|Systematic (IUPAC) name|
|Mol. mass||330.401 g/mol|
SB-205,384 is a GABAA positive allosteric modulator, which binds preferentially to α3, α5, and α6 subunit containing subtypes. 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, with tests showing that it alters the firing of some populations of neurons while leaving others unaffected. Animal studies have shown it to produce both anxiolytic and anti-aggressive effects, but with little sedation or other behavioural changes.
- 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.
- 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".
- 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.
- 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.
- 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.
- 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.