GR-113808

GR-113808
Identifiers
	IUPAC name 1-(2-methylsulfonylaminoethyl-4-piperidinyl)methyl-1-methyl-1H-indole-3-carboxylate;
CAS Number	144625-51-4;
PubChem CID	119376;
IUPHAR/BPS	247;
ChemSpider	106623;
CompTox Dashboard (EPA)	DTXSID40162772 ;
Chemical and physical data
Formula	C19H27N3O4S
Molar mass	393.499 g/mol g·mol−1
3D model (JSmol)	Interactive image;
	SMILES c13ccccc3c(cn1C)C(=O)OCC(CC2)CCN2CCNS(=O)(C)=O;
	InChI InChI=1S/C19H27N3O4S/c1-21-13-17(16-5-3-4-6-18(16)21)19(23)26-14-15-7-10-22(11-8-15)12-9-20-27(2,24)25/h3-6,13,15,20H,7-12,14H2,1-2H3; Key:MOZPSIXKYJUTKI-UHFFFAOYSA-N;
(verify)

GR-113808 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

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.
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.
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.
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 & Motility. 22 (7): 806–13, e226. doi:10.1111/j.1365-2982.2010.01474.x. PMID 20146727.
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.

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[pmid8298805-1] 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.

[pmid18587219-2] 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.

[pmid17325649-3] 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.

[pmid20146727-4] 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 & Motility. 22 (7): 806–13, e226. doi:10.1111/j.1365-2982.2010.01474.x. PMID 20146727.

[pmid21081158-5] 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.