PARDOPRUNOX

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 Search

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

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/20434890 | https://www.ncbi.nlm.nih.gov/pubmed/14619412

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 Target	Pharmacology	Potency
Serotonin 1a (5-HT1a) receptor 172 Target ID: CHEMBL214 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20434890	Agonist 2678	8.5 null [pKi]
Dopamine D2 receptor 297 Target ID: CHEMBL217 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20434890	Partial Agonist 290	8.1 null [pKi]
Dopamine D3 receptor 91 Target ID: CHEMBL234 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20434890	Partial Agonist 290	8.6 null [pKi]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Parkinson's disease 226 Sources: https://clinicaltrials.gov/ct2/show/record/NCT00134251	Palliative		Phase III 656	PARDOPRUNOX Approved Use Unknown

Sourcing

Vendor/Aggregator	ID	URL
AstaTech	F17400	http://astatechinc.com/CPSResult.php?CRNO=F17400
AstaTech	F17401	http://astatechinc.com/CPSResult.php?CRNO=F17401
BLD Pharm	BD630605	http://www.bldpharm.com/search/Search.html?keyword=BD630605
BLD Pharm	BD630606	http://www.bldpharm.com/search/Search.html?keyword=BD630606
BOC Sciences	269718-83-4	http://www.bocsci.com/description.asp?cas=269718-83-4
Chem Scene	CS-4869	http://www.chemscene.com/goproductList/searchProductList?productObj=CS-4869
ChemShuttle	169525	https://www.chemshuttle.com/catalogsearch/result/?q=169525
ChemShuttle	169526	https://www.chemshuttle.com/catalogsearch/result/?q=169526
Excenen	EX-A624	http://www.excenen.com/searchresultlist.php?id=EX-A624
Excenen	EX-A876	http://www.excenen.com/searchresultlist.php?id=EX-A876
Lab Network	LN01342376	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01342376
Lab Network	LN01342727	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01342727
MedChem Express	HY-14958A	https://www.medchemexpress.com/search.html?q=HY-14958A&ft=&fa=&fp=
MolPort	MolPort-005-942-398	https://www.molport.com/shop/molecule-link/MolPort-005-942-398
MolPort	MolPort-046-033-556	https://www.molport.com/shop/molecule-link/MolPort-046-033-556
Molnova	M13825	https://www.molnova.com/en/serch-list.html?keywords=M13825
MuseChem	I008555	https://www.musechem.com/product/I008555.html
MuseChem	I008556	https://www.musechem.com/product/I008556.html
ShangHai Biochempartner	BCP17730	http://www.biochempartner.com/search_BCP17730
ShangHai Biochempartner	BCP17731	http://www.biochempartner.com/search_BCP17731
Toronto Research Chemicals	P205908	https://www.trc-canada.com/product-detail/?CatNum=P205908
eMolecules	295160819	https://orderbb.emolecules.com/search/#?query=295160819
eMolecules	72973047	https://orderbb.emolecules.com/search/#?query=72973047
eMolecules	72973400	https://orderbb.emolecules.com/search/#?query=72973400
mcule	MCULE-1900469117	https://mcule.com/MCULE-1900469117/
mcule	MCULE-4456662339	https://mcule.com/MCULE-4456662339/

PubMed

Title	Date	PubMed
New frontiers in the pharmacological management of Parkinson's disease.	2008 Jul	18806903
Safety and tolerability of pardoprunox, a new partial dopamine agonist, in a randomized, controlled study of patients with advanced Parkinson's disease.	2009	19407454
Double-blind study of pardoprunox, a new partial dopamine agonist, in early Parkinson's disease.	2010 Apr 30	20198713
The Movement Disorder Society--14th International Congress of Parkinson's Disease and Movement Disorders.	2010 Aug	20721824
An in vivo pharmacological evaluation of pardoprunox (SLV308)--a novel combined dopamine D(2)/D(3) receptor partial agonist and 5-HT(1A) receptor agonist with efficacy in experimental models of Parkinson's disease.	2010 Aug	20434890
The partial dopamine agonist pardoprunox (SLV308) administered in combination with l-dopa improves efficacy and decreases dyskinesia in MPTP treated common marmosets.	2010 Dec	20843474
Pardoprunox reverses motor deficits but induces only mild dyskinesia in MPTP-treated common marmosets.	2010 Oct 15	20721904

Patents

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).

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

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Name

Type

Language

PARDOPRUNOX

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