SKF 83959

Description

SKF 83959 is a partial agonist at the dopamine D₁-like receptors (K_is = 1.18 and 7.56 nM, respectively, for D₁ and D₅) that is selective over the D₂-like receptors (K_is = 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.

Uses

SKF 83959 is a D1-like partial agonist.

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.

Hazard

A poison.

storage

Store at RT

Raw materials

Preparation Products