Bazedoxifene - a promising brain active SERM that crosses the blood brain barrier and enhances spatial memory
RA Hill, K Kouremenos, D Tull, A Maggi, A Schroeder, A Gibbons, J Kulkarni, S Sundram, X Du
PSYCHONEUROENDOCRINOLOGY | PERGAMON-ELSEVIER SCIENCE LTD | Published : 2020
Over 20 years of accumulated evidence has shown that the major female sex hormone 17β-estradiol can enhance cognitive functioning. However, the utility of estradiol as a therapeutic cognitive enhancer is hindered by its unwanted peripheral effects (carcinogenic). Selective estrogen receptor modulators (SERMs) avoid the unwanted effects of estradiol by acting as estrogen receptor antagonists in some tissues such as breast and uterus, but as agonists in others such as bone, and are currently used for the treatment of osteoporosis. However, understanding of their actions in the brain are limited. The third generation SERM bazedoxifene has recently been FDA approved for clinical use with an impr..View full abstract
R.A.H. is supported by a National Health and Medical Research Council Career Development (R.D. Wright) Fellowship. This research was supported by a NARSAD Young Investigator award for R.A.H. X.D. was supported by an NHMRC/ARC Dementia Research Development Fellowship.