| 词条 | GW-405,833 |
| 释义 |
| Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 424782539 | IUPAC_name = 1-(2,3-Dichlorobenzoyl)-5-methoxy-2-methyl-3-[2-(4-morpholinyl)ethyl]-1H-indole | image = GW-405,833-2D-skeletal.svg | width = 240px | tradename = | legal_status = | routes_of_administration = | metabolism = | elimination_half-life = | excretion = | index_label = | index2_label = | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 180002-83-9 | PubChem = 9911463 | ChEMBL_Ref = {{ebicite|changed|EBI}} | ChEMBL = 73711 | ChemSpiderID = 8087114 | ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}} | smiles = CC1=C(C2=C(N1C(=O)C3=C(C(=CC=C3)Cl)Cl)C=CC(=C2)OC)CCN4CCOCC4 | smiles2 = C4COCCN4CCc1c(C)n(c(ccc3OC)c1c3)C(=O)c2cccc(Cl)c2Cl | StdInChI_Ref = {{stdinchicite|changed|chemspider}} | StdInChI = 1S/C23H24Cl2N2O3/c1-15-17(8-9-26-10-12-30-13-11-26)19-14-16(29-2)6-7-21(19)27(15)23(28)18-4-3-5-20(24)22(18)25/h3-7,14H,8-13H2,1-2H3 | StdInChIKey_Ref = {{stdinchicite|changed|chemspider}} | StdInChIKey = FSFZRNZSZYDVLI-UHFFFAOYSA-N | C=23 | H=24 | Cl=2 | N=2 | O=3 | molecular_weight = 447.353 g/mol }}GW-405,833 (L-768,242) is a drug that acts as a potent and selective partial agonist for the cannabinoid receptor subtype CB2, with an EC50 of 0.65 nM and selectivity of around 1200x for CB2 over CB1 receptors.[1][2] Animal studies have shown it to possess antiinflammatory and anti-hyperalgesic effects at low doses, followed by ataxia and analgesic effects when the dose is increased.[3][4] Selective CB2 agonist drugs such as GW-405,833 are hoped to be particularly useful in the treatment of allodynia and neuropathic pain for which current treatment options are often inadequate.[5][6] References1. ^Huffman JW. The search for selective ligands for the CB2 receptor. Current Pharmaceutical Design. 2000 Sep;6(13):1323-37. {{DOI|10.2174/1381612003399347}} {{PMID|10903395}} {{Cannabinoids}}{{cannabinoid-stub}}2. ^Marriott KS, Huffman JW. Recent advances in the development of selective ligands for the cannabinoid CB(2) receptor. Current Topics in Medicinal Chemistry. 2008;8(3):187-204. {{DOI|10.2174/156802608783498014}} {{PMID|18289088}} 3. ^Clayton N, Marshall FH, Bountra C, O'Shaughnessy CT. CB1 and CB2 cannabinoid receptors are implicated in inflammatory pain. Pain. 2002 Apr;96(3):253-60. {{PMID|11972997}} 4. ^Valenzano KJ, Tafesse L, Lee G, Harrison JE, Boulet JM, Gottshall SL, Mark L, Pearson MS, Miller W, Shan S, Rabadi L, Rotshteyn Y, Chaffer SM, Turchin PI, Elsemore DA, Toth M, Koetzner L, Whiteside GT. Pharmacological and pharmacokinetic characterization of the cannabinoid receptor 2 agonist, GW405833, utilizing rodent models of acute and chronic pain, anxiety, ataxia and catalepsy. Neuropharmacology. 2005 Apr;48(5):658-72. {{PMID|15814101}} 5. ^Beltramo M, Bernardini N, Bertorelli R, Campanella M, Nicolussi E, Fredduzzi S, Reggiani A. CB2 receptor-mediated antihyperalgesia: possible direct involvement of neural mechanisms. European Journal of Neuroscience. 2006 Mar;23(6):1530-8. {{DOI|10.1111/j.1460-9568.2006.04684.x}} {{PMID|16553616}} 6. ^Leichsenring A, Andriske M, Bäcker I, Stichel CC, Lübbert H. Analgesic and antiinflammatory effects of cannabinoid receptor agonists in a rat model of neuropathic pain. Naunyn Schmiedebergs Archives of Pharmacology. 2009 Jan 18. {{PMID|19152053}} 7 : Cannabinoids|Aminoalkylindoles|Benzoylindoles|Morpholines|Phenol ethers|Chloroarenes|CB2 receptor agonists |
| 随便看 |
|
开放百科全书收录14589846条英语、德语、日语等多语种百科知识，基本涵盖了大多数领域的百科知识，是一部内容自由、开放的电子版国际百科全书。