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Cat. No. Name Size Price Add Cart
KI1432U 95666E5 mg$272
U 95666E10 mg$512
U 95666E50 mg$1552
U 95666E200 mg$3952

Chemical Characteristic

Product NameU 95666E
SynonymsSumanirole maleate
CAS No.179386-44-8
Molecular Weight 319.31
FormulaC11H13N3O.C4H4O4
Chemical Name(R)-5-(methylamino)-5,6-dihydro-1H-imidazo[4,5,1-ij]quinolin-2(4H)-one maleate
Smilesn12C[C@@H](Cc3cccc(c13)[nH]c2=O)NC C(=O)(/C=C\C(=O)O)O
Chemical Structure

Biological activities

Sumanirole maleate is a maleate of sumanirole. Sumanirole maleate is a selective D2 receptor agonist. The affinity of sumanirole for D2 receptor is 9.0 nM. Sumanirole has moderate affinity at the 5-HT1A receptor with a Ki of 95 nM. 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 an EC50 ranging from 17 to 75 nM. In vivo, sumanirole elicits many physiological responses attributed to D2-like receptor function. In rats, sumanirole is a full agonist for elevation of striatal acetylcholine levels with an ED50 of 12.1 mM/kg i.p.. Sumanirole s.c. dose dependently decreases plasma prolactin levels and depresses dopamine neuron firing rates in the substantia nigra pars compacta with an ED50 of 2.3 mmol/kg i.v.[1] Sumanirole maleate dose-dependently increases striatal ACh concentration both in the non-reserpinized and resetpinized rats. Sumanirole maleate also has anxiolytic activity in mice. Sumanirole maleate (3 pmol/kg po) time dependently decreases cerebellar cGMP. Pretreatment with sumanirole maleate dose-dependently attenuates stress-induced elevation in cGMP. [2] Sumanirole decreases prepulse inhibition (PPI) at 60-120 ms prepulse intervals, and increases PPI at 10-20 ms intervals. [3]

Protocols

Sumanirole maleate is dissolved in either distilled water or 0.25% methylcelhtlose sohnion. [2]

References

[1] McCall RB, et al. Sumanirole, a highly dopamine D2-selective receptor agonist: in vitro and in vivo pharmacological characterization and efficacy in animal models of Parkinson's disease. J Pharmacol Exp Ther. 2005, 314(3): 1248-1256.
[2] Sethy VH, U-95666E: a potential anti-parkinsonian drug with anxiolytic activity. Prog Neuropsychopharmacol Biol Psychiatry. 1997, 21(5): 873-883.
[3] Weber M, The effects of the dopamine D2 agonist sumanirole on prepulse inhibition in rats. Eur Neuropsychopharmacol. 2010, 20(6): 421-425.

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