mibolerone

The AR agonists DHT and mibolerone demonstrated similar effects as compared to R1881, differing only in that DHT was approximately 10-fold less efficient in inducing nuclear translocation.

PLoS ONE Alerts: New Articles Adam T. Szafran et al. 2008

Tested compounds include known AR agonist R1881 (A), mibolerone (B), and DHT (C) as well as other steroidal compounds estradiol (D), progesterone

PLoS ONE Alerts: New Articles Adam T. Szafran et al. 2008

For the F764L mutation associated with AIS, it is significant that we were able to observe an increased response with the synthetic androgen R1881 and mibolerone.

PLoS ONE Alerts: New Articles Adam T. Szafran et al. 2008

Because HeLa cells do not express the enzymes necessary to metabolize DHT, the increased responses observed with R1881 and mibolerone are due to characteristics of the ligands, and not higher intracellular concentrations than DHT.

PLoS ONE Alerts: New Articles Adam T. Szafran et al. 2008

[29], the synthetic androgens R1881 and mibolerone are relatively stable [30].

PLoS ONE Alerts: New Articles Adam T. Szafran et al. 2008

The effects of the F764L mutation on AR nuclear translocation (A), nuclear hyperspeckling (B), and transcriptional reporter gene activity (C) in HeLa cells with treated with R1881 (red), mibolerone (black), or DHT (green).

PLoS ONE Alerts: New Articles Adam T. Szafran et al. 2008

[28] were tested over a wide range of concentrations, including R1881, mibolerone, and DHT.

PLoS ONE Alerts: New Articles Adam T. Szafran et al. 2008