The Sound of Evolution
Diazepam
Mechanism of action:
Diazepam is a benzodiazepine derivative. It binds to the benzodiazepine-binding site of the GABA_A receptor and enhances the inhibitory effects of GABA_A receptor signaling. This increases the frequency of chloride channel opening, leading to chloride influx into neurons and causing membrane hyperpolarization. As a result, diazepam produces central nervous system depressant-related effects, including anxiolytic, sedative-hypnotic, and anticonvulsant actions.
Reference(s):
1. Mant A et al. (1993). Benzodiazepine utilisation in Australia: report from a new pharmacoepidemiological database. Aust J Public Health.
2. Earley JV et al. (1979). Quinazolines and 1,4-benzodiazepines. LXXXIX: Haptens useful in benzodiazepine immunoassay development. J Pharm Sci.
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.