Chemistry:RS-127445

From HandWiki

RS-127445, also known as MT-500, is a drug which acts as a potent and selective antagonist at the serotonin 5-HT2B receptor, with around 1,000-fold selectivity over the closely related 5-HT2A and 5-HT2C receptors.[1] The role of the 5-HT2B receptor in the body is still poorly understood, and RS-127445 has been a useful tool in unravelling the function of the various systems in which this receptor is expressed.[2][3][4] The drug was under development for potential use as a pharmaceutical drug by Roche and reached phase 1 clinical trials but was discontinued for unknown reasons.[5][6]

RS-127445 has been found to diminish the head-twitch response, a behavioral proxy of psychedelic effects, induced by the psychedelic drug LSD in rats but not in mice.[7] It also blocked the persistent antidepressant-like effects produced by LSD in rats.[7]

References

  1. ↑ "RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist". British Journal of Pharmacology 127 (5): 1075–82. July 1999. doi:10.1038/sj.bjp.0702632. PMID 10455251. 
  2. ↑ "Function of the serotonin 5-hydroxytryptamine 2B receptor in pulmonary hypertension". Nature Medicine 8 (10): 1129–35. October 2002. doi:10.1038/nm764. PMID 12244304. https://hal.archives-ouvertes.fr/hal-01985063/file/NM_final_rev.pdf. 
  3. ↑ "Pharmacological evidence for a functional serotonin-2B receptor in a human uterine smooth muscle cell line". The Journal of Pharmacology and Experimental Therapeutics 317 (3): 1254–61. June 2006. doi:10.1124/jpet.105.100172. PMID 16517693. 
  4. ↑ "Investigation of the role of 5-HT2 receptor subtypes in the control of the bladder and the urethra in the anaesthetized female rat". British Journal of Pharmacology 155 (3): 343–56. October 2008. doi:10.1038/bjp.2008.273. PMID 18604238. 
  5. ↑ "Delving into the Latest Updates on MT-500 with Synapse". 21 November 2024. https://synapse.patsnap.com/drug/25e3744950dd4ddaadee224eea9973e5. 
  6. ↑ "Structure, Function, and Pharmaceutical Ligands of 5-Hydroxytryptamine 2B Receptor". Pharmaceuticals (Basel) 14 (2): 76. January 2021. doi:10.3390/ph14020076. PMID 33498477. 
  7. ↑ 7.0 7.1 "327. 5-HT2B Receptors Modulate the Antidepressant-like Response of the Psychedelic LSD in Rat But Not in Mice". International Journal of Neuropsychopharmacology 28 (Supplement_2): ii117–ii118. 18 August 2025. doi:10.1093/ijnp/pyaf052.234. ISSN 1461-1457. 



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