptor, but not the glucocorticoid receptor that is not DEA regulated. I know that SARMS (Selective Androgen Receptor Modulators) are something of a hot topic in some corners of some fields, but I'm having some trouble in my laboratory finding one. My research necessitates the independent induction of AR (Androgen Receptor). Does anyone know how to go about this search or know of some chemical?

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Are you looking for literature? If so this is a recent review: Zhang et al. (2013) Deciphering the selective androgen receptor modulators paradigm. EXPERT OPINION ON DRUG DISCOVERY 8: 191-218 DOI: 10.1517/17460441.2013.741582 –  Alan Boyd Jul 1 '13 at 15:51

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up vote 2 down vote accepted

Take a look at the paper by Ojasoo et al. [1] It reports the relative binding affinity for a wide variety of steroids for the AR, PR and GR.

Nandrolone (19-nor testosterone) does not have any affinity for the GR, but is a potent activator of the AR. However, it does have some affinity for the progesterone receptor (does this matter for your research?). Additionally, nandrolone bound to the AR also binds estrogen response elements (does this matter for your research?).

5a-DHT also is a potent AR activator with no affinity for the GR. Do note that a metabolite of 5a-DHT has significant affinity for the estrogen receptor, might that matter for your research.

You might also use a strong GR antagonist in conjunction with an androgen which also has some affinity for the GR. Then you can simply use methyltrienolone, as commonly used as AR ligand.

On a sidenote: do note that androgens usually only lead to significant dissociation of a GR ligand for the GR at very high concentrations. Therefore, androgens most likely act as GR antagonist by heterodimer formation of the AR with GR [2], as well as through squelching [3].

References

  1. Ojasoo, T., et al. "Towards the mapping of the progesterone and androgen receptors." Journal of steroid biochemistry 27.1 (1987): 255-269.
  2. Chen, Sei-yu, et al. "Androgen and glucocorticoid receptor heterodimer formation A possible mechanism for mutual inhibition of transcriptional activity." Journal of Biological Chemistry 272.22 (1997): 14087-14092.
  3. Zhao, Jingbo, et al. "Oxandrolone blocks glucocorticoid signaling in an androgen receptor-dependent manner." Steroids 69.5 (2004): 357-366.
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