Open Access Articles- Top Results for SKF-83,959


File:SKF-83959 structure.png
Systematic (IUPAC) name
Clinical data
PubChem CID 24278699
ChemSpider 10131933 7pxY
ChEMBL CHEMBL520992 7pxY
Chemical data
Formula C18H20ClNO2
317.810 g/mol
 14pxY (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]


  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. PMC 1766439. PMID 17194762. doi:10.1073/pnas.0604049104. 
  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. PMID 23295385. doi:10.1124/mol.112.083840. 
  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. PMID 21538463. doi:10.1002/jnr.22653. 
  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. PMC 2690691. PMID 19503734. doi:10.1371/journal.pone.0005811. 

Further reading

  • Lee SM, Yang Y, Mailman RB (2014). "Dopamine D1 receptor signaling: Does GαQ-phospholipase C actually play a role?". J. Pharmacol. Exp. Ther. 351: 9–17. PMID 25052835. doi:10.1124/jpet.114.214411. 
  • Lee SM, Kant A, Blake D et al. (2014). "SKF-83959 is not a highly-biased functionally selective D1 dopamine receptor ligand with activity at phospholipase C". Neuropharmacology 86: 145–54. PMID 24929112. doi:10.1016/j.neuropharm.2014.05.042. 

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