Acute activation of κ opioid (KOP) receptors results in anticocaine-like effects, but adverse effects, such as dysphoria, aversion, sedation and depression, limit their clinical development. Salvinorin A, isolated from the plant Salvia divinorum, and its semi-synthetic analogues have been shown to have potent KOP receptor agonist activity and may induce a unique response with similar...
Salvinorin A (SalA), a selective κ-opioid receptor (KOR) agonist, produces dysphoria and pro-depressant like effects. These actions have been attributed to inhibition of striatal dopamine release. The dopamine transporter (DAT) regulates dopamine transmission via uptake of released neurotransmitter. KORs are apposed to DAT in dopamine nerve terminals suggesting an additional target by which...
Classic kappa opioid receptor (KOPr) agonists have shown anti-addictive properties in rat models of addiction (Heidbreder et al. 1998; Schenk et al. 1999; Sun et al. 2010), and this has been shown to be partially through modulation of dopamine and serotonin in the synapse (Thompson et al. 2000; Zhang et al. 2004; Zakharova et al. 2008a). However, they have side effects such as depression and...