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PD 168077 maleate
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
PD 168077 maleate图片
CAS NO:630117-19-0
包装与价格：
包装价格(元)
10mg询价
50mg询价

PD 168077 maleate 是一种选择性多巴胺 D4 受体激动剂，Ki 为 9 nM。
Cas No.630117-19-0
化学名maleic acid compound with (Z)-N-((4-(2-cyanophenyl)piperazin-1-yl)methyl)-3-methylbenzimidic acid (1:1)
Canonical SMILESCC1=CC(/C(O)=N/CN2CCN(C3=CC=CC=C3C#N)CC2)=CC=C1.O=C(O)/C([H])=C([H])\C(O)=O
分子式C20H22N4O.C4H4O4
分子量450.49
溶解度<11.26mg/ml in ethanol;<45.05mg/ml in DMSO
储存条件Desiccate at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

PD-168077 maleate is a selective dopamine D4 receptor agonist, with a Ki of 9 nM.

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[1]. 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[2].

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[1].

References:
[1]. Clifford JJ, et al. Topographically based search for an "Ethogram" among a series of novel D(4) dopamine receptor agonists and antagonists. Neuropsychopharmacology. 2000 May;22(5):538-44.
[2]. Gu Z, et al. Activation of dopamine D4 receptors induces synaptic translocation of Ca2+/calmodulin-dependent protein kinase II in cultured prefrontal cortical neurons. Mol Pharmacol. 2006 Mar;69(3):813-22.

 
 
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