| 词条 | A-796,260 |
| 释义 |
| Watchedfields = changed | verifiedrevid = 456505609 |IUPAC_name = [1-(2-morpholin-4-ylethyl)-1H-indol-3-yl]-(2,2,3,3-tetramethylcyclopropyl)methanone | image = A-796260_structure.png | width= 200 | CAS_number_Ref = {{cascite|changed|??}} | CAS_number= 895155-26-7 | ATC_prefix= | ATC_suffix= | ChEMBL_Ref = {{ebicite|correct|EBI}} | ChEMBL = 262865 | PubChem= 11584525 | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 9759290 | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI=1S/C22H30N2O2/c1-21(2)20(22(21,3)4)19(25)17-15-24(18-8-6-5-7-16(17)18)10-9-23-11-13-26-14-12-23/h5-8,15,20H,9-14H2,1-4H3 | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = ZCFHOMLAFTWDFM-UHFFFAOYSA-N | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank= | C=22 | H=30 | N=2 | O=2 | molecular_weight = 354.485 g/mol | smiles = C4COCCN4CCn(c3ccccc13)cc1C(=O)C2C(C)(C)C2(C)C | bioavailability= | metabolism = | elimination_half-life= | excretion = | pregnancy_category = | legal_status = | routes_of_administration= }}A-796,260 is a drug developed by Abbott Laboratories that acts as a potent and selective cannabinoid CB2 receptor agonist. Replacing the aromatic 3-benzoyl or 3-naphthoyl group found in most indole derived cannabinoids with the 3-tetramethylcyclopropylmethanone group, imparts significant selectivity for CB2, and A-796,260 was found to be a highly selective CB2 agonist with little affinity for CB1, having a CB2 Ki of 4.6 nM vs 945 nM at CB1.[1] It has potent analgesic and anti-inflammatory actions in animal models, being especially effective in models of neuropathic pain, but without producing cannabis-like behavioral effects.[2] Legal StatusAs of October 2015 A-796,260 is a controlled substance in China.[3] See also
References1. ^{{Cite journal |last1= Frost |first1= J. M. |doi= 10.1021/jm901214q |title= Indol-3-ylcycloalkyl Ketones: Effects of N1 Substituted Indole Side Chain Variations on CB2 Cannabinoid Receptor Activity |journal= Journal of Medicinal Chemistry |volume= 53 |issue= 1 |pages= 295–315 |year= 2010 |pmid= 19921781 |display-authors=etal}} {{Cannabinoids}}{{cannabinoid-stub}}2. ^{{cite journal |author=Yao BB |title=In vitro and in vivo characterization of A-796260: a selective cannabinoid CB2 receptor agonist exhibiting analgesic activity in rodent pain models |journal=British Journal of Pharmacology |volume=153 |issue=2 |pages=390–401 |date=January 2008 |pmid=17994110 |pmc=2219533 |doi=10.1038/sj.bjp.0707568 |display-authors=etal}} 3. ^{{cite web | url=http://www.sfda.gov.cn/WS01/CL0056/130753.html | title=关于印发《非药用类麻醉药品和精神药品列管办法》的通知 | publisher=China Food and Drug Administration | date=27 September 2015 | language=Chinese | accessdate=1 October 2015}} 4 : Cannabinoids|Cyclopropanes|Aminoalkylindoles|Tetramethylcyclopropanoylindoles |
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