Sumanirole (maleate)

Sumanirole is a dopamine D2 receptor agonist that is selective for D2 over D1, D3, and D4 receptors (Kis = 9.0, >7,140, 1,940, and >2,190 nM, respectively). It inhibits forskolin-stimulated cAMP accumulation in CHO cells expressing human recombinant D2A receptors (EC50 = 17 nM). Sumanirole decreases plasma prolactin levels in rats when administered at doses greater than or equal to 3.1 µmol/kg and inhibits dopamine neuron firing in the substantia nigra pars compacta (SNPC) in anesthetized rats (ED50 = 2.3 µmol/kg). Sumanirole (>12.5 µmol/kg, s.c.) increases horizontal locomotor activity in a reserpinized, alpha-methyl-para-tyrosine (AMPT) rat model of Parkinson's disease. It also decreases time spent in the open arms of the elevated plus maze and time spent immobile in the forced swim test, indicating anxiolytic- and antidepressant-like activities, respectively, in mice with SNPC lesions when administered at a dose of 0.1 mg/kg. Sumanirole (>0.1 mg/kg, s.c.) reduces premature responding, a measure of impulsivity, by rats in the 5-choice serial reaction time test (5CRTT) compared with untreated animals.Formal Name: (5R)-5,6-dihydro-5-(methylamino)-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one, 2Z-butenedioate. CAS Number: 179386-44-8. Synonyms: PNU 95666. Molecular Formula: C11H13N3O . C4H4O4. Formula Weight: 319.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 12.5 mg/ml, DMSO: 16 mg/ml, PBS (pH 7.2): 5 mg/ml. lambdamax: 210, 283 nm. SMILES: O=C(N1)N2C3=C1C=CC=C3C[C@@H](NC)C2.O=C(O)/C=C\C(O)=O. InChi Code: 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.