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20-September-2008 09:55:56 - Gabazine Gabazine Systematic IUPAC name 4-6-imino-3-4-methoxyphenylpyridazin-1-yl butanoic acid hydrobromide Identifiers CAS number 104104-50-9 ATC code ? PubChem 107895 Chemical data Formula C15H18BrN3O3 Mol. mass 368.226 Pharmacokinetic data Bioavailability ? Metabolism ? Half life ? Excretion ? Therapeutic considerations Pregnancy cat. ? Legal status Routes ? 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 depolarisation. While phasic synaptic inhibition is gabazine-sensitive, tonic extrasynaptic inhibition is gabazine-insensitive.3 References ^ Behrens CJ, van den Boom LP, Heinemann U. Effects of the GABAA receptor antagonists bicuculline and gabazine on stimulus-induced sharp wave-ripple complexes in adult rat hippocampus in vitro. European Journal of Neuroscience 2007 Apr;257:2170-81. ^ Ueno S, Bracamontes J, Zorumski C, Weiss DS, Steinbach JH. Bicuculline and gabazine are allosteric inhibitors of channel opening of the GABAA receptor. Journal of Neuroscience 1997 Jan 15;172:625-34. ^ Yeung JY, Canning KJ, Zhu G, Pennefather P, MacDonald JF, Orser BA. Tonically activated GABAA receptors in hippocampal neurons are high-affinity, low-conductance sensors for extracellular GABA. Molecular Pharmacology 2003 Jan;631:2-8. Tablets This pharmacology-related article is a stub. Retrieved from http://en..org/wiki/Gabazine Categories: Pharmacology stubs | Pharmacology | GABA antagonists Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page This page was last modified on 20 September 2007, at 11:2
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