Chemistry:MS-377
MS-377 is a selective antagonist of the sigma-1 receptor.[1] 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.[2]
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.[3] It has also been shown to decrease methamphetamine behavioral sensitization,[4] this is also observed with other sigma antagonists.[5]
References
- ↑ "Drug Information | Therapeutic Target Database" (in en). https://idrblab.net/ttd/data/drug/details/D09OTG.
- ↑ Takahashi, S.; Sonehara, K.; Takagi, K.; Miwa, T.; Horikomi, K.; Mita, N.; Nagase, H.; Iizuka, K. et al. (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.
- ↑ 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.
- ↑ 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.
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