MS-377

MS-377 is a selective antagonist of the sigma-1 receptor. It possesses anti-psychotic properties.

Properties
MS-377 acts selectively at the sigma-1 receptor as an antagonist. It does not act on dopamine or serotonin receptors unlike most anti-psychotics. Tests have shown that MS-377 could displace ligand binding from the sigma-1 receptor, but did this not happen at the sigma-2, 5-HT2 and D2 receptors, suggesting that it is selective for the sigma-1 receptor.

Despite not acting at serotonin and dopamine receptors, it still affects those monoamine systems. It has been shown that MS-377 reduced the release of serotonin and dopamine induced by PCP. It has also been shown to decrease methamphetamine behavioral sensitization, this is also observed with other sigma antagonists.