Benzodiazepine and GABA-gated channels

GABA-gated channels mediate inhibition in the Central Nervous System (CNS). Benzodiazephines such as Diazepam bind to the GABA(a) receptor which increases frequency of GABA-gated channel openings, allowing more Cl(-) ions through the channel at synapse, which cause negative charge hyperpolarization, promoting inhibition in the cell.
Other types of drugs, barbiturates, bind to different sites on the GABA(a) receptor and carry out different tasks which also result in IPSP responses (increasing duration of channel opening). Ethanol also binds to sites on the GABA(a) receptor.



The natural endogenous ligands (binding neurotransmitter) that should resemble benzodiazephine stuctures are yet to be found. They are assumed to exist because receptors for them exist. Similar motivation for the search of endogenous ligands arose from discovery of CB1 and CB2 receptors (cannaboid receptors) where a cannaboid-like ligand was expected to be found (and was found).