MS-377
Names | |
---|---|
IUPAC name (3R)-1-(4-Chlorophenyl)-3-[[4-(2-methoxyethyl)piperazin-1-yl]methyl]pyrrolidin-2-one | |
Identifiers | |
CAS Number |
|
3D model (JSmol) |
|
ChemSpider |
|
PubChem CID |
|
InChI
| |
| |
Properties | |
Chemical formula | C18H26ClN3O2 |
Molar mass | 351.88 g·mol−1 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). Infobox references |
MS-377 is a selective antagonist of the sigma-1 receptor.[3] 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.[4]
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.[5] It has also been shown to decrease methamphetamine behavioral sensitization,[6] this is also observed with other sigma antagonists.[7]
References
- ^ "MS-377 free base".
- ^ "Xj9U35H4R3".
- ^ "Drug Information | Therapeutic Target Database". idrblab.net. Retrieved 2024-02-16.
- ^ Takahashi, S.; Sonehara, K.; Takagi, K.; Miwa, T.; Horikomi, K.; Mita, N.; Nagase, H.; Iizuka, K.; Sakai, K. (August 1999). "Pharmacological profile of MS-377, a novel antipsychotic agent with selective affinity for sigma receptors". Psychopharmacology. 145 (3): 295–302. doi:10.1007/s002130051061. ISSN 0033-3158. PMID 10494578. S2CID 12904841.
- ^ Takahashi, S.; Horikomi, K.; Kato, T. (2001-09-21). "MS-377, a novel selective sigma(1) receptor ligand, reverses phencyclidine-induced release of dopamine and serotonin in rat brain". European Journal of Pharmacology. 427 (3): 211–219. doi:10.1016/s0014-2999(01)01254-7. ISSN 0014-2999. PMID 11567651.
- ^ Takahashi, S.; Miwa, T.; Horikomi, K. (2000-07-28). "Involvement of sigma 1 receptors in methamphetamine-induced behavioral sensitization in rats". Neuroscience Letters. 289 (1): 21–24. doi:10.1016/s0304-3940(00)01258-1. ISSN 0304-3940. PMID 10899399. S2CID 54420748.
- ^ Ujike, H.; Kanzaki, A.; Okumura, K.; Akiyama, K.; Otsuki, S. (1992). "Sigma (sigma) antagonist BMY 14802 prevents methamphetamine-induced sensitization". Life Sciences. 50 (16): PL129–134. doi:10.1016/0024-3205(92)90466-3. ISSN 0024-3205. PMID 1313134.
- v
- t
- e
- Agonists: 3-PPP
- 4-PPBP
- 5-MeO-DMT
- Alazocine (SKF-10047)
- Amantadine
- Arketamine
- BD-737
- BD-1052
- Blarcamesine
- Captodiame
- Citalopram
- CGRPTooltip Calcitonin gene-related peptide
- Cloperastine
- Cocaine
- Cutamesine (SA-4503)
- Cyclazocine
- Dehydroepiandrosterone (DHEA) (prasterone)
- Dehydroepiandrosterone sulfate (DHEA-S) (prasterone sulfate)
- Dextrallorphan
- Dextromethorphan (DXM)
- Dextrorphan (DXO)
- Dimemorfan
- Dimethyltryptamine (DMT)
- Ditolylguanidine (DTG)
- Donepezil
- Eliprodil
- Escitalopram
- Fabomotizole (afobazole)
- Fluoxetine
- Fluvoxamine
- Ifenprodil
- Igmesine (JO-1784)
- IPAB
- Ketamine
- L-687384
- MDMA (midomafetamine)
- Memantine
- Methamphetamine
- Methoxetamine
- Methylphenidate
- Nepinalone
- Neuropeptide Y
- Noscapine
- OPC-14523
- Opipramol
- Pentazocine
- Pentoxyverine (carbetapentane)
- PRE-084
- Pregnenolone
- Pregnenolone sulfate
- Pridopidine
- Racemethorphan (methorphan)
- Racemorphan (morphanol)
- UMB-23
- UMB-82
- Antagonists: 3-PPP
- AC-927
- BD-1008
- BD-1031
- BD-1047
- BD-1060
- BD-1063
- BD-1067
- BMY-14802 (BMS-181100)
- CM-156
- Dup-734
- E-5842
- E-52862 (S1RA)
- Haloperidol
- LR-132
- LR-172
- MS-377
- NE-100
- NPC-16377
- Panamesine (EMD-57455)
- PD-144418
- Pentazocine
- Progesterone
- Rimcazole (BW-234U)
- Sertraline
- SR-31742A
- Allosteric modulators: Phenytoin; Positive: Methylphenylpiracetam
- SOMCL-668
- Unknown/unsorted: 3-Methoxydextrallorphan
- 3-MeO-PCP
- 4C-T-2
- 4-IBP
- 4-IPBS
- 4-MeO-PCP
- 5-MeO-DALT
- 5-MeO-DiPT
- Amitriptyline
- Azidopamil
- Chlorpromazine
- Clemastine
- Clomipramine
- Clorgiline
- D-Deprenyl
- DiPTTooltip N,N-Diisopropyltryptamine
- DPTTooltip N,N-Dipropyltryptamine
- Ibogaine
- Imipramine
- KCR-12-83.1
- Nemonapride
- Noribogaine
- RHL-033
- RS-67,333
- RTI-55
- Saffron
- Safinamide
- Selegiline
- Spipethiane
- Trifluoperazine
- W-18
- YKP10A
- Agonists: 3-PPP
- Arketamine
- BD-1047
- BD1063
- Ditolylguanidine (DTG)
- DKR-1005
- DKR-1051
- Haloperidol
- Ifenprodil
- Ketamine
- MDMA (midomafetamine)
- Methamphetamine
- OPC-14523
- Opipramol
- PB-28
- Phencyclidine
- Siramesine (Lu 28-179)
- UKH-1114
- Unknown/unsorted: 3-Methoxydextrallorphan
- 3-MeO-PCE
- 4-MeO-PCP
- 5-MeO-DALT
- 5-MeO-DiPT
- Clemastine
- DiPTTooltip N,N-Diisopropyltryptamine
- DPTTooltip N,N-Dipropyltryptamine
- Ibogaine
- Nemonapride
- Nepinalone
- Noribogaine
- Pentazocine
- RS-67,333
- Safinamide
- TMATooltip 3,4,5-Trimethoxyamphetamine
- UMB-23
- UMB-82
- W-18
- Antagonists: AHD1
- AZ66
- Lamotrigine
- Naloxone
- SM-21
- UMB-100
- UMB-101
- UMB-103
- UMB-116
- YZ-011
- YZ-069
- YZ-185
- Allosteric modulators: SKF-83959
- Unknown/unsorted: 18-Methoxycoronaridine
- BMY-13980
- Butaclamol
- Caramiphen
- Carvotroline
- Chlorphenamine (chlorpheniramine)
- Chlorpromazine
- Cinnarizine
- Cinuperone
- Clocapramine
- Dezocine
- EMD-59983
- Hypericin (St. John's wort)
- Fluphenazine
- Gevotroline (WY-47384)
- Mepyramine (pyrilamine)
- Molindone
- Perphenazine
- Pimozide
- Proadifen
- Promethazine
- Propranolol
- Quinidine
- Remoxipride
- SL 82.0715
- SR-31747A
- Tiospirone (BMY-13859)
- Venlafaxine