2H-Benzimidazol-2-one, 1-[4-(3,4-dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)butyl]-1,3-dihydro-3-methyl-

Biological Activity

CM398 is a highly selective, orally active sigma-2 receptor ligand (Ki=0.43 nM), with high sigma-1/sigma-2 selectivity rato (1000-fold). CM398 shows notable affinity for dopamine (Ki=32.90 nM) and serotonin transporters (Ki=244.2 nM). CM398 shows promising anti-inflammatory analgesic effects in the formalin model of inflammatory pain in mice[1].

References

[1]. Intagliata S, et al. Discovery of a Highly Selective Sigma-2 Receptor Ligand, 1-(4-(6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)butyl)-3-methyl-1H-benzo[d]imidazol-2(3H)-one (CM398), with Drug-Like Properties and Antinociceptive Effects In Vivo. AAPS J. 2020;22(5):94. Published 2020 Jul 20.