CAS NO: | 630117-19-0 |
包装 | 价格(元) |
10mg | 电议 |
50mg | 电议 |
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 SMILES | CC1=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 tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation 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: |