SB-204741

Last updated
SB-204741
SB-204,741 structure.png
Clinical data
Other namesSB-204,741
Identifiers
  • N-(1-Methyl-1H-indol-5-yl)-N'-(3-methylisothiazol-5-yl)urea
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEBI
CompTox Dashboard (EPA)
ECHA InfoCard 100.150.276 OOjs UI icon edit-ltr-progressive.svg
Chemical and physical data
Formula C14H14N4OS
Molar mass 286.35 g·mol−1
3D model (JSmol)
  • c2c(C)nsc2NC(=O)Nc3ccc1n(C)ccc1c3
  • InChI=1S/C14H14N4OS/c1-9-7-13(20-17-9)16-14(19)15-11-3-4-12-10(8-11)5-6-18(12)2/h3-8H,1-2H3,(H2,15,16,19)
  • Key:USFUFHFQWXDVMH-UHFFFAOYSA-N
   (verify)

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 (March 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 (June 2000). "Further evidence that 5-HT-induced relaxation of pig pulmonary artery is mediated by endothelial 5-HT(2B) receptors". British Journal of Pharmacology. 130 (3): 692–8. doi:10.1038/sj.bjp.0703341. PMC   1572101 . PMID   10821800.
  3. Holohean AM, Hackman JC (October 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   1575347 . PMID   15339859.
  4. Papageorgiou A, Denef C (September 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, et al. (September 2007). "Exogenous serotonin regulates proliferation of interstitial cells of Cajal in mouse jejunum through 5-HT2B receptors" (PDF). Gastroenterology. 133 (3): 897–906. doi:10.1053/j.gastro.2007.06.017. PMID   17854596.