PG 01037 dihydrochloride
Tocris Bioscience, part of Bio-Techne | Catalog # 3887
Selective D3 antagonist
Product Description
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.Product Specifications
Molecular Weight
554.34
Formula
C26H26Cl2N4O.2HCl
Storage
Desiccate at +4°C
Purity
≥98%
Chemical Name
N-[(2E)-4-[4-(2,3-Dichlorophenyl)-1-piperazinyl]-2-buten-1-yl]-4-(2-pyridyl)-benzamide dihydrochloride
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.
Solubility
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
Product Specific Notices for PG 01037 dihydrochloride
For research use only
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