Gabazine

Gabazine
Gabazine bromide
Clinical data
ATC code
  • none
Identifiers
  • 2-(3-carboxypropyl)-6-(4-methoxyphenyl)-2,3-dihydropyridazin-3-iminium bromide
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
Formula C15H18BrN3O3
Molar mass 368.226 g·mol−1
3D model (JSmol)
  • [Br-].C(=O)(O)CCCN1N=C(C=CC1=[NH2+])C1=CC=C(C=C1)OC
  • 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 check
  • Key:GFZHNFOGCMEYTA-UHFFFAOYSA-N check
  (verify)

Gabazine (SR-95531) is a drug that acts as an antagonist at GABAA 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.

Gabazine binds to the GABA recognition site of the receptor-channel complex and acts as an allosteric inhibitor of channel opening. 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.

Gabazine has been found to bind to and antagonize α4βδ subunit-containing GABAA receptors, which may represent the GHB receptor.