SKF 83959 hydrobromide

개요SKF 83959 is a partial agonist at the dopamine D1-like receptors (Kis = 1.18 and 7.56 nM, respectively, for D1 and D5) that is selective over the D2-like receptors (Kis = 920 and 399 nM, respectively, for D2 and D3). It is protective against oxidative stress in retinal ganglion cells after hydrogen peroxide-induced injury in vitro. In a rat methylazoxymethanol acetate (MAM) model of schizophrenia, it had positive effects on hippocampal function, determined using electrophysiology, but impaired spatial learning. SKF 83959 can also act as an allosteric modulator of the sigma-1 (σ1) receptor by enhancing the binding to and delaying the dissociation of the selective σ1-receptor agonist pentazocine.

용도SKF 83959 is a D1-like partial agonist.

정의ChEBI: A hydrobromide salt prepared from N-methyl-6-chloro-1-(3-methylphenyl)-2,3,4,5-tetrahydro-3-benzazepine-7,8-diol and one equivalent of hydrogen bromide. Dopamine D1-like receptor partial agonist (Ki values are 1.18, 7.56, 920 and 399 nM or rat D1, D5, D2 and D3 receptors respectively). May act as an antagonist in vivo, producing anti-Parkinsonian effects and antagonising the behavioral effects of cocaine.