Pramipexole
(Synonyms: 普拉克索) 目录号 : GC11960Pramipexole 是一种选择性和血脑屏障 (BBB) 渗透性多巴胺 D2 型受体激动剂,对 D2 型受体、D2、D3 和 D4 受体的 Kis 分别为 2.2 nM、3.9 nM、0.5 nM 和 1.3 nM。
Cas No.:104632-26-0
Sample solution is provided at 25 µL, 10mM.
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Pramipexole is a dopamine agonist of the non-ergoline class indicated for treating Parkinson's disease (PD) and restless legs syndrome (RLS).Target: Dopamine Receptor Pramipexole also possesses low/insignificant affinity (500-10,000 nM) for the 5-HT1A, 5-HT1B, 5-HT1D, and α2-adrenergic receptors. It has negligible affinity (>10,000 nM) for the D1, D5, 5-HT2, α1-adrenergic, β-adrenergic, H1, and mACh receptors. All sites assayed were done using human tissues. While pramipexole is used clinically, its D3-preferring receptor binding profile has made it a popular tool compound for preclinical research. Pramipexole has been used (in combination with D2- and or D3-preferring antagonists) to interrogate the role of D3 receptor function in rodent models and tasks for neuropsychiatric disorders [1-3].
References:
[1]. Kvernmo, T., S. Hartter, and E. Burger, A review of the receptor-binding and pharmacokinetic properties of dopamine agonists. Clin Ther, 2006. 28(8): p. 1065-78.
[2]. Millan, M.J., et al., Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes. J Pharmacol Exp Ther, 2002. 303(2): p. 791-804.
[3]. Weber, M., et al., Heritable strain differences in sensitivity to the startle gating-disruptive effects of D2 but not D3 receptor stimulation. Behav Pharmacol, 2008. 19(8): p. 786-95.
Cas No. | 104632-26-0 | SDF | |
别名 | 普拉克索 | ||
化学名 | (6S)-6-N-propyl-4,5,6,7-tetrahydro-1,3-benzothiazole-2,6-diamine | ||
Canonical SMILES | CCCNC1CCC2=C(C1)SC(=N2)N | ||
分子式 | C10H17N3S | 分子量 | 211.33 |
溶解度 | ≥ 10.6mg/mL in DMSO | 储存条件 | Store at -20°C |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 4.7319 mL | 23.6597 mL | 47.3194 mL |
5 mM | 0.9464 mL | 4.7319 mL | 9.4639 mL |
10 mM | 0.4732 mL | 2.366 mL | 4.7319 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度: mg/ml;
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1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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