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Submit ReviewPG 01037 dihydrochloride
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%
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 (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.
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 Data 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 | 1.8 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 for PG 01037 dihydrochloride
References for PG 01037 dihydrochloride
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 DA 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 DA D3 receptor ligands: potential substance abuse therapeutic agents. J.Med.Chem. 50 4135 PMID: 17672446
Kumar et al (2009) Evaluation of the D3 DA 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 DA D3 receptor-delective fluorenyl-and 2-pyridylphenyl amides developed for treatment of psychostimulant abuse. J.Pharm.Exp.Ther. 333 854 PMID: 20228156
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Keywords: PG 01037 dihydrochloride, PG 01037 dihydrochloride supplier, PG01037, dopamine, receptors, D3, antagonists, dopaminergic, parkinsons, antiparkinsonian, parkinson's, Receptors, 3887, Tocris Bioscience
Citations for PG 01037 dihydrochloride
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Dopamine Receptors Scientific Review
Written by Phillip Strange and revised by Kim Neve in 2013, this review summarizes the history of the dopamine receptors and provides an overview of individual receptor subtype properties, their distribution and identifies ligands which act at each receptor subtype. Compounds available from Tocris are listed.
Addiction Poster
The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.
Parkinson's Disease Poster
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.