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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

assay

≥98% (HPLC)

Quality Level

100

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

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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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