Vabicaserin

Vabicaserin

Systematic (IUPAC) name
(9aR,12aS)-4,5,6,7,9,9a,10,11,12,12a-decahydrocyclopenta[c][1,4]diazepino[6,7,1-ij]quinoline
Clinical data
Legal status	Uncontrolled
Routes of administration	Oral
Identifiers
CAS Number	620948-34-7 Y
ATC code	none
PubChem	CID: 11521822
ChemSpider	9696609
UNII	WD9550HPNL Y
Chemical data
Formula	C15H21ClN2
Molecular mass	264.79 g/mol
SMILES C1C[C@H]2CN3CCNCC4=C3C(=CC=C4)[C@H]2C1
InChI InChI=1S/C15H20N2/c1-3-11-9-16-7-8-17-10-12-4-2-5-13(12)14(6-1)15(11)17/h1,3,6,12-13,16H,2,4-5,7-10H2/t12-,13-/m0/s1 Key:NPTIPEQJIDTVKR-STQMWFEESA-N
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Vabicaserin (SCA-136) was a novel antipsychotic and anorectic under development by Wyeth. As of 2010 it is no longer in clinical trials for the treatment of psychosis. It was also under investigation as an antidepressant but this indication appears to have been dropped as well.

Vabicaserin acts as a selective 5-HT_2C receptor full agonist (K_i = 3 nM; EC₅₀ = 8 nM; IA = 100% (relative to 5-HT)) and 5-HT_2B receptor antagonist (IC₅₀ = 29 nM). It is also a very weak antagonist at the 5-HT_2A receptor (IC₅₀ = 1,650 nM), though this action is not clinically significant. By activating 5-HT_2C receptors, vabicaserin inhibits dopamine release in the mesolimbic pathway, likely underlying its efficacy in alleviating positive symptoms of schizophrenia, and increases acetylcholine and glutamate levels in the prefrontal cortex, suggesting benefits against cognitive symptoms as well.

See also

• Lorcaserin