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SB-205384

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(Redirected fromSB-205,384)
Chemical compound
Pharmaceutical compound
SB-205384
Legal status
Legal status
Identifiers
  • But-2-ynyl 4-amino-7-hydroxy-2-methyl-5,6,7,8-tetrahydro-[1]benzothiolo[3,2-e]pyridine-3-carboxylate
CAS Number
PubChemCID
ChemSpider
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC17H18N2O3S
Molar mass330.40 g·mol−1
3D model (JSmol)
  • CC#CCOC(=O)c1c(C)nc2sc3CC(O)CCc3c2c1N
  • 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) ☒N
  • Key:JDTZAGLGBRRCJT-UHFFFAOYSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

SB-205384 is ananxiolytic drug. It has similar effects tobenzodiazepine drugs, but is structurally distinct and so is classed as anonbenzodiazepine anxiolytic.

SB-205384 is aGABAApositive 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]

References

[edit]
  1. ^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.PMC 3781410.PMID 23902941.
  2. ^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.
  3. ^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.
  4. ^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.
  5. ^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.
  6. ^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.
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