PD-168077 maleate

PD-168077 maleateCAS号: 630117-19-0分子式: C24H26N4O5分子量: 450.49描述纯度储存/保存方法外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述
PD-168077 maleate is a selective dopamine D4 receptor agonist, with a Ki of 9 nM.
纯度
98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
外观
white powder
可溶性/溶解性
DMSO : 150 mg/mL (332.97 mM; Need ultrasonic)
生物活性
靶点
Dopamine D4 receptor
In vitro(体外研究)
PD-168077 is one of the first agents to be identified as putative selective D4 agonists. It shows >100-fold selectivity over other members of the D2-like receptor family and over their D1-like counterparts; PD-168077 shows a 20-fold selectivity over α1, and α2, a 45-fold selectivity over 5-HT1A, and a 460-fold selectivity over 5-HT2A receptors; PD-168077 evidences intrinsic activity at the D4 receptor in terms of quinpirole-like inhibition of forskolin-stimulated cAMP accumulation or stimulation of [3H]thymidine uptake in CHO cells expressing the human D4 receptor. In the PD-168077-treated cell, p-CaMKII exhibits a significantly increased clustering at synaptic sites, as indicated by the enhanced colocalization with PSD-95.
In vivo(体内研究)
PD-168077 (0.2-25.0 mg/kg) dose-dependently induces locomotion, which takes an unusual and characteristic ”shuffling” form with uncoordinated movements together with yawning, and episodes of myoclonic jerking; grooming, and rearing are reduced.

分子结构图

PD-168077 maleate