SN79 is a potent, orally active sigma receptor antagonist with Ki of 27 and 7 nM for σ1 and σ2, respectively.
SN79 also exhibits moderate affinity for serotonin transporters and norepinephrine transporters, displays a moderate affinity for 5-HT2 receptors and negligible affinity, does not inhibit major cytochrome P450 enzymes.
SN79 significantly attenuates cocaine-induced convulsions and locomotor activity in mice, also significantly attenuates the development and expression of the sensitized response to repeated cocaine exposures.
