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Moclobemide-induced gynecomastia in rats
1State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 200031, China.
Aim:
To study the toxic effect of moclobemide on male breast and to elucidate its mechanism of action.
Methods:
Routine histopathological analysis was used to diagnose the effect of moclobemide on male breast in rats. Plasma concentrations of estrogen, androgen, and prolactin were measured by a ratioimmunometer and relative receptors of mammary gland tissue were detected immunohistochemically.
Results:
After 180-d moclobemide treatment, the presence of gynecomastia was 0, 5, 5, 7/10 rats in 0, 60, 240, and 600 mg/kg groups, respectively. After 30-d convalescence, only one rat in 600 mg/kg group got the incidence of gynecomastia. Serum prolactin concentration had a trend to decrease with increasing dose and prolactin receptors in mammary gland were up-regulated.
Conclusion:
Long-term treatment with moclobemide causes gynecomastia in rats, which is reversible. The mechanism of moclobemide-induced gynecomastia may be related to the increase in prolactin receptors in mammary glands.