PG 01037 dihydrochloride

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Cat.No. 3887 - PG 01037 dihydrochloride | C26H26Cl2N4O.2HCl | CAS No. 675599-62-9
Description: D3 receptor selective antagonist
Chemical Name: N-[(2E)-4-[4-(2,3-Dichlorophenyl)-1-piperazinyl]-2-buten-1-yl]-4-(2-pyridyl)-benzamide dihydrochloride
Purity: ≥98%
Datasheet
Citations
Reviews
Literature

Biological Activity

Dopamine D3 receptor antagonist; 133-fold selective for D3 over D2 receptors in vitro (Ki 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.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 554.34. Batch specific molecular weights may vary from batch to batch due to solvent 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 1.8 mL 9.02 mL 18.04 mL
5 mM 0.36 mL 1.8 mL 3.61 mL
10 mM 0.18 mL 0.9 mL 1.8 mL
50 mM 0.04 mL 0.18 mL 0.36 mL

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Product Datasheets

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References

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

Grundt et al (2005) 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 dopamine D3 receptor. J.Med.Chem. 48 839 PMID: 15689168

Grundt et al (2007) Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3 receptor ligands: potential substance abuse therapeutic agents. J.Med.Chem. 50 4135 PMID: 17672446

Kumar et al (2009) Evaluation of the D3 dopamine receptor selective antagonist PG01037 on L-dopa-dependent abnormal involuntary movements in rats. Neuropharmacology 56 944 PMID: 19371585

Mason et al (2010) Characterization of the transport, metabolism, and pharmacokinetics of the dopamine D3 receptor-delective fluorenyl-and 2-pyridylphenyl amides developed for treatment of psychostimulant abuse. J.Pharm.Exp.Ther. 333 854


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Literature in this Area

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