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SB-204,741: Wikis

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SB-204,741
Systematic (IUPAC) name
N-(1-Methyl-1H-indol-5-yl)- N'-(3-methylisothiazol-5-yl)urea
Identifiers
CAS number 152239-46-8
ATC code  ?
PubChem 3277600
Chemical data
Formula C 14H14N4OS 
Mol. mass 286.352 g/mol
SMILES eMolecules & PubChem
Synonyms SB-204,741
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes  ?

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

  1. ^ Forbes IT, Jones GE, Murphy OE, Holland V, Baxter GS. N-(1-methyl-5-indolyl)-N'-(3-methyl-5-isothiazolyl)urea: a novel, high-affinity 5-HT2B receptor antagonist. Journal of Medicinal Chemistry. 1995 Mar 17;38(6):855-7. PMID 7699699
  2. ^ Glusa E, Pertz HH. Further evidence that 5-HT-induced relaxation of pig pulmonary artery is mediated by endothelial 5-HT(2B) receptors. British Journal of Pharmacology. 2000 Jun;130(3):692-8. PMID 10821800
  3. ^ Holohean AM, Hackman JC. Mechanisms intrinsic to 5-HT2B receptor-induced potentiation of NMDA receptor responses in frog motoneurones. British Journal of Pharmacology. 2004 Oct;143(3):351-60. PMID 15339859
  4. ^ Papageorgiou A, Denef C. 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. 2007 Sep;148(9):4509-22. PMID 17584957
  5. ^ Wouters MM, Gibbons SJ, Roeder JL, Distad M, Ou Y, Strege PR, Szurszewski JH, Farrugia G. Exogenous serotonin regulates proliferation of interstitial cells of Cajal in mouse jejunum through 5-HT2B receptors. Gastroenterology. 2007 Sep;133(3):897-906. PMID 17854596
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