生物活性

• 靶点

  Dopamine Receptor D3 Ki:0.5nM

  Dopamine Receptor D2L Ki:2.2nM

  Dopamine Receptor D2S Ki:3.9nM

  Dopamine Receptor D4 Ki:5.1nM

• 描述Pramipexole (Dihydrochloride) is a nonergolinic dopamine agonist, with high affinity for the D2 subfamily of dopamine receptors. Pramipexole is efficacious for the symptomatic treatment of early Parkinson's Disease (PD) and its early use, before that of levodopa can delay the emergence of levodopa-related motor complication^[3]. Pramipexole is a potent dopamine autoreceptor agonist. Two measurements of receptor activation for dopamine D2, D3, and D4 receptors show that pramipexole is most potent for activation of D3 receptors^[4]. Post-stroke treatment with pramipexole reduced levels of mitochondrial ROS and Ca2+ after ischemia. Pramipexole elevated the mitochondrial membrane potential and mitochondrial oxidative phosphorylation. Thus, post-stroke administration of pramipexole induces the neurological recovery through mitochondrial pathways in ischemia/reperfusion injury^[5]. P-CNs (Pramipexole dihydrochloride loaded chitosan nanoparticles) enhanced antioxidant status in the form of increased superoxide dismutase and catalase activities, along with increased dopamine level in the brain significantly^[6]. Half of the patients stopped the pramipexole an average of 2 months after starting it. For all patients, depressed mood, and the total profile of depressive symptoms improved significantly within 4 weeks and remained significantly improved for as long as 36 weeks^[7].