SB-205384 explained

SB-205384 is an anxiolytic drug. It has similar effects to benzodiazepine drugs, but is structurally distinct and so is classed as a nonbenzodiazepine anxiolytic.

SB-205384 is a GABA_A positive 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]}

Notes and References

1. Heidelberg LS, Warren JW, Fisher JL . 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 . The Journal of Pharmacology and Experimental Therapeutics . 347 . 1 . 235–41 . October 2013 . 23902941 . 3781410 . 10.1124/jpet.113.207324 .
2. 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 . 123 . 6 . 1253–9 . March 1998 . 9559912 . 1565273 . 10.1038/sj.bjp.0701721 .
3. 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 . 121 . 7 . 1334–8 . August 1997 . 9257911 . 1564816 . 10.1038/sj.bjp.0701251 .
4. Ing T, Poulter MO . Diversity of GABA(A) receptor synaptic currents on individual pyramidal cortical neurons . The European Journal of Neuroscience . 25 . 3 . 723–34 . February 2007 . 17313570 . 10.1111/j.1460-9568.2007.05331.x . 9361003 .
5. Navarro JF, Burón E, Martín-López M . Anxiolytic-like activity of SB-205384 in the elevated plus-maze test in mice . Psicothema . 18 . 1 . 100–4 . February 2006 . 17296016 .
6. 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 . 20 . 1 . 144–7 . February 2008 . 18206077 .