SB-204741

SB-204741
Clinical data
Other names	SB-204,741
Identifiers
	IUPAC name N-(1-Methyl-1H-indol-5-yl)-N'-(3-methylisothiazol-5-yl)urea;
CAS Number	152239-46-8 ;
PubChem CID	3277600;
IUPHAR/BPS	221;
ChemSpider	2526822;
UNII	9VHM49MS42;
ChEBI	CHEBI:140936;
CompTox Dashboard (EPA)	DTXSID80390956 ;
ECHA InfoCard	100.150.276
Chemical and physical data
Formula	C14H14N4OS
Molar mass	286.35 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES c2c(C)nsc2NC(=O)Nc3ccc1n(C)ccc1c3;
	InChI 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-HT_2B receptor, with around 135x selectivity over the closely related 5-HT_2C receptor, and even higher over the 5-HT_2A receptor and other targets.[1] It is used in scientific research for investigating the functions of the 5-HT_2B receptor.[2][3][4][5]

References

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.
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.
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.
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.
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.

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[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.