5.05896
Sumanirole Maleate
别名:
Sumanirole Maleate, Dopamine D₂ receptor Agonist, Sumanirole, PNU 95666, PNU95666
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关于此项目
经验公式(希尔记法):
C11H13N3O · xC4H4O4
化学文摘社编号:
分子量:
203.24 (free base basis)
MDL编号:
UNSPSC代码:
12352200
NACRES:
NA.77
方案
≥98% (HPLC)
质量水平
表单
solid
效能
9 nM Ki
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
off-white
溶解性
DMSO: 16 mg/mL
储存温度
−20°C
SMILES字符串
[n]21c3c([nH][c]2=O)cccc3C[C@H](C1)NC.OC(=O)\C=C/C(=O)O
InChI
1S/C11H13N3O.C4H4O4/c1-12-8-5-7-3-2-4-9-10(7)14(6-8)11(15)13-9;5-3(6)1-2-4(7)8/h2-4,8,12H,5-6H2,1H3,(H,13,15);1-2H,(H,5,6)(H,7,8)/b;2-1-/t8-;/m1./s1
InChI key
VOJRMYBBPKNLLI-ORHWHDKWSA-N
相关类别
一般描述
An extremely selective dopamine D2 receptor agonist (Ki = 9 nM). Commonly used in Parkinson′s Disease models and to reproduce cocaine′s discriminative stimulus effects. Sumanirole has greater than 200-fold selectivity for the D2 receptor subtype versus the other dopamine receptor subtypes in radioligand binding assays. In cell-based assays, sumanirole is a fully efficacious agonist, with EC50 values between 17 and 75 nM. In animals, sumanirole elicits many physiological responses attributed to D2-like receptor function.
其他说明
Achat-Mendes, C. et al., 2010. J. Pharmacol. Exp. Ther.334, 556.
McCall, R. B. et al., 2005. J. Pharmacol. Exp. Ther.314, 1248.
McCall, R. B. et al., 2005. J. Pharmacol. Exp. Ther.314, 1248.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
免责声明
Toxicity: Standard Handling (A)
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
此项目有
Robert B McCall et al.
The Journal of pharmacology and experimental therapeutics, 314(3), 1248-1256 (2005-06-28)
The purpose of this study is to demonstrate that sumanirole is a novel dopamine receptor agonist with high in vitro and in vivo selectivity for the D(2) receptor subtype. Sumanirole, (R)-5,6-dihydro-5-(methylamino)-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one (Z)-2-butenedioate (1:1), is unique; it has greater than 200-fold
Cindy Achat-Mendes et al.
The Journal of pharmacology and experimental therapeutics, 334(2), 556-565 (2010-05-25)
Dopamine (DA) D3 and D2 receptor mechanisms are implicated in cocaine's abuse-related behavioral effects, but the relative contribution of the two receptor subtypes is only partially characterized. This study investigated the role of D3 and D2 subtype mechanisms by determining
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