RS-102221

RS-102221 is a drug developed by Hoffmann–La Roche, which was one of the first compounds discovered that acts as a potent and selective antagonist at the serotonin 5-HT_2C receptor, with around 100× selectivity over the closely related 5-HT_2A and 5-HT_2B receptors.^[1] It has anxiolytic effects in animal studies,^[2] increases the effectiveness of SSRI antidepressants,^[3] and shows a complex interaction with cocaine, increasing some effects but decreasing others, reflecting a role for the 5-HT_2C receptor in regulation of the dopamine signalling system in the brain.^[4][5][6][7]

RS-102221

Clinical data
Other names	RS-102,221; 8-[5-(2,4-Dimethoxy-5-(4-trifluoromethylphenylsulphonamido)phenyl -5-oxopentyl]-1,3,8-triazaspiro[4.5]decane-2,4-dione
Identifiers
IUPAC name N-{5-[5-(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)pentanoyl] -2,4-dimethoxyphenyl}-4-(trifluoromethyl)benzenesulfonamide
CAS Number	185376-97-0 Y
PubChem CID	3693566
IUPHAR/BPS	187
ChemSpider	2925610
UNII	48D22QR8GY
ChEMBL	ChEMBL88402 N
CompTox Dashboard (EPA)	DTXSID801028164
Chemical and physical data
Formula	C27H33F3N4O7S
Molar mass	614.64 g·mol−1
3D model (JSmol)	Interactive image
SMILES c4cc(C(F)(F)F)ccc4S(=O)(=O)Nc(c(OC)cc2OC)cc2C(=O)CCCCN(CC3)CCC13NC(=O)NC1=O
InChI InChI=1S/C27H31F3N4O7S/c1-40-22-16-23(41-2)20(33-42(38,39)18-8-6-17(7-9-18)27(28,29)30)15-19(22)21(35)5-3-4-12-34-13-10-26(11-14-34)24(36)31-25(37)32-26/h6-9,15-16,33H,3-5,10-14H2,1-2H3,(H2,31,32,36,37) Key:HZZZZODVDSHQRG-UHFFFAOYSA-N
NY (what is this?)  (verify)

See also

• CEPC
• SB-242084
• Hydantoin