GR-113,808

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GR-113,808
GR-113808 structure.png
Systematic (IUPAC) name
1-(2-methylsulfonylaminoethyl-4-piperidinyl)methyl-1-methyl-1H-indole-3-carboxylate
Clinical data
Legal status ?
Identifiers
CAS number 144625-51-4
ATC code ?
PubChem CID 119376
Chemical data
Formula C19H27N3O4S 
Mol. mass 393.499 g/mol
 YesY (what is this?)  (verify)

GR-113,808 is a drug which acts as a potent and selective 5-HT4 serotonin receptor antagonist.[1] It is used in researching the roles of 5-HT4 receptors in various processes,[2] and has been used to test some of the proposed therapeutic effects of selective 5-HT4 agonists, such as for instance blocking the nootropic effects of 5-HT4 agonists,[3][4] and worsening the respiratory depression produced by opioid analgesic drugs, which appears to be partly 5-HT4 mediated and can be counteracted by certain 5-HT4 agonists.[5]

References[edit]

  1. ^ Kaumann AJ (November 1993). "Blockade of human atrial 5-HT4 receptors by GR 113808". British Journal of Pharmacology 110 (3): 1172–4. doi:10.1111/j.1476-5381.1993.tb13937.x. PMC 2175795. PMID 8298805. 
  2. ^ Mikami T, Sugimoto H, Naganeo R, Ohmi T, Saito T, Eda H (July 2008). "Contribution of active and inactive states of the human 5-HT4d receptor to the functional activities of 5-HT4-receptor agonists". Journal of Pharmacological Sciences 107 (3): 251–9. doi:10.1254/jphs.fp0072230. PMID 18587219. 
  3. ^ Cachard-Chastel M, Lezoualc'h F, Dewachter I, Deloménie C, Croes S, Devijver H, Langlois M, Van Leuven F, Sicsic S, Gardier AM (April 2007). "5-HT4 receptor agonists increase sAPPalpha levels in the cortex and hippocampus of male C57BL/6j mice". British Journal of Pharmacology 150 (7): 883–92. doi:10.1038/sj.bjp.0707178. PMC 2013878. PMID 17325649. 
  4. ^ Matsuyoshi H, Kuniyasu H, Okumura M, Misawa H, Katsui R, Zhang GX, Obata K, Takaki M (July 2010). "A 5-HT(4)-receptor activation-induced neural plasticity enhances in vivo reconstructs of enteric nerve circuit insult". Neurogastroenterology and Motility : the Official Journal of the European Gastrointestinal Motility Society 22 (7): 806–13, e226. doi:10.1111/j.1365-2982.2010.01474.x. PMID 20146727. 
  5. ^ Kamei J, Ohsawa M, Hayashi SS, Nakanishi Y (February 2011). "Effect of chronic pain on morphine-induced respiratory depression in mice". Neuroscience 174: 224–33. doi:10.1016/j.neuroscience.2010.11.012. PMID 21081158.