SB-204741

SB-204741
Identifiers
Synonyms SB-204,741
CAS Number 152239-46-8 YesY
PubChem (CID) 3277600
IUPHAR/BPS 221
ECHA InfoCard 100.150.276
Chemical and physical data
Formula C14H14N4OS
Molar mass 286.352 g/mol
3D model (Jmol) Interactive image
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SB-204741 is a drug which acts as a potent and selective antagonist at the serotonin 5-HT2B receptor, with around 135x selectivity over the closely related 5-HT2C receptor, and even higher over the 5-HT2A receptor and other targets.[1] It is used in scientific research for investigating the functions of the 5-HT2B receptor.[2][3][4][5]

References

  1. Forbes, IT; Jones, GE; Murphy, OE; Holland, V; Baxter, GS (1995). "N-(1-methyl-5-indolyl)-N'-(3-methyl-5-isothiazolyl)urea: a novel, high-affinity 5-HT2B receptor antagonist". Journal of Medicinal Chemistry. 38 (6): 855–7. doi:10.1021/jm00006a001. PMID 7699699.
  2. Glusa, E; Pertz, HH (2000). "Further evidence that 5-HT-induced relaxation of pig pulmonary artery is mediated by endothelial 5-HT2B receptors". British Journal of Pharmacology. 130 (3): 692–8. doi:10.1038/sj.bjp.0703341. PMC 1572101Freely accessible. PMID 10821800.
  3. Holohean, AM; Hackman, JC (2004). "Mechanisms intrinsic to 5-HT2B receptor-induced potentiation of NMDA receptor responses in frog motoneurones". British Journal of Pharmacology. 143 (3): 351–60. doi:10.1038/sj.bjp.0705935. PMC 1575347Freely accessible. PMID 15339859.
  4. Papageorgiou, A; Denef, C (2007). "Stimulation of growth hormone release by 5-hydroxytryptamine (5-HT) in cultured rat anterior pituitary cell aggregates: evidence for mediation by 5-HT2B, 5-HT7, 5-HT1B, and ketanserin-sensitive receptors". Endocrinology. 148 (9): 4509–22. doi:10.1210/en.2007-0034. PMID 17584957.
  5. Wouters, MM; Gibbons, SJ; Roeder, JL; Distad, M; Ou, Y; Strege, PR; Szurszewski, JH; Farrugia, G (2007). "Exogenous serotonin regulates proliferation of interstitial cells of Cajal in mouse jejunum through 5-HT2B receptors". Gastroenterology. 133 (3): 897–906. doi:10.1053/j.gastro.2007.06.017. PMID 17854596.



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