| 词条 | SKF-83,959 |
| 释义 |
| Watchedfields = changed | verifiedrevid = 464385404 | IUPAC_name = 6-chloro-7,8-dihydroxy-3-methyl-1-(3-methylphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepine | image = SKF-83959_structure.png | tradename = | pregnancy_category = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number = | ATC_prefix = | ATC_suffix = | PubChem = 24278699 | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 10131933 | ChEMBL_Ref = {{ebicite|correct|EBI}} | ChEMBL = 520992 | C=18 | H=20 | Cl=1 | N=1 | O=2 | molecular_weight = 317.810 g/mol | smiles = Br.Clc1c3c(cc(O)c1O)C(c2cccc(c2)C)CN(CC3)C | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/C18H20ClNO2.BrH/c1-11-4-3-5-12(8-11)15-10-20(2)7-6-13-14(15)9-16(21)18(22)17(13)19;/h3-5,8-9,15,21-22H,6-7,10H2,1-2H3;1H | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = FHYWNBUFNGHNCP-UHFFFAOYSA-N }}SKF-83,959 is a synthetic benzazepine derivative used in scientific research which acts as an agonist at the D1-D2 dopamine receptor.[1] It behaves as a full agonist at the D1 protomer and a high-affinity partial agonist at the D2 protomer. It was further shown to act as an allosteric modulator of the sigma-1 receptor.[2] SKF-83,959 is a racemate that consists of the R-(+)- and S-(−)-enantiomers MCL 202 and MCL 201, respectively. SKF-83,959 inhibits sodium channels[3] as well as delayed rectifier potassium channels.[4] References1. ^{{cite journal |vauthors=Rashid AJ, So CH, Kong MM, etal |title=D1-D2 dopamine receptor heterooligomers with unique pharmacology are coupled to rapid activation of Gq/11 in the striatum |journal=Proc. Natl. Acad. Sci. U.S.A. |volume=104 |issue=2 |pages=654–9 |year=2007 |pmid=17194762 |pmc=1766439 |doi=10.1073/pnas.0604049104 |url=}} 2. ^{{cite journal |vauthors=Guo L, Zhao J, Jin G, etal |title=SKF83959 is a potent allosteric modulator of sigma-1 receptor |journal=Mol. Pharmacol. |volume=83 |issue=3 |pages=577–86 |year=2013 |pmid=23295385 |doi=10.1124/mol.112.083840 |url=}} 3. ^{{cite journal |vauthors=Chu HY, Wu Q, Zhou S, etal |title=SKF83959 suppresses excitatory synaptic transmission in rat hippocampus via a dopamine receptor-independent mechanism |journal=J. Neurosci. Res. |volume=89 |issue=8 |pages=1259–66 |year=2011 |pmid=21538463 |doi=10.1002/jnr.22653 |url=}} 4. ^{{cite journal |vauthors=Chen XQ, Zhang J, Neumeyer JL, etal |title=Arylbenzazepines are potent modulators for the delayed rectifier K+ channel: a potential mechanism for their neuroprotective effects |journal=PLoS ONE |volume=4 |issue=6 |pages=e5811 |year=2009 |pmid=19503734 |pmc=2690691 |doi=10.1371/journal.pone.0005811 |url=}} Further reading
8 : Benzazepines|GlaxoSmithKline|GlaxoSmithKline brands|Dopamine antagonists|Dopamine agonists|Phenols|Chloroarenes|Receptor heteromer ligands |
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