MS-377
{{Short description|Sigma-1 receptor antagonist}}
{{Chembox
| Reference = {{cite web | url=https://pubchem.ncbi.nlm.nih.gov/compound/9892249 | title=MS-377 free base }}{{cite web | url=https://pubchem.ncbi.nlm.nih.gov/compound/9892248 | title=Xj9U35H4R3 }}
| ImageFile = MS-377.svg
| IUPACName = (3R)-1-(4-Chlorophenyl)-3-
| Section1 = {{Chembox Identifiers
| CASNo = 206862-30-8
| CASNo_Comment = (free base)
| CASNo1 = 206862-48-8
| CASNo1_Comment = (L-tartrate)
| ChemSpiderID = 4095365
| PubChem = 9892249
| SMILES = COCCN1CCN(CC1)C[C@H]2CCN(C2=O)C3=CC=C(C=C3)Cl
| InChI = 1S/C18H26ClN3O2/c1-24-13-12-20-8-10-21(11-9-20)14-15-6-7-22(18(15)23)17-4-2-16(19)3-5-17/h2-5,15H,6-14H2,1H3/t15-/m1/s1
| InChIKey = DKVVPXLIRYCKCS-OAHLLOKOSA-N
}}
| Section2 = {{Chembox Properties
|C=18 |H=26 |Cl=1 |N=3 |O=2
}}
}}
MS-377 is a selective antagonist of the sigma-1 receptor.{{Cite web |title=Drug Information {{!}} Therapeutic Target Database |url=https://idrblab.net/ttd/data/drug/details/D09OTG |access-date=2024-02-16 |website=idrblab.net |language=en}} 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.{{Cite journal |last1=Takahashi |first1=S. |last2=Sonehara |first2=K. |last3=Takagi |first3=K. |last4=Miwa |first4=T. |last5=Horikomi |first5=K. |last6=Mita |first6=N. |last7=Nagase |first7=H. |last8=Iizuka |first8=K. |last9=Sakai |first9=K. |date=August 1999 |title=Pharmacological profile of MS-377, a novel antipsychotic agent with selective affinity for sigma receptors |url=https://pubmed.ncbi.nlm.nih.gov/10494578/ |journal=Psychopharmacology |volume=145 |issue=3 |pages=295–302 |doi=10.1007/s002130051061 |issn=0033-3158 |pmid=10494578|s2cid=12904841 }}
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.{{Cite journal |last1=Takahashi |first1=S. |last2=Horikomi |first2=K. |last3=Kato |first3=T. |date=2001-09-21 |title=MS-377, a novel selective sigma(1) receptor ligand, reverses phencyclidine-induced release of dopamine and serotonin in rat brain |url=https://pubmed.ncbi.nlm.nih.gov/11567651/ |journal=European Journal of Pharmacology |volume=427 |issue=3 |pages=211–219 |doi=10.1016/s0014-2999(01)01254-7 |issn=0014-2999 |pmid=11567651}} It has also been shown to decrease methamphetamine behavioral sensitization,{{Cite journal |last1=Takahashi |first1=S. |last2=Miwa |first2=T. |last3=Horikomi |first3=K. |date=2000-07-28 |title=Involvement of sigma 1 receptors in methamphetamine-induced behavioral sensitization in rats |url=https://pubmed.ncbi.nlm.nih.gov/10899399/ |journal=Neuroscience Letters |volume=289 |issue=1 |pages=21–24 |doi=10.1016/s0304-3940(00)01258-1 |issn=0304-3940 |pmid=10899399|s2cid=54420748 }} this is also observed with other sigma antagonists.{{Cite journal |last1=Ujike |first1=H. |last2=Kanzaki |first2=A. |last3=Okumura |first3=K. |last4=Akiyama |first4=K. |last5=Otsuki |first5=S. |date=1992 |title=Sigma (sigma) antagonist BMY 14802 prevents methamphetamine-induced sensitization |url=https://pubmed.ncbi.nlm.nih.gov/1313134/ |journal=Life Sciences |volume=50 |issue=16 |pages=PL129–134 |doi=10.1016/0024-3205(92)90466-3 |issn=0024-3205 |pmid=1313134}}
References
{{Reflist}}
{{Sigma receptor modulators}}
Category:Sigma receptor modulators