Background: Salbutamol has been shown to mediate anabolic effects after intravenous administration. However, the underlying mechanism responsible for anabolic actions of salbutamol remains unknown.
Objective: To investigate potential mechanism by which salbutamol mediates anabolic effects in vitro.
Methods: Potential androgenic activity of salbutamol was investigated in vitro by the A-Screen assay that measures androgen-dependent inhibition of proliferation of the androgen receptor (AR)-positive human mammary carcinoma cell line, MCF7-AR1.
Results: The assay was validated with three known androgens (methyltrienolone (R1881), 5-αdihydrotestosterone (DHT) and danazol). IC50 values of R1881, DHT and danazol, 4.41 x 10–11, 4.44 x 10-11 and 1.08 x 10-8 M, were in the range known from earlier studies. Our results indicate that salbutamol exhibits androgenic activity, with an IC50 value of 8.93 x 10-6 M. Anti-estrogenic or cytotoxic effects which might have interfered with the assay, were excluded by additional experiments on wildtype MCF7 and MCF7-AR1 cells, respectively.
Conclusion: These data indicate that salbutamol exerts anabolic effects through androgen receptor agonistic activity in vitro.
- androgen receptor
- beta-2 agonist