The Sound of Evolution
Estazolam
Mechanism of action:
Estazolam is a 1,4-benzodiazepine derivative. Estazolam binds to the benzodiazepine-binding site of the GABA_A receptor and increases the affinity of GABA for its receptor. This increases the frequency of chloride channel (Cl⁻ channel) opening, allowing chloride ions to flow into neurons and causing membrane hyperpolarization. These effects are associated with central nervous system depression, including sedation, hypnosis, anxiolysis, and anticonvulsant activity.
Reference(s):
1. Watanabe S et al. (1986). Electroencephalographic effects of 450191-S and its metabolites in rabbits with chronic electrode implants. Nihon Yakurigaku Zasshi.
2. Oishi R et al. (1986). Diazepam-induced decrease in histamine turnover in mouse brain. Eur J Pharmacol.
3. Usami N et al. (2002). Substrate specificity of human 3(20)alpha-hydroxysteroid dehydrogenase for neurosteroids and its inhibition by benzodiazepines. Biol Pharm Bull.