Pardoprunox
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CAS No. | 269718-84-5 | Cat. No. | BCP17731 |
Name | Pardoprunox | ||
Synonyms | SLV-308;SLV308;SLV 308;DU-126891;DU126891;DU 126891; | ||
SMILES | |||
Chemical Name | |||
Formula | C12H15N3O2 | M. Wt | 233.27 |
Purity | 98% | Storage | Store at 4-8°C |
Description | in vitro: SLV308 acted as a potent but partial D(2) receptor agonist (pEC(50) = 8.0 and pA(2) = 8.4) with an efficacy of 50% on forskolin stimulated cAMP accumulation. At human recombinant dopamine D(3) receptors, SLV308 acted as a partial agonist in the induction of [(35)S]GTPgammaS binding (intrinsic activity of 67%; pEC(50) = 9.2) and antagonized the dopamine induction of [(35)S]GTPgammaS binding (pA(2) = 9.0). SLV308 acted as a full 5-HT(1) (A) receptor agonist on forskolin induced cAMP accumulation at cloned human 5-HT(1) (A) receptors but with low potency (pEC(50) = 6.3) . in vivo: Unified PD Rating Scale (UPDRS)-Motor score was improved in pardoprunox-treated patients (overall mean dose 23.8 mg/d; -7.3 points), as compared with placebo (-3.0 points; P = 0.0001), from baseline to end point. At end point, there were more responders (> or = 30% reduction in UPDRS-Motor score) in the pardoprunox group (50.7%) than in the placebo group (15.7%; P < 0.0001) . Surprisingly in the SNc, p |
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