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. 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.
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- ^ 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. doi:10.1038/sj.bjp.0701251. PMC 1564816. PMID 9257911.
- ^ 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. doi:10.1111/j.1460-9568.2007.05331.x. PMID 17313570.
- ^ 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.
- ^ 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.