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5.05896

Sumanirole Maleate

Name: Sumanirole Maleate
Brand: MM

Synonym(s):

Sumanirole Maleate, Dopamine D₂ receptor Agonist, Sumanirole, PNU 95666, PNU95666

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About This Item

Empirical Formula (Hill Notation):

C₁₁H₁₃N₃O · xC₄H₄O₄

CAS Number:

179386-44-8

Molecular Weight:

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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Properties

Quality Level

100

assay

≥98% (HPLC)

form

solid

potency

9 nM K_i

manufacturer/tradename

Calbiochem^®

storage condition

OK to freeze, protect from light

color

off-white

solubility

DMSO: 16 mg/mL

storage temp.

−20°C

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

Description

General description

An extremely selective dopamine D₂ receptor agonist (K_i = 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

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Information

新产品

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Sumanirole, a highly dopamine D2-selective receptor agonist: in vitro and in vivo pharmacological characterization and efficacy in animal models of Parkinson's disease.

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

Dopamine D3 and D2 receptor mechanisms in the abuse-related behavioral effects of cocaine: studies with preferential antagonists in squirrel monkeys.

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

Global Trade Item Number

SKU	GTIN
5058960001	04055977262506