SKF-83,959
SKF-83,959 is a synthetic benzazepine derivative used in scientific research which acts as an agonist at the D1-D2 dopamine receptor. It behaves as a full agonist at the D1protomer 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 is a racemate that consists of the R-(+)- and S-(−)-enantiomers MCL 202 and MCL 201, respectively. SKF-83,959 inhibits sodium channels as well as delayed rectifier potassium channels.
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: 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.