Pardoprunox  (Synonyms: SLV-308; DU-126891)

Pardoprunox (SLV-308) is a partial dopamine D2 and D3 receptor partial agonist and a serotonin 5-HT1A receptor agonist, with pEC₅₀s of 8, 9.2, and 6.3, respectively^[1].

Pardoprunox (SLV-308) acts as a potent but partial D2 receptor agonist (pEC₅₀= 8.0 and pA₂=8.4) with an efficacy of 50% on forskolin stimulated cAMP accumulation. At human recombinant dopamine D3 receptors, Pardoprunox acts as a partial agonist in the induction of [(35)S]GTPgammaS binding (intrinsic activity of 67%; pEC₅₀=9.2) and antagonized the dopamine induction of [(35)S]GTPgammaS binding (pA₂=9.0). Pardoprunox acts as a full 5-HT1A receptor agonist on forskolin induced cAMP accumulation at cloned human 5-HT1A receptors but with low potency (pEC₅₀=6.3)^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

233.27

C₁₂H₁₅N₃O₂

269718-84-5

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• [1]. Glennon JC, et al. In vitro characterization of SLV308 (7-[4-methyl-1-piperazinyl]-2(3H)-benzoxazolone, monohydrochloride): a novel partial dopamine D2 and D3 receptor agonist and serotonin 5-HT1A receptor agonist. Synapse. 2006 Dec 15;60(8):599-608.  [Content Brief]

  [2]. Bronzova J, et al. Double-blind study of pardoprunox, a new partial dopamine agonist, in early Parkinson's disease. Mov Disord. 2010 Apr 30;25(6):738-46.  [Content Brief]

  [3]. Bétry C, et al. In vivo effects of pardoprunox (SLV308), a partial D?/D? receptor and 5-HT1A receptor agonist, on rat dopamine and serotonin neuronal activity. Synapse. 2011 Oct;65(10):1042-51.  [Content Brief]