PG 01037 dihydrochloride

Name: PG 01037 dihydrochloride
Brand: Tocris Bioscience
SKU: 3887

Tocris Bioscience, part of Bio-Techne | Catalog # 3887

Citations (2)

COA / SDS

Selective D3 antagonist

Key Product Details

Description:	Selective D₃ antagonist
Chemical Name:	N-[(2E)-4-[4-(2,3-Dichlorophenyl)-1-piperazinyl]-2-buten-1-yl]-4-(2-pyridyl)-benzamide dihydrochloride
Purity:	≥98%
Molecular Weight:	554.34

View Full Technical Details for PG 01037 dihydrochloride

Technical Data
Citations

Biological Activity for PG 01037 dihydrochloride

PG 01037 dihydrochloride is a dopamine D₃ receptor antagonist; 133-fold selective for D₃ over D₂ receptors in vitro (K_i values are 0.70, 93.3 and 375 nM for D₃, D₂ and D₄ receptors respectively). Attenuates abnormal involuntary movements associated with L-DOPA (Cat. No. 3788) in rat models of Parkinson's disease. Inhibits the effects of methamphetamine; attenuates drug-induced behaviors in vivo.

Compound Libraries for PG 01037 dihydrochloride

PG 01037 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for PG 01037 dihydrochloride

M. Wt	554.34
Formula	C₂₆H₂₆Cl₂N₄O.2HCl
Storage	Desiccate at +4°C
Purity	≥98%
CAS Number	675599-62-9
PubChem ID	90488894
InChi Key	DACFFMAXBWGOKQ-CZEFNJPISA-N
Smiles	ClC(C(Cl)=CC=C4)=C4N(CC3)CCN3C/C=C/CNC(C1=CC=C(C2=NC=CC=C2)C=C1)=O.Cl.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for PG 01037 dihydrochloride

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	water	11.09	20 with gentle warming
	DMSO	55.43	100

Preparing Stock Solutions for PG 01037 dihydrochloride

The following data is based on the product molecular weight 554.34.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.80 mL	9.02 mL	18.04 mL
5 mM	0.36 mL	1.80 mL	3.61 mL
10 mM	0.18 mL	0.90 mL	1.80 mL
50 mM	0.04 mL	0.18 mL	0.36 mL

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References for PG 01037 dihydrochloride

References are publications that support the biological activity of the product.

Mason Characterization of the transport, metabolism, and pharmacokinetics of the DA D3 receptor-delective fluorenyl-and 2-pyridylphenyl amides developed for treatment of psychostimulant abuse. J.Pharm.Exp.Ther. 2010 PMID: 20228156
Grundt Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-butyl)arylcarboxamides with functionalized linking chains as novel DA D3 receptor ligands: potential substance abuse therapeutic agents. J.Med.Chem. 2007 PMID: 17672446
Kumar Evaluation of the D3 DA receptor selective antagonist PG01037 on L-dopa-dependent abnormal involuntary movements in rats. Neuropharmacology 2009 PMID: 19371585
Grundt Novel heterocyclic trans olefin analogues of N-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl}arylcarboxamides as selective probes with high affinity for the DA D3 receptor. J.Med.Chem. 2005 PMID: 15689168