MS-377 is a selective

antagonist An antagonist is a character in a story who is presented as the main enemy or rival of the protagonist and is often depicted as a villain.sigma-1 receptor The sigma-1 receptor (σ1R), one of two sigma receptor subtypes, is a Chaperone (protein), chaperone protein at the endoplasmic reticulum (ER) that modulates calcium signaling through the IP3 receptor. In humans, the σ1 receptor is encoded by ...

. It possesses

anti-psychotic Antipsychotics, previously known as neuroleptics and major tranquilizers, are a class of psychotropic medication primarily used to manage psychosis (including delusions, hallucinations, paranoia or disordered thought), principally in schizoph ...

properties.

Properties

MS-377 acts selectively at the sigma-1 receptor as an antagonist. It does not act on

dopamine Dopamine (DA, a contraction of 3,4-dihydroxyphenethylamine) is a neuromodulatory molecule that plays several important roles in cells. It is an organic chemical of the catecholamine and phenethylamine families. It is an amine synthesized ...

serotonin receptors 5-HT receptors, 5-hydroxytryptamine receptors, or serotonin receptors, are a group of G protein-coupled receptor and ligand-gated ion channels found in multiple tissues including the Central nervous system, central and peripheral nervous systems ...

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 Serotonin (), also known as 5-hydroxytryptamine (5-HT), is a monoamine neurotransmitter with a wide range of functions in both the central nervous system (CNS) and also peripheral tissues. It is involved in mood, cognition, reward, learning, ...

and

dopamine receptors Dopamine receptors are a class of G protein-coupled receptors that are prominent in the vertebrate central nervous system (CNS). Dopamine receptors activate different effectors through not only G-protein coupling, but also signaling through diff ...

, it still affects those

monoamine Monoamine neurotransmitters are neurotransmitters and neuromodulators that contain one amino group connected to an aromatic ring by a two-carbon chain (such as -CH2-CH2-). Examples are dopamine, norepinephrine and serotonin. All monoamines are ...

systems. It has been shown that MS-377 reduced the release of

and dopamine induced by PCP. It has also been shown to decrease

methamphetamine Methamphetamine (contracted from ) is a potent central nervous system (CNS) stimulant that is mainly used as a recreational drug use, recreational or Performance-enhancing substance, performance-enhancing drug and less commonly as a secon ...

behavioral sensitization, this is also observed with other

sigma antagonists Sigma ( ; uppercase Σ, lowercase σ, lowercase in word-final position ς; ) is the eighteenth letter of the Greek alphabet. In the system of Greek numerals, it has a value of 200. In general mathematics, uppercase Σ is used as an operato ...

References

{{Sigma receptor modulators Receptor antagonists Sigma receptor modulators Pyrrolidones Piperazines 4-Chlorophenyl compounds Methoxy compounds Ethanolamines