SB-204,741

From Wikipedia, the free encyclopedia
Jump to: navigation, search
SB-204,741
SB-204,741 structure.png
Systematic (IUPAC) name
N-(1-Methyl-1H-indol-5-yl)-N'-(3-methylisothiazol-5-yl)urea
Clinical data
Legal status ?
Identifiers
CAS number 152239-46-8 YesY
ATC code ?
PubChem CID 3277600
IUPHAR ligand 221
Synonyms SB-204,741
Chemical data
Formula C14H14N4OS 
Mol. mass 286.352 g/mol
 YesY (what is this?)  (verify)

SB-204,741 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[edit]

  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 Medical 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 1572101. 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 1575347. 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.