BACKGROUND: Salbutamol has been shown to mediate anabolic effects after intravenous administration. However, the mechanism responsible for the anabolic actions of salbutamol remains unknown. AIM: To investigate the potential mechanism by which salbutamol mediates anabolic effects in vitro. METHODS: The 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), 5alpha-dihydrotestosterone (DHT) and danazol. IC50 values of R1881, DHT and danazol, 4.41x10(-11), 4.44x10(-11) and 1.08x10(-8) M, respectively, were in the ranges known from earlier studies. Our results demonstrate that salbutamol exhibits androgenic activity, with an IC50 value of 8.93x10(-6) M. Anti-estrogenic or cytotoxic effects, which might have interfered with the assay, were excluded by additional experiments on wild-type MCF7 and MCF7-AR1 cells, respectively. CONCLUSION: These data indicate that salbutamol exerts anabolic effects through androgen receptor agonistic activity in vitro.
BACKGROUND:Salbutamol has been shown to mediate anabolic effects after intravenous administration. However, the mechanism responsible for the anabolic actions of salbutamol remains unknown. AIM: To investigate the potential mechanism by which salbutamol mediates anabolic effects in vitro. METHODS: The 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), 5alpha-dihydrotestosterone (DHT) and danazol. IC50 values of R1881, DHT and danazol, 4.41x10(-11), 4.44x10(-11) and 1.08x10(-8) M, respectively, were in the ranges known from earlier studies. Our results demonstrate that salbutamol exhibits androgenic activity, with an IC50 value of 8.93x10(-6) M. Anti-estrogenic or cytotoxic effects, which might have interfered with the assay, were excluded by additional experiments on wild-type MCF7 and MCF7-AR1 cells, respectively. CONCLUSION: These data indicate that salbutamol exerts anabolic effects through androgen receptor agonistic activity in vitro.
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