SB-205384 is a GABAApositive allosteric modulator, which binds preferentially to α3, α5, and α6 subunit containing subtypes.[1][2] It has a novel mechanism of action, prolonging the duration of GABA-mediated chloride flux but without increasing the intensity of the response, and this may give it an unusual pharmacological profile,[3] with tests showing that it alters the firing of some populations of neurons while leaving others unaffected.[4] Animal studies have shown it to produce both anxiolytic and anti-aggressive effects, but with little sedation or other behavioural changes.[5][6]
Referencesedit
^Heidelberg LS, Warren JW, Fisher JL (October 2013). "SB-205384 is a positive allosteric modulator of recombinant GABAA receptors containing rat α3, α5, or α6 subunit subtypes coexpressed with β3 and γ2 subunits". The Journal of Pharmacology and Experimental Therapeutics. 347 (1): 235–41. doi:10.1124/jpet.113.207324. PMC3781410. PMID 23902941.
^Meadows HJ, Kumar CS, Pritchett DB, Blackburn TP, Benham CD (March 1998). "SB-205384: a GABA(A) receptor modulator with novel mechanism of action that shows subunit selectivity". British Journal of Pharmacology. 123 (6): 1253–9. doi:10.1038/sj.bjp.0701721. PMC1565273. PMID 9559912.
^Meadows HJ, Harries MH, Thompson M, Benham CD (August 1997). "Effect of SB-205384 on the decay of GABA-activated chloride currents in granule cells cultured from rat cerebellum". British Journal of Pharmacology. 121 (7): 1334–8. doi:10.1038/sj.bjp.0701251. PMC1564816. PMID 9257911.
^Ing T, Poulter MO (February 2007). "Diversity of GABA(A) receptor synaptic currents on individual pyramidal cortical neurons". The European Journal of Neuroscience. 25 (3): 723–34. doi:10.1111/j.1460-9568.2007.05331.x. PMID 17313570. S2CID 9361003.
^Navarro JF, Burón E, Martín-López M (February 2006). "Anxiolytic-like activity of SB-205384 in the elevated plus-maze test in mice". Psicothema. 18 (1): 100–4. PMID 17296016.
^Navarro JF, Burón E, Martín-López M (February 2008). "Effects of SB-205384, a positive modulator of alpha3-subunit-containing GABA-A receptors, on isolation-induced aggression in male mice". Psicothema. 20 (1): 144–7. PMID 18206077.
This article about an anxiolytic is a stub. You can help Wikipedia by expanding it.
205384, anxiolytic, drug, similar, effects, benzodiazepine, drugs, structurally, distinct, classed, nonbenzodiazepine, anxiolytic, legal, statuslegal, statusus, investigational, drugidentifiersiupac, name, ynyl, amino, hydroxy, methyl, tetrahydro, benzothiolo,. SB 205384 is an anxiolytic drug It has similar effects to benzodiazepine drugs but is structurally distinct and so is classed as a nonbenzodiazepine anxiolytic SB 205384Legal statusLegal statusUS Investigational New DrugIdentifiersIUPAC name But 2 ynyl 4 amino 7 hydroxy 2 methyl 5 6 7 8 tetrahydro 1 benzothiolo 3 2 e pyridine 3 carboxylateCAS Number160296 13 9 YPubChem CID197690ChemSpider171116 NCompTox Dashboard EPA DTXSID00936259Chemical and physical dataFormulaC 17H 18N 2O 3SMolar mass330 40 g mol 13D model JSmol Interactive imageSMILES CC CCOC O c1c C nc2sc3CC O CCc3c2c1NInChI InChI 1S C17H18N2O3S c1 3 4 7 22 17 21 13 9 2 19 16 14 15 13 18 11 6 5 10 20 8 12 11 23 16 h10 20H 5 8H2 1 2H3 H2 18 19 NKey JDTZAGLGBRRCJT UHFFFAOYSA N N N Y what is this verify SB 205384 is a GABAA positive allosteric modulator which binds preferentially to a3 a5 and a6 subunit containing subtypes 1 2 It has a novel mechanism of action prolonging the duration of GABA mediated chloride flux but without increasing the intensity of the response and this may give it an unusual pharmacological profile 3 with tests showing that it alters the firing of some populations of neurons while leaving others unaffected 4 Animal studies have shown it to produce both anxiolytic and anti aggressive effects but with little sedation or other behavioural changes 5 6 References edit Heidelberg LS Warren JW Fisher JL October 2013 SB 205384 is a positive allosteric modulator of recombinant GABAA receptors containing rat a3 a5 or a6 subunit subtypes coexpressed with b3 and g2 subunits The Journal of Pharmacology and Experimental Therapeutics 347 1 235 41 doi 10 1124 jpet 113 207324 PMC 3781410 PMID 23902941 Meadows HJ Kumar CS Pritchett DB Blackburn TP Benham CD March 1998 SB 205384 a GABA A receptor modulator with novel mechanism of action that shows subunit selectivity British Journal of Pharmacology 123 6 1253 9 doi 10 1038 sj bjp 0701721 PMC 1565273 PMID 9559912 Meadows HJ Harries MH Thompson M Benham CD August 1997 Effect of SB 205384 on the decay of GABA activated chloride currents in granule cells cultured from rat cerebellum British Journal of Pharmacology 121 7 1334 8 doi 10 1038 sj bjp 0701251 PMC 1564816 PMID 9257911 Ing T Poulter MO February 2007 Diversity of GABA A receptor synaptic currents on individual pyramidal cortical neurons The European Journal of Neuroscience 25 3 723 34 doi 10 1111 j 1460 9568 2007 05331 x PMID 17313570 S2CID 9361003 Navarro JF Buron E Martin Lopez M February 2006 Anxiolytic like activity of SB 205384 in the elevated plus maze test in mice Psicothema 18 1 100 4 PMID 17296016 Navarro JF Buron E Martin Lopez M February 2008 Effects of SB 205384 a positive modulator of alpha3 subunit containing GABA A receptors on isolation induced aggression in male mice Psicothema 20 1 144 7 PMID 18206077 nbsp This article about an anxiolytic is a stub You can help Wikipedia by expanding it vte Retrieved from https en wikipedia org w index php title SB 205384 amp oldid 1135083390, wikipedia, wiki, book, books, library,
