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Gabazine

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
Gabazine
Gabazinebromide
Clinical data
ATC code
  • none
Identifiers
  • 2-(3-carboxypropyl)-6-(4-methoxyphenyl)-2,3-dihydropyridazin-3-iminium bromide
CAS Number
PubChemCID
ChemSpider
UNII
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC15H18BrN3O3
Molar mass368.231 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 checkY
  • Key:GFZHNFOGCMEYTA-UHFFFAOYSA-N checkY
  (verify)

Gabazine (SR-95531) is adrug that acts as anantagonist atGABAAreceptors. It is used in scientific research and has no role in medicine, as it would be expected to produceconvulsions if used in humans.[1]

Gabazine binds to the GABA recognition site of the receptor-channel complex and acts as anallosteric inhibitor of channel opening.[2] The net effect is to reduce GABA-mediatedsynaptic inhibition by inhibitingchloride 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 α4βδsubunit-containing GABAA receptors, which may represent theGHB receptor.[4]

References

[edit]
  1. ^Behrens CJ, van den Boom LP, Heinemann U (April 2007). "Effects of the GABA(A) receptor antagonists bicuculline and gabazine on stimulus-induced sharp wave-ripple complexes in adult rat hippocampus in vitro".The European Journal of Neuroscience.25 (7):2170–2181.doi:10.1111/j.1460-9568.2007.05462.x.PMID 17419756.S2CID 85328190.
  2. ^Ueno S, Bracamontes J, Zorumski C, Weiss DS, Steinbach JH (January 1997)."Bicuculline and gabazine are allosteric inhibitors of channel opening of the GABAA receptor".The Journal of Neuroscience.17 (2):625–634.doi:10.1523/jneurosci.17-02-00625.1997.PMC 6573228.PMID 8987785.
  3. ^Yeung JY, Canning KJ, Zhu G, Pennefather P, MacDonald JF, Orser BA (January 2003). "Tonically activated GABAA receptors in hippocampal neurons are high-affinity, low-conductance sensors for extracellular GABA".Molecular Pharmacology.63 (1):2–8.doi:10.1124/mol.63.1.2.PMID 12488530.S2CID 6827514.
  4. ^Absalom N, Eghorn LF, Villumsen IS, Karim N, Bay T, Olsen JV, et al. (August 2012)."α4βδ GABA(A) receptors are high-affinity targets for γ-hydroxybutyric acid (GHB)".Proceedings of the National Academy of Sciences of the United States of America.109 (33):13404–13409.Bibcode:2012PNAS..10913404A.doi:10.1073/pnas.1204376109.PMC 3421209.PMID 22753476.
Ionotropic
GABAATooltip γ-Aminobutyric acid A receptor
GABAA-ρTooltip γ-Aminobutyric acid A-rho receptor
Metabotropic
GABABTooltip γ-Aminobutyric acid B receptor
Receptor
(ligands)
GHBRTooltip GHB receptor
GABABTooltip γ-Aminobutyric acid B receptor
Transporter
(blockers)
MCTsTooltip Monocarboxylate transporters
SMCTsTooltip Sodium-coupled monocarboxylate transporters
VIATTTooltip Vesicular inhibitory amino acid transporter
Enzyme
(inhibitors)
SSRTooltip Succinic semialdehyde reductase
GHBDHTooltip 4-Hydroxybutyrate dehydrogenase
HOTTooltip Hydroxyacid-oxoacid transhydrogenase
ADHTooltip Alcohol dehydrogenase
ALDHTooltip Aldehyde dehydrogenase
GABA receptor antagonists
GABA synthesis inhibitors
Glycine receptor antagonists
Glutamate receptor agonists
Convulsantbarbiturates
Other
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