AIM: To study the toxic effect of moclobemide on male breast and to elucida
te its mechanism of action. METHODS: Routine histopathological analysis was
used to diagnose the effect of moclobemide on male breast in mts. Plasma c
oncentrations of estrogen, androgen, and prolactin were measured by a ratio
immunometer and relative receptors of mammary gland tissue were detected im
munohistochemically. RESULTS: After 180-d moclobemide treatment, the presen
ce of gynecomastia was 0, 5, 5, 7/10 rats in 0, 60, 240, and 600 mg/kg grou
ps, respectively. After 30-d convalescence, only one rat in 600 mg/kg group
got the incidence of gynecomastia. Serum prolactin concentration had a tre
nd to decrease with increasing dose and prolactin receptors in mammary glan
d were up-regulated. CONCLUSION: Long-term treatment with moclobemide cause
s gynecomastia in rats, which is reversible. The mechanism of moclobemide-i
nduced gynecomastia may be related to the increase in prolactin receptors i
n mammary glands.