269718-84-5
269718-84-5 結(jié)構(gòu)式
基本信息
DU 126891
Pardoprunox
SLV-308
DU-126891
pardoprunox (SLV308)
Pardoprunox，DU 126891
7-(4-Methyl-1-piperazinyl)-2(3H)-benzoxazolone
2(3H)-Benzoxazolone, 7-(4-methyl-1-piperazinyl)-
7-(4-methylpiperazin-1-yl)-3H-1,3-benzoxazol-2-one
物理化學(xué)性質(zhì)
常見(jiàn)問(wèn)題列表
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5-HT 1A Receptor 6.3 (pEC 50 ) |
D 2 Receptor 8 (pEC 50 ) |
D 3 Receptor 9.2 (pEC 50 ) |
Pardoprunox (SLV-308) 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 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 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).