Pardoprunox

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Pardoprunox(SLV-308) 是一种新型部分多巴胺 D2 和 D3 受体激动剂和血清素 5-HT1A 受体激动剂。

Pardoprunox(SLV-308) is a novel partial dopamine D2 and D3 receptor agonist and serotonin 5-HT1A receptor agonist; D2 (pKi = 8.1) and D3 receptor (pKi = 8.6) partial agonist (IA = 50% and 67%, respectively) and 5-HT1A receptor (pKi = 8.5) full agonist (IA = 100%); also binds to D4 (pKi = 7.8), α1-adrenergic (pKi = 7.8), α2-adrenergic (pKi = 7.4), and 5-HT7 receptors (pKi = 7.2) with lower affinity.

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).

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Endocrinology/Hormones

5-HT Receptor

5-HT1A| α2-adrenergic receptor| D2| D3

Neurological Disease

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269718-84-5

233.27

C12H15N3O2

>98% (HPLC)

DMSO: 10 mM

CN1CCN(CC1)C1=CC=CC2=C1OC(=O)N2

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(-20℃)

With Ice Pack

≥ 2 years