AC927 or 1-(2-phenylethyl)piperidine is a selective sigma receptor

antagonist An antagonist is a character in a story who is presented as the chief foe of the protagonist. Etymology The English word antagonist comes from the Greek ἀνταγωνιστής – ''antagonistēs'', "opponent, competitor, villain, enemy, riv ...

, with reported

binding affinity In biochemistry and pharmacology, a ligand is a substance that forms a complex with a biomolecule to serve a biological purpose. The etymology stems from ''ligare'', which means 'to bind'. In protein-ligand binding, the ligand is usually a mol ...

of ''K''_i = 30 ± 2 nM for the sigma-1 receptor and ''K''_i = 138 ± 18 nM for the

sigma-2 receptor The sigma-2 receptor (σ2R) is a sigma receptor subtype that has attracted attention due to its involvement in diseases such as cancer and neurological diseases. It is currently under investigation for its potential diagnostic and therapeutic use ...

, and negligible binding affinity for other major

central nervous system The central nervous system (CNS) is the part of the nervous system consisting primarily of the brain and spinal cord. The CNS is so named because the brain integrates the received information and coordinates and influences the activity of all par ...

receptors, transporters, and ion channels. AC927 is reported to attenuate the locomotor stimulation induced by methamphetamine in mice.

References

{{Sigma receptor modulators 1-Piperidinyl compounds Phenyl compounds