S 32212 (hydrochloride)

S 32212 is an inverse agonist of the serotonin (5-HT) receptor subtypes 5-HT_2CINI and 5-HT_2CVSV (K_is = 6.6 and 8.9 nM, respectively).¹ It is also an antagonist of the 5-HT_2A receptor and the α_2B-adrenergic receptor (K_i = 5.8 nM for both). S 32212 is greater than 70-fold selective for these receptors in a panel of 80 receptors, enzymes, and ion channels. S 32212 reduces binding of GTPγS to Gα_q and decreases the activity of phospholipase C (PLC) in HEK293 cells expressing 5-HT_2CINI receptors (EC₅₀s = 38 and 18.6 nM, respectively) and in CHO cells expressing 5-HT_2CVSV receptors (EC₅₀s = 38 and 18.6 nM, respectively). S 32212 (2.5 mg/kg) decreases head twitching, penile erections, and drug discrimination induced by 5-HT receptor agonists in mice and rats. It reduces immobility time in the forced swim test and decreases marble burying in mice and rats when administered at doses of 10 and 40 mg/kg, indicating anti-depressant-like and anxiolytic activities.^1,2

WARNING This product is not for human or veterinary use.

1. Millan, M.J., Mannoury la Cour, C., Chanrion, B., et al. S32212, a novel serotonin type ²C receptor inverse agonist/α2-adrenoceptor antagonist and potential antidepressant: I. A mechanistic characterization. J. Pharmacol. Exp. Ther. 340(3), 750-764 (2012).

2. Dekeyne, A., Brocco, M., Loiseau, F., et al. S32212, a novel serotonin type ²C receptor inverse agonist/α2-adrenoceptor antagonist and potential antidepressant: II. A behavioral, neurochemical, and electrophysiological characterization. J. Pharmacol. Exp. Ther. 340(3), 765-780 (2012).