MRS8209

MRS8209

Identifiers
IUPAC name 4-[6-(cyclopentylamino)-2-iodopurin-9-yl]-2,3-dihydroxybicyclo[3.1.0]hexane-1-carbonitrile
Chemical and physical data
Formula	C17H19IN6O2
Molar mass	466.283 g·mol−1
3D model (JSmol)	Interactive image
SMILES O[C@H]1[C@@H](O)[C@@H]([C@H]2C[C@]21C#N)n1cnc2c1nc(I)nc2NC1CCCC1

MRS8209 is an experimental drug which acts as a potent, peripherally selective 5-HT_2B receptor antagonist with high selectivity over other serotonin receptor subtypes. It has been investigated for possible applications in the treatment of heart and lung fibrosis and intestinal or vascular conditions mediated by 5-HT_2B, while sparing 5-HT_2B mediated activity in the brain. ^[1]

References

1. Tosh DK, Pavan M, Clark AA, Lammers J, Villano S, Marri S, Sgambellone S, Choi S, Lee J, Ivancich MS, Bock HA, Campbell RG, Lewicki SA, Levitan IM, Chen E, Liu N, Demby T, Gavrilova O, Gao ZG, Lucarini L, McCorvy JD, Jacobson KA. Potent and Selective Human 5-HT2B Serotonin Receptor Antagonists: 4'-Cyano-(N)-methanocarba-adenosines by Synthetic Serendipity. J Med Chem. 2024 Dec 12;67(23):21264-21291. doi : 10.1021/acs.jmedchem.4c02174 PMID   39589936