PG 01037 dihydrochloride

Cat. No. 3887

PG 01037 dihydrochloride C26H26Cl2N4O.2HCl [675599-62-9]

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Chemical Name: N-[(2E)-4-[4-(2,3-Dichlorophenyl)-1-piperazinyl]-2-buten-1-yl]-4-(2-pyridyl)-benzamide dihydrochloride

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.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

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.

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.

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.

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.

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Keywords: PG 01037 dihydrochloride, supplier, PG01037, dopamine, receptors, D3, antagonists, dopaminergic, parkinsons, antiparkinsonian, parkinson's, Tocris Bioscience, D3 Receptor Antagonist products

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