SKF-83,959, a synthetic benzazepine derivative used in scientific research, acts as an agonist at the D1–D2 dopamine receptor heteromer. 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. SKF-83,959 additionally inhibits sodium channels as well as delayed rectifier potassium channels. SKF-83,959 is a racemate that consists of the R-( )- and S-(−)-enantiomers MCL-202 and MCL-201, respectively.
SKF-83,959 was described as a SNDRI. The synthesis has been described.
References
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 (1): 9–17. doi:10.1124/jpet.114.214411. PMC 4165024. 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. PMC 4188748. PMID 24929112.
