SKF-83,959

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SKF-83,959
SKF-83959 structure.png
Systematic (IUPAC) name
6-chloro-7,8-dihydroxy-3-methyl-1-(3-methylphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepine
Clinical data
Legal status ?
Identifiers
ATC code ?
PubChem CID 24278699
ChemSpider 10131933 YesY
ChEMBL CHEMBL520992 YesY
Chemical data
Formula C18H20ClNO2 
Mol. mass 317.810 g/mol
 YesY (what is this?)  (verify)

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]

SNDRI[edit]

A recent article reported this compound is a SNDRI (TRI).[5]

References[edit]

  1. ^ Rashid AJ, So CH, Kong MM, et al. (2007). "D1-D2 dopamine receptor heterooligomers with unique pharmacology are coupled to rapid activation of Gq/11 in the striatum". Proc. Natl. Acad. Sci. U.S.A. 104 (2): 654–9. doi:10.1073/pnas.0604049104. PMC 1766439. PMID 17194762. 
  2. ^ Guo L, Zhao J, Jin G, et al. (2013). "SKF83959 is a potent allosteric modulator of sigma-1 receptor". Mol. Pharmacol. 83 (3): 577–86. doi:10.1124/mol.112.083840. PMID 23295385. 
  3. ^ Chu HY, Wu Q, Zhou S, et al. (2011). "SKF83959 suppresses excitatory synaptic transmission in rat hippocampus via a dopamine receptor-independent mechanism". J. Neurosci. Res. 89 (8): 1259–66. doi:10.1002/jnr.22653. PMID 21538463. 
  4. ^ Chen XQ, Zhang J, Neumeyer JL, et al. (2009). "Arylbenzazepines are potent modulators for the delayed rectifier K+ channel: a potential mechanism for their neuroprotective effects". PLoS ONE 4 (6): e5811. doi:10.1371/journal.pone.0005811. PMC 2690691. PMID 19503734. 
  5. ^ Fang, X.; Guo, L.; Jia, J.; Jin, G. Z.; Zhao, B.; Zheng, Y. Y.; Li, J. Q.; Zhang, A.; Zhen, X. C. (2013). "SKF83959 is a novel triple reuptake inhibitor that elicits anti-depressant activity". Acta Pharmacologica Sinica 34 (9): 1149–55. doi:10.1038/aps.2013.66. PMID 23892272.  edit