Ro 41-5253 is a potent and selective retinoic acid receptor-α (RARα) antagonist with IC50 of 16 nM.
Ro41-5253 treatment ameliorated the depressive-like behaviors in CUMS rats, as evidenced by increased sucrose preference in SPT, raised numbers of crossing and rearing in OFT, reduced immobility time and prolonged swimming time in FST.
Ro41-5253 (1 mg/kg) attenuated HPA axis hyperactivity by reduced serum corticosterone level, decreased adrenal gland index, reduced corticotrophin-releasing hormone protein level in hypothalamus, and recovered hypothalamic glucocorticoid receptor protein level.
Ro41-5253 (1 mg/kg) treatment downregulated RARα protein expression in hypothalamic PVN and hypothalamus, and increased the protein levels of BDNF, PSD95, SYP and MAP2 in the hippocampus.
Ro41-5253 completely abolished atRA-induced increase in fms transcript levels in breast carcinoma cells.
