PD128907 HCl 是一种有效的选择性多巴胺 D3 受体激动剂,EC50 为 0.64 nM,选择性是多巴胺 D2 受体的 53 倍。
产品描述
PD 128907 HCl is a potent and selective dopamine D3 receptor agonist, with EC50 of 0.64 nM, exhibits 53-fold selectivity over dopamine D2 receptor.
体外活性
PD 128907 HCl is a potent and selective dopamine D3 receptor agonist, with EC50 of 0.64 nM, exhibits 53-fold selectivity over dopamine D2 receptor. [1] When using [3H]spiperone as the radioligand in CHOKl-cells, PD 128907 exhibits about a l000-fold selectivity for human D3 receptors (Ki, 1 nM) versus human D2 receptors (Ki, 1183 nM) and a l0000-fold selectivity versus human D4receptors (Ki, 7000 nM) [2] PD 128907 is used for studying the role of these receptors in the brain, in roles such as inhibitory autoreceptors that act to limit further dopamine release.[3]
体内活性
PD 128907 is active in reducing DA synthesis both in normal and γ-butyrolactone (GBL) treated rats. [4] PD 128907 (3 mg/kg) reduces toxicity from cocaine overdose, completely prevented the convulsant and lethal effects of cocaine. [5] The protection occurs through a D3-linked mechanism and that protection is extended to seizure kindling. [6]
Cas No.
112960-16-4
分子式
C14H20ClNO3
分子量
285.77
别名
PD128907 HCl
储存和溶解度
H2O:46 mg/mL (161 mM)
DMSO:10 mg/mL (35 mM)
Ethanol:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years