In vitro study | [ 3 H]Carabersat ([ 3 H]SB 204269) binds to rat forebrain membranes with moderate affinity (K d 40 nM) and pK i values of 7.3. Carabersat is able to bind to mouse forebrain membranes, and the binding is saturable and stereospecific, with a K d of 53 nM. The labelled [ 3 H]Carabersat produces a K d of 32 nM. Carabersat (SB-204269, 1-100 μM) has no effect on Na + current in cultured hippocampal neurones. Carabersat also shows no effect on action potential discharges evoked by elevating external K + . Carabersat (SB-204269) is structurally-related to the benzopyran ATP-sensitive potassium channel (KATP) opener, cromakalim, but has opposite stereochemistry, and the mechanism of action of Carabersat is not thought to involve KATP. |