SB-215505: Difference between revisions

Page 1
Page 2
Content deleted Content added
CheMoBot (talk | contribs)
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
Added s2cid. Added the cs1 style template to denote Vancouver ("vanc") citation style, because references contain "vauthors" attribute to specify the list of authors.
 
(23 intermediate revisions by 15 users not shown)
Line 1: Line 1:
{{Short description|Chemical compound}}
{{cs1 config|name-list-style=vanc}}
{{Drugbox
{{Drugbox
| Verifiedfields = changed
| verifiedrevid = 449561713
| verifiedrevid = 451223119
| 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
| image = SB-215,505_structure.png
| image = SB-215,505 structure.png
| width = 220
| width = 300


<!--Clinical data-->
<!--Clinical data-->
Line 25: Line 28:


<!--Identifiers-->
<!--Identifiers-->
| CAS_number_Ref = {{cascite|correct|??}}
| CAS_number = 162100-15-4
| CAS_number = 162100-15-4
| ATC_prefix =
| ATC_prefix =
Line 31: Line 35:
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
| DrugBank =
| DrugBank =
| ChEMBL_Ref = {{ebicite|changed|EBI}}
| ChEMBL = 525998
| ChemSpiderID = 5036305


<!--Chemical data-->
<!--Chemical data-->
| C=19 | H=16 | Cl=1 | N=3 | O=1
| C=19 | H=16 | Cl=1 | N=3 | O=1
| molecular_weight = 337.803 g/mol
| 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
| 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)
| StdInChIKey = BPVGSWDWIRIUME-UHFFFAOYSA-N
}}
}}


'''SB-215,505''' 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 |author=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 |year=2004 |month=August |pmid=15265808 |pmc=1575194 |doi=10.1038/sj.bjp.0705887 |url=}}</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 |author=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 |year=2004 |month=August |pmid=15302781 |doi=10.1161/01.CIR.0000139856.20505.57 |url=}}</ref><ref name="pmid16962085">{{cite journal |author=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 |year=2006 |month=November |pmid=16962085 |doi=10.1016/j.cardiores.2006.08.003 |url=}}</ref><ref name="pmid18591460">{{cite journal |author=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 |year=2008 |month=August |pmid=18591460 |doi=10.1161/HYPERTENSIONAHA.107.105551 |url=}}</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 |author=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 |year=1999 |month=February |pmid=10188965 |pmc=1565856 |doi=10.1038/sj.bjp.0702350 |url=}}</ref><ref name="pmid12377394">{{cite journal |author=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 |year=2002 |month=October |pmid=12377394 |doi=10.1016/S0893-133X(02)00342-1 |url=}}</ref><ref name="pmid17673981">{{cite journal |author=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 |year=2007 |month=December |pmid=17673981 |doi=10.1007/s00213-007-0891-z |url=}}</ref>
'''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>


== References ==
==References==
{{reflist}}
{{Reflist|2}}


{{Serotonergics}}
{{Serotonergics}}


[[Category:5-HT2B antagonists]]
[[Category:5-HT2B antagonists]]
[[Category:Organochlorides]]
[[Category:Chloroarenes]]
[[Category:Indoles]]
[[Category:Indolines]]
[[Category:Amides]]
[[Category:Ureas]]
[[Category:Quinolines]]
[[Category:Quinolines]]