Description
SKF 83959 is a partial agonist at the dopamine D
1-like receptors (K
is = 1.18 and 7.56 nM, respectively, for D
1 and D
5) that is selective over the D
2-like receptors (K
is = 920 and 399 nM, respectively, for D
2 and D
3). 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 (σ
1) receptor by enhancing the binding to and delaying the dissociation of the selective σ
1-receptor agonist pentazocine.
Definition
ChEBI: 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.
