Peripheral-type benzodiazepine receptors on human blood mononuclear cells are not regulated by ovarian steroids.
Peripheral-type benzodiazepine receptors (pBZr) have been shown to be sensitive to hormonal perturbations, including changes in ovarian steroids. This study examines whether estradiol and progesterone modulate pBZr binding in membranes of human blood mononuclear cells, as measured by binding of both 3H-PK 11195 and 3H-Ro 5-4864. Our findings were negative. There was no steroidal modulation of pBZr binding to these membrane preparations in vivo in normal women studied at different sex-steroid phases of the menstrual cycle, or during 8-30 weeks of pregnancy. There was also no effect of hormones on the binding sites in cultures of mononuclear cells treated with estradiol or progesterone (up to 10(-5) M) over a period between 2 and 72 h. Further, we performed in vitro competition experiments, which showed that both steroids are not active at the pBZr. Our data suggest that pBZr located in human blood mononuclear cells are insensitive to the physiological variations of circulating female hormones.
Ferrero
P
P
Department of Neurology, University of Turin, Italy.
Rocca
P
P
Montalenti
E
E
Benna
P
P
Milani
A
A
Ravizza
L
L
Bergamasco
B
B
D001570:Benzodiazepinones / Q000493:pharmacokinetics; D004958:Estradiol / Q000502:physiology*; D005260:Female; D006801:Humans; D007546:Isoquinolines / Q000493:pharmacokinetics; D008597:Menstrual Cycle / Q000502:physiology; D009000:Monocytes / Q000378:metabolism*; D011374:Progesterone / Q000502:physiology*; D011963:Receptors, GABA-A / Q000502:physiology*; D012016:Reference Values
D001570:Benzodiazepinones; D007546:Isoquinolines; D011963:Receptors, GABA-A; C028513:4'-chlorodiazepam; D011374:Progesterone; D004958:Estradiol; C037850:PK 11195