Sumanirole maleate - CAS 179386-44-8
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
Dopamine Receptor
Sumanirole maleate, also referred as PNU 95666E or U95666E, is a high affinity D2 receptor full agonist that shows >200-fold selectivity over dopamine receptor subtypes (Ki values are 9.0, 1940, >2190 and >7140 for D2, D3, D4 and D1 receptors respectively)
with an ED50 of about 46 nM.
IC50 value: 46 nM (EC50)
Target: D2 receptor
Sumanirole was developed for the treatment of Parkinson's disease and restless leg syndrome. While it has never been approved for medical use. Sumanirole is a highly valuable tool compound for basic research to identify neurobiological mechanisms that are based on a dopamine D2-linked (vs. D1, D3, D4, and D5-linked) mechanism of action.
Brife Description:
A highly selective D2 receptor full agonist
5,6-dihydro-5-(methylamino)-4H-imidazo(4,5,1ij)-quinolin-2(1H)-one (Z)-2-butenedioate; PNU-95666; PNU95666; PNU 95666; Sumanirole; U 95666E; U-95666E; U95666E
10 mM in DMSO
Store in a cool and dry place (or refer to the Certificate of Analysis).
Canonical SMILES:
1.Sumanirole, a highly dopamine D2-selective receptor agonist: in vitro and in vivo pharmacological characterization and efficacy in animal models of Parkinson's disease.
McCall RB;Lookingland KJ;Bédard PJ;Huff RM J Pharmacol Exp Ther. 2005 Sep;314(3):1248-56. Epub 2005 Jun 24.
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 selectivity for the D(2) receptor subtype versus the other dopamine receptor subtypes in radioligand binding assays. In cell-based assays, sumanirole is a fully efficacious agonist, with EC(50) values between 17 and 75 nM. In animals, sumanirole elicits many physiological responses attributed to D(2)-like receptor function. In rats, sumanirole is a full agonist for elevation of striatal acetylcholine levels (ED(50) = 12.1 micromol/kg i.p.). Sumanirole s.c. dose dependently decreased plasma prolactin levels and depressed dopamine neuron firing rates in the substantia nigra pars compacta with an ED(50) of 2.3 micromol/kg i.v. This high selectivity for D(2) receptors translates into excellent locomotor stimulant activity in animal models of Parkinson's disease. In reserpinized, alpha-methyl-para-tyrosine-treated rats, sumanirole caused a significant and sustained increase in horizontal activity at doses > or =12.
2.Dopamine D3 and D2 receptor mechanisms in the abuse-related behavioral effects of cocaine: studies with preferential antagonists in squirrel monkeys.
Achat-Mendes C;Grundt P;Cao J;Platt DM;Newman AH;Spealman RD J Pharmacol Exp Ther. 2010 Aug;334(2):556-65. doi: 10.1124/jpet.110.167619. Epub 2010 May 21.
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 the degree to which the D3-preferring antagonist PG01037 [N-{4-[4-(2,3-dichlorophenyl)-piperazin- 1-yl]-trans-but-2-enyl}-4-pyridine-2-yl-benzamide HCl] and the D2-preferring antagonist L-741626 [3-[4-(4-chlorophenyl)-4- hydroxypiperidin-1-yl]methyl-1H-indole] attenuated several behavioral effects of cocaine in squirrel monkeys. Quantitative observational studies established doses of each antagonist that did not produce untoward effects, which were used in subsequent comparisons. In addition, the ability of the D3-preferring agonist PD128907 [(R-(+)-trans-3,4a,10b-tetrahydro-4-propyl-2H,5H-[1]benzopyrano[4,3-b]-1,4-oxazin-9-ol)] and the D2-preferring agonist sumanirole [(R)-5,6-dihydro-5-(methylamino)-4H- imidazo[4,5,1-ij]quinolin-2(1H)-one(Z)-2-butenedioate] to reproduce cocaine's discriminative stimulus (DS) and priming effects were compared. In monkeys trained to discriminate cocaine from vehicle, both DA antagonists attenuated and both DA agonists partially reproduced cocaine's DS effects.
3.Asymmetric synthesis of tetrahydroquinolin-3-ols via CoCl2-catalyzed reductive cyclization of nitro cyclic sulfites with NaBH4.
Jagdale AR;Reddy RS;Sudalai A Org Lett. 2009 Feb 19;11(4):803-6. doi: 10.1021/ol8028109.
A new method for the construction of chiral 3-substituted tetrahydroquinoline derivatives based on asymmetric dihydroxylation and CoCl(2)-catalyzed reductive cyclization of nitro cyclic sulfites with NaBH(4) has been described with high optical purities. This method has been successfully applied in the formal synthesis of PNU 95666E and anachelin H chromophore.
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CAS 179386-44-8 Sumanirole maleate

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