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Merck
CN

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:
179386-44-8
分子量:
203.24 (free base basis)
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD09832637
Assay:
≥98% (HPLC)
Form:
solid
Quality level:
100
Storage condition:
OK to freeze
protect from light

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Quality Level

100

SMILES string

[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

assay

≥98% (HPLC)

form

solid

potency

9 nM Ki

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

off-white

solubility

DMSO: 16 mg/mL

storage temp.

−20°C

相关类别

Disclaimer

Toxicity: Standard Handling (A)

General description

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.

Other Notes

Achat-Mendes, C. et al., 2010. J. Pharmacol. Exp. Ther.334, 556.
McCall, R. B. et al., 2005. J. Pharmacol. Exp. Ther.314, 1248.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

法规信息

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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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