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Details

Stereochemistry ACHIRAL
Molecular Formula C12H15N3O2
Molecular Weight 233.2664
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of PARDOPRUNOX

SMILES

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

InChI

InChIKey=YVPUUUDAZYFFQT-UHFFFAOYSA-N
InChI=1S/C12H15N3O2/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)

HIDE SMILES / InChI

Molecular Formula C12H15N3O2
Molecular Weight 233.2664
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

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.

Approval Year

Targets

Targets

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

Conditions

ConditionModalityTargetsHighest PhaseProduct
Palliative
PARDOPRUNOX

Approved Use

Unknown
Sourcing

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
Double-blind study of pardoprunox, a new partial dopamine agonist, in early Parkinson's disease.
2010 Apr 30
The partial dopamine agonist pardoprunox (SLV308) administered in combination with l-dopa improves efficacy and decreases dyskinesia in MPTP treated common marmosets.
2010 Dec
Patents

Sample Use Guides

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
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).
Substance Class Chemical
Created
by admin
on Fri Dec 15 16:29:29 UTC 2023
Edited
by admin
on Fri Dec 15 16:29:29 UTC 2023
Record UNII
5R72CHP32S
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
PARDOPRUNOX
INN   USAN   WHO-DD  
USAN   INN  
Official Name English
7-(4-Methylpiperazin-1-yl)-1,3-benzoxazol-2(3H)-one
Systematic Name English
SLV-308
Code English
PARDOPRUNOX [USAN]
Common Name English
SLV308
Code English
pardoprunox [INN]
Common Name English
2(3H)-BENZOXAZOLONE, 7-(4-METHYL-1-PIPERAZINYL)-
Systematic Name English
Pardoprunox [WHO-DD]
Common Name English
DU-126891
Code English
DU126891
Code English
Classification Tree Code System Code
NCI_THESAURUS C47794
Created by admin on Fri Dec 15 16:29:29 UTC 2023 , Edited by admin on Fri Dec 15 16:29:29 UTC 2023
NCI_THESAURUS C66884
Created by admin on Fri Dec 15 16:29:29 UTC 2023 , Edited by admin on Fri Dec 15 16:29:29 UTC 2023
Code System Code Type Description
EPA CompTox
DTXSID40949747
Created by admin on Fri Dec 15 16:29:29 UTC 2023 , Edited by admin on Fri Dec 15 16:29:29 UTC 2023
PRIMARY
CAS
269718-84-5
Created by admin on Fri Dec 15 16:29:29 UTC 2023 , Edited by admin on Fri Dec 15 16:29:29 UTC 2023
PRIMARY
PUBCHEM
6918525
Created by admin on Fri Dec 15 16:29:29 UTC 2023 , Edited by admin on Fri Dec 15 16:29:29 UTC 2023
PRIMARY
EVMPD
SUB129672
Created by admin on Fri Dec 15 16:29:29 UTC 2023 , Edited by admin on Fri Dec 15 16:29:29 UTC 2023
PRIMARY
WIKIPEDIA
Pardoprunox
Created by admin on Fri Dec 15 16:29:29 UTC 2023 , Edited by admin on Fri Dec 15 16:29:29 UTC 2023
PRIMARY
USAN
UU-83
Created by admin on Fri Dec 15 16:29:29 UTC 2023 , Edited by admin on Fri Dec 15 16:29:29 UTC 2023
PRIMARY
NCI_THESAURUS
C80765
Created by admin on Fri Dec 15 16:29:29 UTC 2023 , Edited by admin on Fri Dec 15 16:29:29 UTC 2023
PRIMARY
SMS_ID
100000155636
Created by admin on Fri Dec 15 16:29:29 UTC 2023 , Edited by admin on Fri Dec 15 16:29:29 UTC 2023
PRIMARY
ChEMBL
CHEMBL2103832
Created by admin on Fri Dec 15 16:29:29 UTC 2023 , Edited by admin on Fri Dec 15 16:29:29 UTC 2023
PRIMARY
MESH
C480679
Created by admin on Fri Dec 15 16:29:29 UTC 2023 , Edited by admin on Fri Dec 15 16:29:29 UTC 2023
PRIMARY
DRUG BANK
DB12061
Created by admin on Fri Dec 15 16:29:29 UTC 2023 , Edited by admin on Fri Dec 15 16:29:29 UTC 2023
PRIMARY
INN
8727
Created by admin on Fri Dec 15 16:29:29 UTC 2023 , Edited by admin on Fri Dec 15 16:29:29 UTC 2023
PRIMARY
FDA UNII
5R72CHP32S
Created by admin on Fri Dec 15 16:29:29 UTC 2023 , Edited by admin on Fri Dec 15 16:29:29 UTC 2023
PRIMARY
Related Record Type Details
TARGET -> AGONIST
SALT/SOLVATE -> PARENT
TARGET->PARTIAL AGONIST
TARGET->PARTIAL AGONIST
Related Record Type Details
ACTIVE MOIETY