Pardoprunox hydrochloride

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 Hydrochloride 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 hydrochloride 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 and 5-HT1A receptor (pKi = 8.5) full agonist.(In Vitro):Pardoprunox (SLV-308) hydrochloride 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 hydrochloride 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 hydrochloride 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).

Pardoprunox (SLV-308) hydrochloride 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 hydrochloride 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 hydrochloride 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).

——

SLV-308 hydrochloride | DU-126891 hydrochloride

MAPK/ERK Signaling

p38 MAPK

5-HT1A| D2| D3

Neurological Disease

——

269718-83-4

269.73

C12H16ClN3O2

>98% (HPLC)

H2O : < 0.1 mg/mL

O=c1oc2c(N3CCN(C)CC3)cccc2[nH]1.Cl.Cl

——

(-20℃)

With Ice Pack

≥ 2 years