SB-205,384

drugbox
IUPAC_name = but-2-ynyl 4-amino-7-hydroxy-2-methyl-5,6,7,8-tetrahydro- [1] benzothiolo [3,2-e] pyridine-3-carboxylate

---

width = 250
CAS_number = 160296-13-9
ATC_prefix =
ATC_suffix =
PubChem = 197690
DrugBank =
C=17|H=18|N=2|O=3|S=1
molecular_weight = 330.401 g/mol
smiles = CC#CCOC(=O)c1c(C)nc2sc3CC(O)CCc3c2c1N
bioavailability =
protein_bound =
metabolism =
elimination_half-life =
excretion =
pregnancy_AU =
pregnancy_US =
pregnancy_category=
legal_AU =
legal_CA =
legal_UK =
legal_US =
legal_status = Investigational New Drug
routes_of_administration =

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

References