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]

SB-204741
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 InfoCard100.150.276 Edit this at Wikidata
Chemical and physical data
FormulaC14H14N4OS
Molar mass286.35 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)

References

edit
  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 7699699.855-7&rft.date=1995-03&rft_id=info:doi/10.1021/jm00006a001&rft_id=info:pmid/7699699&rft.aulast=Forbes&rft.aufirst=IT&rft.au=Jones, GE&rft.au=Murphy, OE&rft.au=Holland, V&rft.au=Baxter, GS&rfr_id=info:sid/en.wikipedia.org:SB-204741" class="Z3988">
  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 10821800.692-8&rft.date=2000-06&rft_id=https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1572101#id-name=PMC&rft_id=info:pmid/10821800&rft_id=info:doi/10.1038/sj.bjp.0703341&rft.aulast=Glusa&rft.aufirst=E&rft.au=Pertz, HH&rft_id=https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1572101&rfr_id=info:sid/en.wikipedia.org:SB-204741" class="Z3988">
  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 15339859.351-60&rft.date=2004-10&rft_id=https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1575347#id-name=PMC&rft_id=info:pmid/15339859&rft_id=info:doi/10.1038/sj.bjp.0705935&rft.aulast=Holohean&rft.aufirst=AM&rft.au=Hackman, JC&rft_id=https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1575347&rfr_id=info:sid/en.wikipedia.org:SB-204741" class="Z3988">
  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 17584957.4509-22&rft.date=2007-09&rft_id=info:doi/10.1210/en.2007-0034&rft_id=info:pmid/17584957&rft.aulast=Papageorgiou&rft.aufirst=A&rft.au=Denef, C&rft_id=https://doi.org/10.1210%2Fen.2007-0034&rfr_id=info:sid/en.wikipedia.org:SB-204741" class="Z3988">
  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 17854596.897-906&rft.date=2007-09&rft_id=info:doi/10.1053/j.gastro.2007.06.017&rft_id=info:pmid/17854596&rft.aulast=Wouters&rft.aufirst=MM&rft.au=Gibbons, SJ&rft.au=Roeder, JL&rft.au=Distad, M&rft.au=Ou, Y&rft.au=Strege, PR&rft.au=Szurszewski, JH&rft.au=Farrugia, G&rft_id=https://lirias.kuleuven.be/bitstream/123456789/160659/1/2007+Gastro+5-HT.pdf&rfr_id=info:sid/en.wikipedia.org:SB-204741" class="Z3988">