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CAS No. : 630117-19-0
MCE 国际站: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 Ki 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-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: 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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