Small molecule
PubChem CID 3016
Diazepam
Valium
- Mechanism of action
- GABA-A receptor positive allosteric modulator
- In plain language
- Calms overactive brain activity by boosting the effect of a natural chemical that puts the brakes on nerve signals.
- How it works
- Diazepam is a benzodiazepine that binds to an allosteric site on the GABA-A receptor complex, distinct from the GABA binding site itself. This binding increases the frequency of GABA-gated chloride channel opening, potentiating the inhibitory effect of GABA, the principal inhibitory neurotransmitter in the CNS. The resulting enhanced chloride influx hyperpolarizes neurons, reducing overall neuronal excitability across cortical and limbic circuits. This broad CNS inhibition underlies diazepam's anxiolytic, sedative, muscle-relaxant, anticonvulsant, and amnestic effects.
- Therapeutic applications
- Indicated for the management of anxiety disorders and short-term relief of anxiety symptoms; symptomatic relief of acute alcohol withdrawal; adjunctive therapy for skeletal muscle spasm due to local pathology or spasticity from upper motor neuron disorders; and adjunctive (not sole) therapy in convulsive disorders.
- Class
- Small molecule
- Therapeutic area
- CNS / Anxiety
View
Related compounds