Purpose: To investigate the effects of formoterol (a beta2-adrenoreceptor agonist) on serum and peritoneal fluid VEGF, malondialdehyde (MDA) levels, and on VEGF-stained cell counts in the ovaries and endometrium of rats with ovarian hyperstimulation syndrome (OHSS) within the framework of immunohistochemical analysis. Materials and Methods: A total of 28 immature female Wistar rats were randomly divided into four groups. Three groups were given ten IU pregnant mare serum gonadotropin/day on days 22–25 of life. They were administered 30 IU hCG on day 26 of life to mimic OHSS. On days 26 and 27 of life, 24 mcg/kg/day formoterol in group 3 and 48 mcg/kg formoterol in group 4 were administered intraperitoneally per animal. Results: Although, there were no statistically significant differences between the groups in terms of serum and peritoneal fluid VEGF or MDA levels (serum VEGF: p = 0.281, peritoneal VEGF: p = 0.674, serum MDA: p = 0.543, peritoneal MDA: p = 0.506), there was a significant difference between the control and the OHSS placebo groups (p = 0.013) regarding the VEGF in the ovarian cortex. There was a significant difference between the control and the other groups in terms of ovarian stroma (p = 0.001), and there was also a statistically significant difference between the OHSS placebo and the other groups regarding VEGF in the endometrium (OHSS placebo vs. control group p = 0.002, OHSS placebo vs. the formoterol 24 mcg/kg group, p = 0.008, and OHSS-placebo vs. the formoterol 48 mcg/kg group, p = 0.001). Conclusions: Formoterol represents a potential novel strategy for the management of OHSS. Further studies, including those examining the dosage of formoterol, are warranted.