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SKF 83959 (CAS 67287-95-0)

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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]

Jump up^ 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.
Jump up^ 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.
Jump up^ 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.
Jump up^ 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.