Increased number of brain benzodiazepine receptors after in-vivo administration of estazolam to rats.
Estazolam significantly increased the Kd of [3H]flunitrazepam in-vitro, like other benzodiazepines (BDZs) acting competitively at the receptor site. At variance with other BDZs, estazolam significantly raised the Bmax for [3H]flunitrazepam, at concentrations lower than its Ki for BDZ receptors. This effect may be responsible for the observed increase in [3H]diazepam binding after in-vivo administration of estazolam to rats.
D000818:Animals; D014151:Anti-Anxiety Agents / Q000494:pharmacology*; D001665:Binding Sites / Q000187:drug effects; D001921:Brain / Q000378:metabolism*; D002531:Cerebellum / Q000378:metabolism; D003975:Diazepam / Q000378:metabolism; D004949:Estazolam / Q000494:pharmacology*; D005445:Flunitrazepam / Q000494:pharmacology; D006624:Hippocampus / Q000378:metabolism; D066298:In Vitro Techniques; D007700:Kinetics; D008297:Male; D051381:Rats; D011963:Receptors, GABA-A / Q000378:metabolism*; D005680:gamma-Aminobutyric Acid / Q000378:metabolism
D014151:Anti-Anxiety Agents; D011963:Receptors, GABA-A; D004949:Estazolam; D005680:gamma-Aminobutyric Acid; D005445:Flunitrazepam; D003975:Diazepam