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PD-168077 maleate

CAS No. : 630117-19-0

MCE 站：PD-168077 maleate

产品活性：PD-168077 maleate 是一个选择性的多巴胺 D₄ 受体激动剂，其 K_i 值为 9 nM。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Dopamine Receptor

In Vitro: 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-HT_1A, and a 460-fold selectivity over 5-HT_2A 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: 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.

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