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Gabazine chemical structure
Gabazine

4-[6-imino-3-(4-methoxyphenyl)pyridazin-1-yl] butanoic acid hydrobromide
IUPAC name
CAS number
104104-50-9
ATC code

none{{{ATC_suffix}}}

PubChem
107895
DrugBank
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Chemical formula {{{chemical_formula}}}
Molecular weight 368.226
Bioavailability
Metabolism
Elimination half-life
Excretion
Pregnancy category {{{pregnancy_category}}}
Legal status
Routes of administration {{{routes_of_administration}}}


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]

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]

See alsoEdit

ReferencesEdit

  1. (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.
  2. (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.
  3. (2003). Tonically activated GABAA receptors in hippocampal neurons are high-affinity, low-conductance sensors for extracellular GABA. Molecular Pharmacology 63 (1): 2–8.



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