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Details

Stereochemistry ACHIRAL
Molecular Formula C12H15N3O2.ClH
Molecular Weight 269.727
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of PARDOPRUNOX HYDROCHLORIDE

SMILES

Cl.CN1CCN(CC1)C2=C3OC(=O)NC3=CC=C2

InChI

InChIKey=NQRIKTDKFHAOKC-UHFFFAOYSA-N
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

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Description

Pardoprunox is a partial D2/3 dopamine receptor agonist and full 5-HT1A serotonin receptor agonist. Partial D(2/3) dopamine (DA) receptor agonists provide a novel approach to the treatment of the motor symptoms of Parkinson's disease that may avoid common dopaminergic side effects, including dyskinesia and psychosis. Pardoprunox passed phase III clinical trial for the treatment of Parkinson's disease.

CNS Activity

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
8.5 null [pKi]
8.1 null [pKi]
8.6 null [pKi]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Palliative
PARDOPRUNOX

PubMed

Sample Use Guides

In Vivo Use Guide
Pardoprunox was titrated to each patient’s optimal dose (9–45 mg/d) over 2 to 6 weeks and then maintained at this dose for a further 3 weeks.
Route of Administration: Oral
In Vitro Use Guide
At cloned human dopamine D2 receptors, pardoprunox (SLV308) acted as a potent but partial agonist (pEC50 = 8.0) with an efficacy of 50% on forskolin-stimulated cAMP accumulation. At human recombinant dopamine D3 receptors, SLV308 acted as a partial agonist in the induction of [(35)S]GTPgammaS binding (an intrinsic activity of 67%; pEC50 = 9.2). SLV308 acted as a full 5-HT1A receptor agonist on forskolin-induced cAMP accumulation at cloned human 5-HT1A receptors but with low potency (pEC50 = 6.3).