PG 01037 dihydrochloride (N-[(2E)-4-[4-(2,3-Dichlorophenyl)-1-piperazinyl]-2-buten-1-yl]-4-(2-pyridyl)-benzamide dihydrochloride) | 675599-62-9

name

pg 01037 dihydrochloride

chemical name

n-[(2e)-4-[4-(2,3-dichlorophenyl)-1-piperazinyl]-2-buten-1-yl]-4-(2-pyridyl)-benzamide dihydrochloride

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.

MW

554.34

Formula:

c26h26cl2n4o.2hcl

Solubility:

soluble to 100 mm in water and to 100 mm in dmso

Purity:

>99 %

Storage:

desiccate at +4°c

CAS No:

675599-62-9

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.