PG 01037 dihydrochloride

Catalog # Availability Size / Price Qty
3887/10
3887/50
Dopamine D3 Receptor Antagonists Small Molecule
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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%

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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
Solubility:
Soluble to 20 mM in water with gentle warming and to 100 mM in DMSO
Purity:
≥98%
Storage:
Desiccate at +4°C
CAS No:
675599-62-9

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.

Background References

  1. 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.
    Grundt et al.
    J.Med.Chem., 2005;48:839
  2. 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.
    Grundt et al.
    J.Med.Chem., 2007;50:4135
  3. Evaluation of the D3 DA receptor selective antagonist PG01037 on L-dopa-dependent abnormal involuntary movements in rats.
    Kumar et al.
    Neuropharmacology, 2009;56:944
  4. Characterization of the transport, metabolism, and pharmacokinetics of the DA D3 receptor-delective fluorenyl-and 2-pyridylphenyl amides developed for treatment of psychostimulant abuse.
    Mason et al.
    J.Pharm.Exp.Ther., 2010;333:854

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