Synonyms GABA(A) receptor subunit delta, GABA(A) receptor, delta, GABRD + [3] |
Introduction Delta subunit of the heteropentameric ligand-gated chloride channel gated by gamma-aminobutyric acid (GABA), a major inhibitory neurotransmitter in the brain (PubMed:35355020). GABA-gated chloride channels, also named GABA(A) receptors (GABAAR), consist of five subunits arranged around a central pore and contain GABA active binding site(s) located at the alpha and beta subunit interface(s) (PubMed:35355020). When activated by GABA, GABAARs selectively allow the flow of chloride anions across the cell membrane down their electrochemical gradient (PubMed:35355020). GABAARs containing delta/GABRD subunits are predominantly located in extrasynaptic or perisynaptic positions on hippocampus and cerebellar granule cells, and contribute to the tonic GABAergic inhibition (By similarity). GABAAR containing alpha-4-beta-3-delta subunits can simultaneously bind GABA and histamine where histamine binds at the interface of two neighboring beta subunits, which may be involved in the regulation of sleep and wakefulness (PubMed:35355020). |
Target |
Mechanism GABRA2 modulators [+1] |
Active Org.- |
Originator Org. |
Active Indication- |
Inactive Indication |
Drug Highest PhaseDiscontinued |
First Approval Ctry. / Loc.- |
First Approval Date20 Jan 1800 |
Target |
Mechanism GABRA4 modulators [+3] |
Active Org.- |
Originator Org. |
Active Indication- |
Inactive Indication |
Drug Highest PhasePending |
First Approval Ctry. / Loc.- |
First Approval Date20 Jan 1800 |