SB-215505: Difference between revisions
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Updating {{drugbox}} (no changed fields - added verified revid - updated 'ChemSpiderID_Ref', 'UNII_Ref', 'ChEMBL_Ref', 'ChEBI_Ref', 'KEGG_Ref', 'StdInChI_Ref', 'StdInChIKey_Ref', 'ChEBI_Ref') per Chem/Drugbox validation (report [[Wik |
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{{Short description|Chemical compound}} |
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{{cs1 config|name-list-style=vanc}} |
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{{Drugbox |
{{Drugbox |
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| Verifiedfields = changed |
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| verifiedrevid = |
| verifiedrevid = 451223119 |
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| IUPAC_name = 6-chloro-5-methyl-N-quinolin-4-yl-2,3-dihydroindole-1-carboxamide |
| IUPAC_name = 6-chloro-5-methyl-N-quinolin-4-yl-2,3-dihydroindole-1-carboxamide |
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| image = SB-215, |
| image = SB-215,505 structure.png |
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| width = |
| width = 300 |
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<!--Clinical data--> |
<!--Clinical data--> |
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<!--Identifiers--> |
<!--Identifiers--> |
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| CAS_number_Ref = {{cascite|correct|??}} |
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| CAS_number = 162100-15-4 |
| CAS_number = 162100-15-4 |
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| ATC_prefix = |
| ATC_prefix = |
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| DrugBank_Ref = {{drugbankcite|correct|drugbank}} |
| DrugBank_Ref = {{drugbankcite|correct|drugbank}} |
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| DrugBank = |
| DrugBank = |
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| ChEMBL_Ref = {{ebicite|changed|EBI}} |
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| ChEMBL = 525998 |
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| ChemSpiderID = 5036305 |
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<!--Chemical data--> |
<!--Chemical data--> |
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| C=19 | H=16 | Cl=1 | N=3 | O=1 |
| C=19 | H=16 | Cl=1 | N=3 | O=1 |
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| molecular_weight = 337.803 g/mol |
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| smiles = CC1=C(C=C2C(=C1)CCN2C(=O)NC3=CC=NC4=CC=CC=C43)Cl |
| smiles = CC1=C(C=C2C(=C1)CCN2C(=O)NC3=CC=NC4=CC=CC=C43)Cl |
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| StdInChI = 1S/C19H16ClN3O/c1-12-10-13-7-9-23(18(13)11-15(12)20)19(24)22-17-6-8-21-16-5-3-2-4-14(16)17/h2-6,8,10-11H,7,9H2,1H3,(H,21,22,24) |
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| StdInChIKey = BPVGSWDWIRIUME-UHFFFAOYSA-N |
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'''SB- |
'''SB-215505''' 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 good selectivity over the related [[5-HT2A receptor|5-HT<sub>2A</sub>]] and [[5-HT2C receptor|5-HT<sub>2C</sub>]] receptors.<ref name="pmid15265808">{{cite journal |vauthors=Kantor S, Jakus R, Balogh B, Benko A, Bagdy G |title=Increased wakefulness, motor activity and decreased theta activity after blockade of the 5-HT2B receptor by the subtype-selective antagonist SB-215505 |journal=[[British Journal of Pharmacology]] |volume=142 |issue=8 |pages=1332–42 |date=August 2004 |pmid=15265808 |pmc=1575194 |doi=10.1038/sj.bjp.0705887 }}</ref> It is used in scientific research into the function of the 5-HT<sub>2</sub> family of receptors, especially to study the role of 5-HT<sub>2B</sub> receptors in the heart,<ref name="pmid15302781">{{cite journal |vauthors=Jaffré F, Callebert J, Sarre A, Etienne N, Nebigil CG, Launay JM, Maroteaux L, Monassier L |title=Involvement of the serotonin 5-HT2B receptor in cardiac hypertrophy linked to sympathetic stimulation: control of interleukin-6, interleukin-1beta, and tumor necrosis factor-alpha cytokine production by ventricular fibroblasts |journal=Circulation |volume=110 |issue=8 |pages=969–74 |date=August 2004 |pmid=15302781 |doi=10.1161/01.CIR.0000139856.20505.57 |url=https://hal.archives-ouvertes.fr/hal-01274954/file/Circulation110_969_jaffre.pdf|doi-access=free }}</ref><ref name="pmid16962085">{{cite journal |vauthors=Liang YJ, Lai LP, Wang BW, Juang SJ, Chang CM, Leu JG, Shyu KG |title=Mechanical stress enhances serotonin 2B receptor modulating brain natriuretic peptide through nuclear factor-kappaB in cardiomyocytes |journal=Cardiovascular Research |volume=72 |issue=2 |pages=303–12 |date=November 2006 |pmid=16962085 |doi=10.1016/j.cardiores.2006.08.003 |doi-access=free }}</ref><ref name="pmid18591460">{{cite journal |vauthors=Monassier L, Laplante MA, Jaffré F, Bousquet P, Maroteaux L, de Champlain J |title=Serotonin 5-HT(2B) receptor blockade prevents reactive oxygen species-induced cardiac hypertrophy in mice |journal=Hypertension |volume=52 |issue=2 |pages=301–7 |date=August 2008 |pmid=18591460 |doi=10.1161/HYPERTENSIONAHA.107.105551 |doi-access=free }}</ref> and to distinguish 5-HT<sub>2B</sub>-mediated responses from those produced by 5-HT<sub>2A</sub> or 5-HT<sub>2C</sub>.<ref name="pmid10188965">{{cite journal |vauthors=Reavill C, Kettle A, Holland V, Riley G, Blackburn TP |title=Attenuation of haloperidol-induced catalepsy by a 5-HT2C receptor antagonist |journal=British Journal of Pharmacology |volume=126 |issue=3 |pages=572–4 |date=February 1999 |pmid=10188965 |pmc=1565856 |doi=10.1038/sj.bjp.0702350 }}</ref><ref name="pmid12377394">{{cite journal |vauthors=Fletcher PJ, Grottick AJ, Higgins GA |title=Differential effects of the 5-HT(2A) receptor antagonist M100907 and the 5-HT(2C) receptor antagonist SB242084 on cocaine-induced locomotor activity, cocaine self-administration and cocaine-induced reinstatement of responding |journal=Neuropsychopharmacology |volume=27 |issue=4 |pages=576–86 |date=October 2002 |pmid=12377394 |doi=10.1016/S0893-133X(02)00342-1 |doi-access=free }}</ref><ref name="pmid17673981">{{cite journal |vauthors=Fletcher PJ, Tampakeras M, Sinyard J, Higgins GA |title=Opposing effects of 5-HT(2A) and 5-HT(2C) receptor antagonists in the rat and mouse on premature responding in the five-choice serial reaction time test |journal=Psychopharmacology |volume=195 |issue=2 |pages=223–34 |date=December 2007 |pmid=17673981 |doi=10.1007/s00213-007-0891-z |s2cid=8334076 }}</ref> |
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== |
==References== |
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{{ |
{{Reflist|2}} |
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{{Serotonergics}} |
{{Serotonergics}} |
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[[Category:5-HT2B antagonists]] |
[[Category:5-HT2B antagonists]] |
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[[Category: |
[[Category:Chloroarenes]] |
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[[Category: |
[[Category:Indolines]] |
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[[Category: |
[[Category:Ureas]] |
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[[Category:Quinolines]] |
[[Category:Quinolines]] |
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