Vabicaserin

Vabicaserin (codenamed SCA-136) was a novel antipsychotic and anorectic under development by Wyeth.^[1] As of 2010 it is no longer in clinical trials for the treatment of psychosis.^[1][2] It was also under investigation as an antidepressant but this indication appears to have been dropped as well.^[3]

Vabicaserin

Clinical data
Routes of administration	By mouth
ATC code	None
Legal status
Legal status	In general: uncontrolled
Identifiers
IUPAC name (9aR,12aS)-4,5,6,7,9,9a,10,11,12,12a-Decahydrocyclopenta[c][1,4]diazepino[6,7,1-ij]quinoline
CAS Number	887258-95-9 Y
PubChem CID	11521822
ChemSpider	9696609 N
UNII	WD9550HPNL
CompTox Dashboard (EPA)	DTXSID601336565 DTXSID80977680, DTXSID601336565
Chemical and physical data
Formula	C15H21ClN2
Molar mass	264.80 g·mol−1
3D model (JSmol)	Interactive image
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 N Key:NPTIPEQJIDTVKR-STQMWFEESA-N N
NY (what is this?)  (verify)

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).^[4][5][6] It is also a very weak antagonist at the 5-HT_2A receptor (IC₅₀ = 1,650 nM), though this action is not clinically significant.^[4] 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.^[6][7][8]

See also

• Bexicaserin
• BMB-101
• Lorcaserin
• WAY-163909