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)

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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.

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