S32212

S32212

Clinical data
ATC code	None
Identifiers
IUPAC name N-[4-methoxy-3-(4-methylpiperazin-1-yl)phenyl]-1,2-dihydro-3H-benzo[e]indole-3-carboxamide
CAS Number	847968-58-5
PubChem CID	11384503
ChemSpider	9559416
CompTox Dashboard (EPA)	DTXSID201030313
Chemical and physical data
Formula	C25H28N4O2
Molar mass	416.525 g·mol^−1
3D model (JSmol)	Interactive image
SMILES O=C(N3c2ccc1c(cccc1)c2CC3)Nc4cc(c(OC)cc4)N5CCN(C)CC5
InChI InChI=1S/C25H28N4O2/c1-27-13-15-28(16-14-27)23-17-19(8-10-24(23)31-2)26-25(30)29-12-11-21-20-6-4-3-5-18(20)7-9-22(21)29/h3-10,17H,11-16H2,1-2H3,(H,26,30) Key:HNWBOBAUHUFDES-UHFFFAOYSA-N

S32212 is a drug which is under preclinical investigation as a potential antidepressant medicine.[1][2] It behaves as a selective, combined 5-HT_2C receptor inverse agonist and α₂-adrenergic receptor antagonist (at all three subtypes—α_2A, α_2B, and α_2C) with additional 5-HT_2A and, to a lesser extent, 5-HT_2B receptor antagonistic properties, and lacks any apparent affinity for the monoamine reuptake transporters or for the α₁-adrenergic, H₁, or mACh receptors.[1] This profile of activity is compatible with the definition of a noradrenergic and specific serotonergic antidepressant (NaSSA), and as such, S32212 could in turn be classified as a NaSSA.

In animal studies, S32212 raised BDNF concentrations in the hippocampus and amygdala, increased the firing rate of neurons in the adrenergic perikarya in the locus coeruleus, increased levels of norepinephrine in the frontal cortex and hippocampus, and elevated frontal cortex levels of dopamine and acetylcholine, though not of serotonin or histamine.[2] It produces effects indicative of antidepressant, anxiolytic, antiobsessional, antiaggressive, and cognitive- and sleep-enhancing properties in animal models, all while not perturbing body weight or sexual behavior.[2]

See also

• Noradrenergic and specific serotonergic antidepressant

References

1. Millan MJ, Mannoury la Cour C, Chanrion B, et al. (March 2012). "S32212, a novel serotonin type 2C receptor inverse agonist/α2-adrenoceptor antagonist and potential antidepressant: I. A mechanistic characterization". The Journal of Pharmacology and Experimental Therapeutics. 340 (3): 750–64. doi:10.1124/jpet.111.187468. PMID 22178752. S2CID 8546314.
2. Dekeyne A, Brocco M, Loiseau F, et al. (March 2012). "S32212, a novel serotonin type 2C receptor inverse agonist/α2-adrenoceptor antagonist and potential antidepressant: II. A behavioral, neurochemical, and electrophysiological characterization". The Journal of Pharmacology and Experimental Therapeutics. 340 (3): 765–80. doi:10.1124/jpet.111.187534. PMID 22178753. S2CID 11363664.