U 95666E(Sumanirole maleate)

• Catalog No.: S2191
• CAS Number: 179386-44-8
• M. F.: C15H17N3O5
• M. W.: 319.31258
• Storage: -20°C

SYNONYMS

• IUPAC name: (10R)-10-(methylamino)-1,3-diazatricyclo[6.3.1.0^{4,12}]dodeca-4,6,8(12)-trien-2-one; (2Z)-but-2-enedioic acid
• IUPAC Traditional name: (10R)-10-(methylamino)-1,3-diazatricyclo[6.3.1.0^{4,12}]dodeca-4,6,8(12)-trien-2-one; maleic acid
• Synonyms: PNU 95666; Sumanirole maleate; U95666E

DATABASE IDS

• CAS Number: 179386-44-8

PROPERTIES

• Target: Dopamine Receptor
• Salt Data: maleate
• Storage Condition: -20°C

DETAILS

Description (English)

Research Area: Neurological Disease
Biological Activity:
Sumanirole maleate is a highly selective D2 receptor full agonist with an ED50 of about 46 nM. It 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. In rats, sumanirole is a full agonist for elevation of striatal acetylcholine levels (ED50 = 12.1 μmol/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 ED50 of 2.3 μmol/kg i.v. [1][2]References on U 95666E(Sumanirole maleate)[1] http://en.wikipedia.org/wiki/Sumanirole, , [2] J Pharmacol Exp Ther., 2005 Sep, 314(3):1248-56.

REFERENCES

• McCall RB et al. J Pharmacol Exp Ther. 2005 Sep;314(3):1248-56