货号 | 3887/50 |
别名 | N-[(2E)-4-[4-(2,3-Dichlorophenyl)-1 |
供应商 | Tocris |
生物活性 | Dopamine D3 receptor antagonist; 133-fold selective for D3 over D2receptorsin 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. |
运输条件 | Blue Ice |
存放说明 | 4℃ |
纯度 | >98 % |
计算分子量 | 554.34 |
分子式 | C26H26Cl2N4O.2HCl |
可溶性/溶解性 | Soluble to 20 mM in water with gentle warming and to 100 mM in DMSO |
CAS号 | 790658-27-4 |
参考文献 | Masonet 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. 333854. Kumaret 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. Grundtet 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. Grundtet 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. |