盐酸帕多芦诺

中文名称:

盐酸帕多芦诺

中文同义词:

帕多芦诺盐酸盐;盐酸帕多芦诺

英文名称:

2(3H)-BENZOXAZOLONE, 7-(4-METHYL-1-PIPERAZINYL)-, MONOHYDROCHLORIDE

英文同义词:

Pardoprunox (hydrochloride);pardoprunox.HCl;Pardoprunox.HCl(SLV-308);SLV-308 hydrochloride;2(3H)-BENZOXAZOLONE, 7-(4-METHYL-1-PIPERAZINYL)-, MONOHYDROCHLORIDE;DU-126891 hydrochloride;SLV-308 HYDROCHLORIDE; DU-126891 HYDROCHLORIDE;SLV308;SLV 308;pardoprunox.HCl.H2O

CAS号:

269718-83-4

分子式:

C12H16ClN3O2

分子量:

269.72734

EINECS号:

相关类别:

医药

Mol文件:

269718-83-4.mol

储存条件 

Inert atmosphere,2-8°C

生物活性

Pardoprunox hydrochloride (DU-126891, SME-308)是一种有效的部分 dopamine D2 receptor 的激动剂，对应的pEC50值为8.0，也是诱导 [35S]GTPγS binding 的部分激动剂，对应的pEC50值为9.2，和 serotonin 5-HT1A receptor 的激动剂，pEC50值为6.3。

靶点

Target Value [ (Cell-free assay) 9.2(pEC50) D2 receptor (Cell-free assay) 8.0(pEC50) 5-HT1A receptor (Cell-free assay) 6.3(pEC50)

Target

Value

[ (Cell-free assay)

9.2(pEC50)

D2 receptor (Cell-free assay)

8.0(pEC50)

5-HT1A receptor (Cell-free assay)

6.3(pEC50)

体外研究

Pardoprunox (SLV-308) hydrochloride acts as a potent but partial D2 receptor agonist (pEC 50 = 8.0 and pA 2 =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%; pEC 50 =9.2) and antagonized the dopamine induction of [(35)S]GTPgammaS binding (pA 2 =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 (pEC 50 =6.3).