| 词条 | GR-113808 |
| 释义 |
| verifiedrevid = 449689555 | IUPAC_name = 1-(2-methylsulfonylaminoethyl-4-piperidinyl)methyl-1-methyl-1H-indole-3-carboxylate | image = GR-113808_structure.png | width = 220 | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | IUPHAR_ligand = 247 | CAS_number = 144625-51-4 | ATC_prefix = | ATC_suffix = | PubChem = 119376 | ChemSpiderID = 106623 | C=19 | H=27 | N=3 | O=4 | S=1 | molecular_weight = 393.499 g/mol | smiles = c13ccccc3c(cn1C)C(=O)OCC(CC2)CCN2CCNS(=O)(C)=O | StdInChI = 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 | StdInChIKey = MOZPSIXKYJUTKI-UHFFFAOYSA-N | melting_point = | melting_high = }}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] References1. ^{{cite journal |author=Kaumann AJ |title=Blockade of human atrial 5-HT4 receptors by GR 113808 |journal=British Journal of Pharmacology |volume=110 |issue=3 |pages=1172–4 |date=November 1993 |pmid=8298805 |pmc=2175795 |doi= 10.1111/j.1476-5381.1993.tb13937.x|url=}} {{Serotonergics}}{{nervous-system-drug-stub}}2. ^{{cite journal |vauthors=Mikami T, Sugimoto H, Naganeo R, Ohmi T, Saito T, Eda H |title=Contribution of active and inactive states of the human 5-HT4d receptor to the functional activities of 5-HT4-receptor agonists |journal=Journal of Pharmacological Sciences |volume=107 |issue=3 |pages=251–9 |date=July 2008 |pmid=18587219 |doi= 10.1254/jphs.fp0072230|url=}} 3. ^{{cite journal |vauthors=Cachard-Chastel M, Lezoualc'h F, Dewachter I, Deloménie C, Croes S, Devijver H, Langlois M, Van Leuven F, Sicsic S, Gardier AM |title=5-HT4 receptor agonists increase sAPPalpha levels in the cortex and hippocampus of male C57BL/6j mice |journal=British Journal of Pharmacology |volume=150 |issue=7 |pages=883–92 |date=April 2007 |pmid=17325649 |pmc=2013878 |doi=10.1038/sj.bjp.0707178 |url=}} 4. ^{{cite journal |vauthors=Matsuyoshi H, Kuniyasu H, Okumura M, Misawa H, Katsui R, Zhang GX, Obata K, Takaki M |title=A 5-HT(4)-receptor activation-induced neural plasticity enhances in vivo reconstructs of enteric nerve circuit insult |journal=Neurogastroenterology & Motility |volume=22 |issue=7 |pages=806–13, e226 |date=July 2010 |pmid=20146727 |doi=10.1111/j.1365-2982.2010.01474.x |url=}} 5. ^{{cite journal |vauthors=Kamei J, Ohsawa M, Hayashi SS, Nakanishi Y |title=Effect of chronic pain on morphine-induced respiratory depression in mice |journal=Neuroscience |volume=174 |issue= |pages=224–33 |date=February 2011 |pmid=21081158 |doi=10.1016/j.neuroscience.2010.11.012 |url=}} 6 : 5-HT4 antagonists|Amines|Piperidines|Indoles|Carboxylic acids|Sulfonamides |
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