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SB-205,384: Wikis

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SB-205,384
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
Identifiers
CAS number 160296-13-9
ATC code  ?
PubChem 197690
Chemical data
Formula C 17H18N2O3S 
Mol. mass 330.401 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status Investigational New Drug
Routes  ?

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 subtype selective GABAA partial agonist, which binds preferentially to the α3 subtype.[1] 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,[2] with tests showing that it alters the firing of some populations of neurons while leaving others unaffected.[3] Animal studies have shown it to produce both anxiolytic and anti-aggressive effects, but with little sedation or other behavioural changes.[4][5]

References

  1. ^ Meadows HJ, Kumar CS, Pritchett DB, Blackburn TP, Benham CD. SB-205384: a GABA(A) receptor modulator with novel mechanism of action that shows subunit selectivity. British Journal of Pharmacology. 1998 Mar;123(6):1253-9. PMID 9559912
  2. ^ Meadows HJ, Harries MH, Thompson M, Benham CD. Effect of SB-205384 on the decay of GABA-activated chloride currents in granule cells cultured from rat cerebellum. British Journal of Pharmacology. 1997 Aug;121(7):1334-8. PMID 9257911
  3. ^ Ing T, Poulter MO. Diversity of GABA(A) receptor synaptic currents on individual pyramidal cortical neurons. European Journal of Neuroscience. 2007 Feb;25(3):723-34. PMID 17313570
  4. ^ Navarro JF, Burón E, Martín-López M. Anxiolytic-like activity of SB-205384 in the elevated plus-maze test in mice. Psicothema. 2006 Feb;18(1):100-4. PMID 17296016
  5. ^ Navarro JF, Burón E, Martín-López M. Effects of SB-205384, a positive modulator of alpha3-subunit-containing GABA-A receptors, on isolation-induced aggression in male mice. Psicothema. 2008 Feb;20(1):144-7. PMID 18206077
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