PG 01037 dihydrochloride是D3 受体选择性拮抗剂。
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] 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.
[2] 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.
[3] 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.
[4] 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.
分子式 C26H26Cl2N4O.2HCl |
分子量 554.34 |
CAS号 675599-62-9 |
储存方式 ﹣20 ℃长期储存。冰袋运输 |
溶剂(常温) |
DMSO 100 mM |
Water 100 mM |
Ethanol |
体内溶解度
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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