Gabazine (SR-95531) is a drug that acts as an antagonist at GABAAreceptors. 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]
Gabazine has been found to bind to and antagonize α4βδ subunit-containing GABAA receptors, which may represent the GHB receptor.[4]
Referencesedit
^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.
^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. PMC6573228. PMID 8987785.
^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.
^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. PMC3421209. PMID 22753476.
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gabazine, 95531, drug, that, acts, antagonist, gabaa, receptors, used, scientific, research, role, medicine, would, expected, produce, convulsions, used, humans, bromideclinical, dataatc, codenoneidentifiersiupac, name, carboxypropyl, methoxyphenyl, dihydropyr. 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 GabazineGabazine bromideClinical dataATC codenoneIdentifiersIUPAC name 2 3 carboxypropyl 6 4 methoxyphenyl 2 3 dihydropyridazin 3 iminium bromideCAS Number104104 50 9 YPubChem CID107895ChemSpider4925141 YUNII99460MG420ChEMBLChEMBL303580 YCompTox Dashboard EPA DTXSID40908798Chemical and physical dataFormulaC 15H 18Br N 3O 3Molar mass368 231 g mol 13D model JSmol Interactive imageSMILES Br C O O CCCN1N C C CC1 NH2 C1 CC C C C1 OCInChI 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 YKey GFZHNFOGCMEYTA UHFFFAOYSA N Y verify 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 Gabazine has been found to bind to and antagonize a4bd subunit containing GABAA receptors which may represent the GHB receptor 4 References edit 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 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 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 Absalom N Eghorn LF Villumsen IS Karim N Bay T Olsen JV et al August 2012 a4bd GABA A receptors are high affinity targets for g 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 nbsp This drug article relating to the nervous system is a stub You can help Wikipedia by expanding it vte Retrieved from https en wikipedia org w index php title Gabazine amp oldid 1215442870, wikipedia, wiki, book, books, library,
