PD128907 HCl

产品编号 T6142Cas号 112960-16-4

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。

产品编号 T6142Cas号 112960-16-4

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。

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生物活性

产品描述	PD128907 HCl is a potent and selective dopamine D3 receptor agonist, with EC50 of 0.64 nM, exhibits 53-fold selectivity over dopamine D2 receptor.
靶点活性	D3 receptor:0.64 nM (Ki)
体外活性	PD128907 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	PD128907 HCl is active in reducing DA synthesis both in normal and γ-butyrolactone (GBL) treated rats. [4] PD128907 HCl (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]

化学信息

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

溶解度信息

Ethanol: <1 mg/mL

H2O: 46 mg/mL (161 mM)

DMSO: 10 mg/mL (35 mM)

溶液配制表

DMSO/H2O