| CAS NO: | 587870-77-7 |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 50mg | 电议 |
| Physical Appearance | White solid |
| Storage | Store at -20°C |
| M.Wt | 402.75 |
| Cas No. | 587870-77-7 |
| Formula | C17H19N5·3HCl |
| Solubility | <40.27mg/ml in H2O |
| Chemical Name | 2-((4-(pyridin-2-yl)piperazin-1-yl)methyl)-1H-benzo[d]imidazole trihydrochloride |
| Canonical SMILES | N1(CC2=NC3=CC=CC=C3N2)CCN(C4=NC=CC=C4)CC1.Cl.Cl.Cl |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
ABT 724 trihydrochloride是高选择性D4多巴胺激动剂[1,2],在转染人D4受体的CHO细胞中,其提高GTPγS结合活性的EC50值为281 nM,在共转染G蛋白(Gαq05)和大鼠/人D4受体的HEK-293细胞中,其提高Ca2+流的EC50值为12.4 nM [3].
神经递质多巴胺(DA)在调节人类T细胞功能中发挥重要作用.通过D1/D5\D2和D3受体,DA通过刺激表面整联蛋白的表达及细胞因子的释放,从而激活静息期T细胞.通过下调非受体酪氨酸激酶,DA能抑制活化T细胞的增殖.刺激多巴胺D4受体能诱导T细胞休眠[1].
在D4受体存在的情况下,在用anti-CD3/CD28刺激TCR 48小时的起始用1 μM特异性D4 DA激动剂PD 168,077处理T细胞,以使D4 DA激动剂贯穿整个时期.[3H]胸苷掺入实验表明,这些细胞的增殖受到显著抑制.另一种D4 DA激动剂,即1 μM ABT 724 trihydrochloride对T细胞有类似的效应[1].
Clozapine对多巴胺D4受体具有高亲和力[4].相比于Clozapine单纯处理,Clozapine联合50 μM或25 μM ABT-724能够显著增加斑马鱼幼虫的自发活动.ABT-724以剂量依赖的方式保护幼虫抵抗Clozapine诱导的活动减退[5].
参考文献：
[1]. Sarkar C, Das S, Chakroborty D, et al. Cutting Edge: Stimulation of dopamine D4 receptors induce T cell quiescence by up-regulating Kruppel-like factor-2 expression through inhibition of ERK1/ERK2 phosphorylation. J Immunol, 2006, 177(11):7525-9.
[2]. Melis MR, Succu S, Mascia MS, et al. PD-168077, a selective dopamine D4 receptor agonist, induces penile erection when injected into the paraventricular nucleus of male rats. Neurosci Lett, 2005, 379(1):59-62.
[3]. Sanna F, Contini A, Melis MR, et al. Role of dopamine D4 receptors in copulatory behavior: Studies with selective D4 agonists and antagonists in male rats. Pharmacol Biochem Behav, 2015, 137:110-8.
[4]. Arranz M, Collier D, Sodhi M, et al. Association between clozapine response and allelic variation in 5-HT2A receptor gene. Lancet, 1995, 346(8970):281-2.
[5]. Boehmler W, Carr T, Thisse C, et al. D4 Dopamine receptor genes of zebrafish and effects of the antipsychotic clozapine on larval swimming behaviour. Genes Brain Behav, 2007, 6(2):155-66.
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