SB-204741: Difference between revisions
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Importing Wikidata short description: "Chemical compound" |
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{{Short description|Chemical compound}} |
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{{Drugbox |
{{Drugbox |
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| verifiedrevid = |
| verifiedrevid = 449586687 |
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| IUPAC_name = ''N''-(1-Methyl-1''H''-indol-5-yl)-''N'''-(3-methylisothiazol-5-yl)urea |
| IUPAC_name = ''N''-(1-Methyl-1''H''-indol-5-yl)-''N'''-(3-methylisothiazol-5-yl)urea |
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| image = SB-204,741_structure.png |
| image = SB-204,741_structure.png |
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<!--Identifiers--> |
<!--Identifiers--> |
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| CAS_number_Ref = {{cascite|correct|CAS}} |
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| CAS_number = 152239-46-8 |
| CAS_number = 152239-46-8 |
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| UNII_Ref = {{fdacite|correct|FDA}} |
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| UNII = 9VHM49MS42 |
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| ATC_prefix = |
| ATC_prefix = |
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| ATC_suffix = |
| ATC_suffix = |
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| PubChem = 3277600 |
| PubChem = 3277600 |
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| ChEBI = 140936 |
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| IUPHAR_ligand = 221 |
| IUPHAR_ligand = 221 |
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| DrugBank_Ref = {{drugbankcite|correct|drugbank}} |
| DrugBank_Ref = {{drugbankcite|correct|drugbank}} |
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| DrugBank = |
| DrugBank = |
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| ChemSpiderID = 2526822 |
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<!--Chemical data--> |
<!--Chemical data--> |
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| C=14 | H=14 | N=4 | O=1 | S=1 |
| C=14 | H=14 | N=4 | O=1 | S=1 |
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| molecular_weight = 286.352 g/mol |
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| smiles = c2c(C)nsc2NC(=O)Nc3ccc1n(C)ccc1c3 |
| smiles = c2c(C)nsc2NC(=O)Nc3ccc1n(C)ccc1c3 |
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| synonyms = SB-204,741 |
| synonyms = SB-204,741 |
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| StdInChI = 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) |
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| StdInChIKey = USFUFHFQWXDVMH-UHFFFAOYSA-N |
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}} |
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'''SB- |
'''SB-204741''' is a drug which acts as a potent and selective [[Antagonist (pharmacology)|antagonist]] at the [[serotonin]] [[5-HT2B receptor|5-HT<sub>2B</sub>]] [[Receptor (biochemistry)|receptor]], with around 135x selectivity over the closely related [[5-HT2C receptor|5-HT<sub>2C</sub>]] receptor, and even higher over the [[5-HT2A receptor|5-HT<sub>2A</sub>]] receptor and other targets.<ref>{{cite journal | vauthors = Forbes IT, Jones GE, Murphy OE, Holland V, Baxter GS | title = N-(1-methyl-5-indolyl)-N'-(3-methyl-5-isothiazolyl)urea: a novel, high-affinity 5-HT2B receptor antagonist | journal = Journal of Medicinal Chemistry | volume = 38 | issue = 6 | pages = 855–7 | date = March 1995 | pmid = 7699699 | doi = 10.1021/jm00006a001 }}</ref> It is used in scientific research for investigating the functions of the 5-HT<sub>2B</sub> receptor.<ref>{{cite journal | vauthors = Glusa E, Pertz HH | title = Further evidence that 5-HT-induced relaxation of pig pulmonary artery is mediated by endothelial 5-HT(2B) receptors | journal = British Journal of Pharmacology | volume = 130 | issue = 3 | pages = 692–8 | date = June 2000 | pmid = 10821800 | pmc = 1572101 | doi = 10.1038/sj.bjp.0703341 }}</ref><ref>{{cite journal | vauthors = Holohean AM, Hackman JC | title = Mechanisms intrinsic to 5-HT2B receptor-induced potentiation of NMDA receptor responses in frog motoneurones | journal = British Journal of Pharmacology | volume = 143 | issue = 3 | pages = 351–60 | date = October 2004 | pmid = 15339859 | pmc = 1575347 | doi = 10.1038/sj.bjp.0705935 }}</ref><ref>{{cite journal | vauthors = Papageorgiou A, Denef C | title = 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 | journal = Endocrinology | volume = 148 | issue = 9 | pages = 4509–22 | date = September 2007 | pmid = 17584957 | doi = 10.1210/en.2007-0034 | doi-access = free }}</ref><ref>{{cite journal | vauthors = Wouters MM, Gibbons SJ, Roeder JL, Distad M, Ou Y, Strege PR, Szurszewski JH, Farrugia G | display-authors = 6 | title = Exogenous serotonin regulates proliferation of interstitial cells of Cajal in mouse jejunum through 5-HT2B receptors | journal = Gastroenterology | volume = 133 | issue = 3 | pages = 897–906 | date = September 2007 | pmid = 17854596 | doi = 10.1053/j.gastro.2007.06.017 | url = https://lirias.kuleuven.be/bitstream/123456789/160659/1/2007+Gastro+5-HT.pdf }}</ref> |
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== References == |
== References == |
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{{ |
{{Reflist|2}} |
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{{Serotonergics}} |
{{Serotonergics}} |
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[[Category:Ureas]] |
[[Category:Ureas]] |
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[[Category:Indoles]] |
[[Category:Indoles]] |
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{{nervous-system-drug-stub}} |
{{nervous-system-drug-stub}} |