Androgenic agonist activity

A highly fluorinated androgen agonist, LGD-2941, is in early clinical development for the treatment of several indications related to the beneficial effects of the androgen receptor activation (e.g., hypogonadism). 

Fig. 5. Specificity of steroid response element. A. In this example (mouse mammary tumour virus), the element will bind receptors for glucocorticoids (G), androgen (A), progestin (P) and mineralocorticoid (M) so that each of these classes of steroid stimulate transcription. This type of specificity can vary from cell to cell possibly due to other protein factors (not shown). B. Although oestrogen (E) receptor will not act as an agonist for mouse mammary tumour virus transcription, it may antagonise the agonist activity of glucocorticoids (G).

Androgens Testosterone receptor agonists active against some breast and renal cancers. Mechanism unknown. 

In addition to quinoline-based SARMs, tetrahydroquinoline-derived drug candidates were reported to possess tissue-selective androgen receptor agonist activity. Two representatives are S-40503 and 2-methyl-2-(8-nitro-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]chinolin-4-yl)propan-l-ol (Fig. 4.9,12 and 13), and the mass spectrometric behavior was studied for both compounds. The protonated molecule of 13 at m/z 289 dissociates under CID conditions by the loss of a hydroxyl radical (-17 Da) originating from the nitro function. The proton affinity of 1,2,3,4-tetrahydroquinoline was determined as 225 kcal/mol and... 

---