Gabazine

Gabazine

Gabazine bromide
Clinical data
ATC code	none
Identifiers
IUPAC name 2-(3-carboxypropyl)-6-(4-methoxyphenyl)-2,3-dihydropyridazin-3-iminium bromide
JSmol)	Interactive image
SMILES [Br-].C(=O)(O)CCCN1N=C(C=CC1=[NH2+])C1=CC=C(C=C1)OC
InChI InChI=1S/C15H17N3O3.BrH/c1-21-12-6-4-11(5-7-12)13-8-9-14(16)18(17-13)10-2-3-15(19)20;/h4-9,16H,2-3,10H2,1H3,(H,19,20);1H Y Key:GFZHNFOGCMEYTA-UHFFFAOYSA-N Y
(verify)

Gabazine (SR-95531) is a drug that acts as an antagonist at GABA_A receptors. It is used in scientific research and has no role in medicine, as it would be expected to produce convulsions if used in humans.^[1]

Gabazine binds to the GABA recognition site of the receptor-channel complex and acts as an allosteric inhibitor of channel opening.^[2] The net effect is to reduce GABA-mediated synaptic inhibition by inhibiting chloride flux across the cell membrane, and thus inhibiting neuronal hyperpolarization. While phasic (synaptic) inhibition is gabazine-sensitive, tonic (extrasynaptic) inhibition is relatively gabazine-insensitive.^[3]

Gabazine has been found to bind to and antagonize α₄βδ subunit-containing GABA_A receptors, which may represent the GHB receptor.^[4]

References