SKF-83,959

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SKF-83,959
SKF-83959 structure.png
Identifiers
PubChem CID
ChemSpider
ChEMBL
Chemical and physical data
Formula C18H20ClNO2
Molar mass 317.810 g/mol
3D model (Jmol)
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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]

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 1766439Freely accessible. 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 2690691Freely accessible. PMID 19503734. 

Further reading[edit]

  • 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. doi:10.1124/jpet.114.214411. PMID 25052835. 
  • 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. doi:10.1016/j.neuropharm.2014.05.042. PMID 24929112. 


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