^Donevan, S.D; Rogawski, M.A (1998). "Allosteric regulation of α-amino-3-hydroxy-5-methyl-4-isoxazole-propionate receptors by thiocyanate and cyclothiazide at a common modulatory site distinct from that of 2,3-benzodiazepines". Neuroscience. 87 (3): 615–629. doi:10.1016/s0306-4522(98)00109-2. PMID 9758228. S2CID 14817743.
^Donevan, Sean D.; Rogawski, Michael A. (1993). "GYKI 52466, a 2,3-benzodiazepine, is a highly selective, noncompetitive antagonist of AMPA/Kainate receptor responses". Neuron. 10 (1): 51–59. doi:10.1016/0896-6273(93)90241-i. PMID 7678966. S2CID 16011527.
^Tarnawa, István; Farkas, Sándor; Berzsenyi, Pál; Pataki, Ágnes; Andrási, Ferenc (1989). "Electrophysiological studies with a 2,3-benzodiazepine muscle relaxant: GYKI 52466". European Journal of Pharmacology. 167 (2): 193–199. doi:10.1016/0014-2999(89)90579-7. PMID 2574112.
^Rzeski, W.; Turski, L.; Ikonomidou, C. (2001). "Glutamate antagonists limit tumor growth". Proceedings of the National Academy of Sciences. 98 (11): 6372–6377. doi:10.1073/pnas.091113598. PMC33475. PMID 11331750.
^Paternain, Ana V.; Morales, Miguel; Lerma, Juan (1995). "Selective antagonism of AMPA receptors unmasks kainate receptor-mediated responses in hippocampal neurons". Neuron. 14 (1): 185–189. doi:10.1016/0896-6273(95)90253-8. PMID 7826635. S2CID 6037517.
^Szabados, Tamás; Gigler, Gábor; Gacsályi, István; Gyertyán, István; Lévay, György (2001). "Comparison of anticonvulsive and acute neuroprotective activity of three 2,3-benzodiazepine compounds, GYKI 52466, GYKI 53405, and GYKI 53655". Brain Research Bulletin. 55 (3): 387–391. doi:10.1016/s0361-9230(01)00516-0. PMID 11489346. S2CID 23142293.
January 01, 1970
gyki, 52466, benzodiazepine, that, acts, ionotropic, glutamate, receptor, antagonist, which, competitive, ampa, receptor, antagonist, ic50, values, ampa, kainate, nmda, induced, responses, respectively, orally, active, anticonvulsant, skeletal, muscle, relaxan. GYKI 52466 is a 2 3 benzodiazepine that acts as an ionotropic glutamate receptor antagonist which is a non competitive AMPA receptor antagonist IC50 values are 10 20 450 and gt gt 50 mM for AMPA kainate and NMDA induced responses respectively orally active anticonvulsant and skeletal muscle relaxant 1 2 3 4 Unlike conventional 1 4 benzodiazepines GYKI 52466 and related 2 3 benzodiazepines do not act on GABAA receptors 5 Like other AMPA receptor antagonists GYKI 52466 has anticonvulsant and neuroprotective properties 6 GYKI 52466 Names Preferred IUPAC name 4 8 Methyl 2H 9H 1 3 dioxolo 4 5 h 2 3 benzodiazepin 5 yl aniline Identifiers CAS Number 102771 26 6 Y192065 56 8 HCl salt N 3D model JSmol Interactive image ChEBI CHEBI 79560 N ChEMBL ChEMBL275006 N ChemSpider 3417 N ECHA InfoCard 100 162 378 IUPHAR BPS 4210 KEGG C15040 N PubChem CID 3538 UNII 471V8NZ5X3 N CompTox Dashboard EPA DTXSID40145500 InChI InChI 1S C17H15N3O2 c1 10 6 12 7 15 16 22 9 21 15 8 14 12 17 20 19 10 11 2 4 13 18 5 3 11 h2 5 7 8H 6 9 18H2 1H3 NKey LFBZZHVSGAHQPP UHFFFAOYSA N NInChI 1 C17H15N3O2 c1 10 6 12 7 15 16 22 9 21 15 8 14 12 17 20 19 10 11 2 4 13 18 5 3 11 h2 5 7 8H 6 9 18H2 1H3Key LFBZZHVSGAHQPP UHFFFAOYAH SMILES CC1 NN C C2 CC3 C C C2C1 OCO3 C4 CC C C C4 N Properties Chemical formula C 17H 15N 3O 2 Molar mass 293 326 g mol 1 Appearance Yellow solid HCl salt Density 1 393 g cm3 Solubility in water gt 10 mg mL HCl salt Except where otherwise noted data are given for materials in their standard state at 25 C 77 F 100 kPa N verify what is Y N Infobox referencesSee also editGYKI 52895 another 2 3 benzodiazepine with other than GABAergic function Tifluadom LufuradomReferences edit Donevan S D Rogawski M A 1998 Allosteric regulation of a amino 3 hydroxy 5 methyl 4 isoxazole propionate receptors by thiocyanate and cyclothiazide at a common modulatory site distinct from that of 2 3 benzodiazepines Neuroscience 87 3 615 629 doi 10 1016 s0306 4522 98 00109 2 PMID 9758228 S2CID 14817743 Donevan Sean D Rogawski Michael A 1993 GYKI 52466 a 2 3 benzodiazepine is a highly selective noncompetitive antagonist of AMPA Kainate receptor responses Neuron 10 1 51 59 doi 10 1016 0896 6273 93 90241 i PMID 7678966 S2CID 16011527 Tarnawa Istvan Farkas Sandor Berzsenyi Pal Pataki Agnes Andrasi Ferenc 1989 Electrophysiological studies with a 2 3 benzodiazepine muscle relaxant GYKI 52466 European Journal of Pharmacology 167 2 193 199 doi 10 1016 0014 2999 89 90579 7 PMID 2574112 Rzeski W Turski L Ikonomidou C 2001 Glutamate antagonists limit tumor growth Proceedings of the National Academy of Sciences 98 11 6372 6377 doi 10 1073 pnas 091113598 PMC 33475 PMID 11331750 Paternain Ana V Morales Miguel Lerma Juan 1995 Selective antagonism of AMPA receptors unmasks kainate receptor mediated responses in hippocampal neurons Neuron 14 1 185 189 doi 10 1016 0896 6273 95 90253 8 PMID 7826635 S2CID 6037517 Szabados Tamas Gigler Gabor Gacsalyi Istvan Gyertyan Istvan Levay Gyorgy 2001 Comparison of anticonvulsive and acute neuroprotective activity of three 2 3 benzodiazepine compounds GYKI 52466 GYKI 53405 and GYKI 53655 Brain Research Bulletin 55 3 387 391 doi 10 1016 s0361 9230 01 00516 0 PMID 11489346 S2CID 23142293 Retrieved from https en wikipedia org w index php title GYKI 52466 amp oldid 1095880342, wikipedia, wiki, book, books, library,
