SB-205384 is a GABAApositive 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]
^Ing T, Poulter MO (February 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. PMID17313570. S2CID9361003.
^Navarro JF, Burón E, Martín-López M (February 2006). "Anxiolytic-like activity of SB-205384 in the elevated plus-maze test in mice". Psicothema. 18 (1): 100–4. PMID17296016.
^Navarro JF, Burón E, Martín-López M (February 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. PMID18206077.
