Piboserod: Difference between revisions

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{{drugbox

{{Drugbox

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|image= Piboserod.png

| Verifiedfields = changed

| Watchedfields = changed

| verifiedrevid = 408035930

| IUPAC_name = ''N''-((1-Butyl-4-piperidyl)-methyl)-3,4-dihydro-2''H''-(1,3)oxazino(3,2-a)indole-10-carboxamide

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| image = Piboserod.png

| tradename = Serlipet

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| legal_status = Clinical phase II

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| routes_of_administration = Oral

| CAS_number_Ref = {{cascite|correct|??}}

| CAS_number = 152811-62-6

| ATC_prefix = none

| PubChem = 177336

| IUPHAR_ligand = 225

| UNII_Ref = {{fdacite|changed|FDA}}

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| C = 22 | H = 31 | N = 3 | O = 2

| UNII = 4UQ3S81B25

| molecular_weight = 369.50 g/mol

| ChEMBL_Ref = {{ebicite|changed|EBI}}

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| legal_status = Clinical phase II

| ChEMBL = 356359

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| routes_of_administration = Oral

| ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}}

| ChemSpiderID = 154413

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| C=22 | H=31 | N=3 | O=2

| smiles = CCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1

| StdInChI_Ref = {{stdinchicite|changed|chemspider}}

| StdInChI = 1S/C22H31N3O2/c1-2-3-11-24-13-9-17(10-14-24)16-23-21(26)20-18-7-4-5-8-19(18)25-12-6-15-27-22(20)25/h4-5,7-8,17H,2-3,6,9-16H2,1H3,(H,23,26)

| StdInChIKey_Ref = {{stdinchicite|changed|chemspider}}

| StdInChIKey = KVCSJPATKXABRQ-UHFFFAOYSA-N

}}

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==Mechanism of action==

In 2002 a research group at the [[Oslo University|University of Oslo]] discovered that muscles from the [[Cardiac ventricle|ventricle]] of failing hearts have increased responsiveness to [[serotonin]].<ref>~~Bratteli~~ T. et ~~al.~~, Functional serotonin 5-HT4 receptors in porcine and human ventricular myocardium with increased 5-HT4 mRNA in heart failure. Naunyn-Schmiedeberg's ~~Arch.~~ ~~Pharmacol.,~~ 370~~:157-166,~~ 2004</ref> They later demonstrated that the effect was due to an [[Expression (genetics)|expression]] of functional 5-HT4 receptors in the failing muscle. On the basis of these findings, and in analogy with the success of [[betablocker]]s in heart failure, the group made the hypothesis that 5-HT4 receptor antagonists could be useful to treat heart failure. Their hypothesis was tested in [[animal model]]s of heart failure with positive results.<ref>Birkeland JA. et ~~al.~~, Effects of treatment with a 5-HT4 receptor antagonist in heart failure. Br J ~~Pharmacol.~~ ~~2007~~ ~~Jan;~~150(2~~):143-52.~~ ~~Epub~~ ~~2006~~ ~~Dec~~ 11. </ref>

In 2002 a research group at the [[Oslo University|University of Oslo]] discovered that muscles from the [[Cardiac ventricle|ventricle]] of failing hearts have increased responsiveness to [[serotonin]].<ref>{{cite journal | vauthors = Brattelid T, Qvigstad E, Lynham JA, Molenaar P, Aass H, Geiran O, Skomedal T, Osnes JB, Levy FO, Kaumann AJ | display-authors = 6 | title = Functional serotonin 5-HT4 receptors in porcine and human ventricular myocardium with increased 5-HT4 mRNA in heart failure | journal = Naunyn-Schmiedeberg's Archives of Pharmacology | volume = 370 | issue = 3 | pages = 157–66 | date = September 2004 | pmid = 15365689 | doi = 10.1007/s00210-004-0963-0 | s2cid = 12306762 }}</ref> They later demonstrated that the effect was due to an [[Expression (genetics)|expression]] of functional 5-HT4 receptors in the failing muscle. On the basis of these findings, and in analogy with the success of [[betablocker]]s in heart failure, the group made the hypothesis that 5-HT4 receptor antagonists could be useful to treat heart failure. Their hypothesis was tested in [[animal model]]s of heart failure with positive results.<ref>{{cite journal | vauthors = Birkeland JA, Sjaastad I, Brattelid T, Qvigstad E, Moberg ER, Krobert KA, Bjørnerheim R, Skomedal T, Sejersted OM, Osnes JB, Levy FO | display-authors = 6 | title = Effects of treatment with a 5-HT4 receptor antagonist in heart failure | journal = British Journal of Pharmacology | volume = 150 | issue = 2 | pages = 143–52 | date = January 2007 | pmid = 17160012 | pmc = 2042907 | doi = 10.1038/sj.bjp.0706966 }}</ref>

==References==

== References ==

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[[Category:5-HT4 antagonists]]

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~~[[Category:~~GlaxoSmithKline]]

[[Category:Piperidines]]

[[Category:~~Amides~~]]

[[Category:Carboxamides]]

[[Category:Indoles]]

[[Category:Drugs developed by GSK plc]]