Gabazine

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Gabazine
Gabazine.svg
Systematic (IUPAC) name
4-[6-imino-3-(4-methoxyphenyl)pyridazin-1-yl] butanoic acid hydrobromide
Clinical data
Legal status
?
Identifiers
CAS number 104104-50-9
ATC code None
PubChem CID 107895
ChemSpider 4925141 YesY
ChEMBL CHEMBL303580 YesY
Chemical data
Formula C15H18BrN3O3 
Mol. mass 368.226
 YesY (what is this?)  (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.[1] Gabaminergic drugs (such as benzodiazepines and barbiturates) would likely antagonize gabazines effects, effectively functioning as antidotes.

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]

References[edit]

  1. ^ Behrens, CJ; Van Den Boom, LP; Heinemann, U (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): 2170–81. doi:10.1111/j.1460-9568.2007.05462.x. PMID 17419756. 
  2. ^ Ueno, S; Bracamontes, J; Zorumski, C; Weiss, DS; Steinbach, JH (1997). "Bicuculline and gabazine are allosteric inhibitors of channel opening of the GABAA receptor". The Journal of neuroscience : the official journal of the Society for Neuroscience 17 (2): 625–34. PMID 8987785. 
  3. ^ Yeung, JY; Canning, KJ; Zhu, G; Pennefather, P; MacDonald, JF; Orser, BA (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.