Pardoprunox (hydrochloride)

Pardoprunox is a partial agonist of dopamine D2 and D3 receptors (EC50s = 10 and 0.63 nM, respectively) and a full agonist of the serotonin (5-HT) receptor subtype 5-HT1A (EC50 = 501 nM) in radioligand binding assays. It is selective for dopamine D2 and D3 and 5-HT1A receptors over a panel of neurotransmitter receptors (Kis = >1,000 nM). Pardoprunox reduces the accumulation of cAMP induced by forskolin (Cay-11018) in a concentration-dependent manner and blocks quinpirole-induced inhibition of dopamine release (pA2 = 8.5) in rat striatal slices. Pardoprunox increases contralateral turning behavior in a 6-OHDA rat model of Parkinson's disease (ED50 = 0.03 mg/kg). It also reduces hyperlocomotion induced by amphetamine (Cay-14204, Cay-15650, Cay-ISO60188) and induces 5-HT1A-mediated flat body posturing and lower lip retraction in rats. Pardoprunox (0.01-0.3 mg/kg) increases locomotor activity in a marmoset model of Parkinson's disease induced by MPTP in a dose-dependent manner. Formulations containing pardoprunox are under clinical investigation for the treatment of Parkinson's disease-associated motor fluctuations.Formal Name: 7-(4-methyl-1-piperazinyl)-2(3H)-benzoxazolone, monohydrochloride. CAS Number: 269718-83-4. Synonyms: DU-126891, SLV 308. Molecular Formula: C12H15N3O2 . HCl. Formula Weight: 269.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 1 mg/ml, DMSO: 5 mg/ml, Ethanol: 0.1 mg/ml, PBS (pH 7.2): 5 mg/ml. lambdamax: 219 nm. SMILES: CN1CCN(C2=CC=CC(N3)=C2OC3=O)CC1.Cl. InChi Code: InChI=1S/C12H15N3O2.ClH/c1-14-5-7-15(8-6-14)10-4-2-3-9-11(10)17-12(16)13-9,/h2-4H,5-8H2,1H3,(H,13,16),1H. InChi Key: NQRIKTDKFHAOKC-UHFFFAOYSA-N.