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Open Access Articles- Top Results for SB-205,384

SB-205,384

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SB-205,384
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Systematic (IUPAC) name
but-2-ynyl 4-amino-7-hydroxy-2-methyl-5,6,7,8-tetrahydro-[1]benzothiolo[3,2-e]pyridine-3-carboxylate
Clinical data
  • Investigational New Drug
Identifiers
160296-13-9 7pxY
PubChem CID 197690
Chemical data
Formula C17H18N2O3S
330.401 g/mol
 14pxY (what is this?)  (verify)

SB-205,384 is an anxiolytic drug. It has similar effects to benzodiazepine drugs, but is structurally distinct and so is classed as a nonbenzodiazepine anxiolytic.

SB-205,384 is a GABAA positive 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

  1. Heidelberg LS, Warren JW, Fisher JL (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". J. Pharmacol. Exp. Ther. 347 (1): 235–41. PMID 23902941. doi:10.1124/jpet.113.207324. 
  2. Meadows, HJ; Kumar, CS; Pritchett, DB; Blackburn, TP; Benham, CD (1998). "SB-205384: a GABAA receptor modulator with novel mechanism of action that shows subunit selectivity". British Journal of Pharmacology 123 (6): 1253–9. PMC 1565273. PMID 9559912. doi:10.1038/sj.bjp.0701721. 
  3. Meadows, HJ; Harries, MH; Thompson, M; Benham, CD (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. PMC 1564816. PMID 9257911. doi:10.1038/sj.bjp.0701251. 
  4. Ing, T; Poulter, MO (2007). "Diversity of GABA(A) receptor synaptic currents on individual pyramidal cortical neurons". The European Journal of Neuroscience 25 (3): 723–34. PMID 17313570. doi:10.1111/j.1460-9568.2007.05331.x. 
  5. Navarro, JF; Burón, E; Martín-López, M (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 (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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