Dihydrokainic acid
(Synonyms: 2-羧基-4-异丙基-3-吡咯烷乙酸,DHK) 目录号 : GC14271An inhibitor of EAAT2
Cas No.:52497-36-6
Sample solution is provided at 25 µL, 10mM.
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- Purity: >95.00%
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Dihydrokainic acid (DHK) is an inhibitor of excitatory amino acid transporter 2 (EAAT2; Ki = 23 µM for glutamate uptake by COS cells expressing EAAT2).[1] It is selective for EEAT2 over EAAT1 and EAAT3 (Ki = >3 mM for both). DHK microinfusion (5 nmol) into the rat infralimbic cortex reduces the time spent immobile in the forced swim test, indicating antidepressant-like behavior, an effect that is blocked by the AMPA receptor antagonist NBQX and the serotonin (5-HT) receptor subtype 5-HT1A antagonist WAY-100635 .[2],[3] It also increases glutamate and serotonin levels and the expression of c-Fos in the dorsal raphe nucleus. In contrast, DHK microinjection (6.25 nmol) into the rat prefrontal cortex (PFC) increases the latency to drink sucrose in a sucrose intake test, indicating anhedonia-like behavior.[4] It also impairs memory acquisition, consolidation, and retrieval in mice in the novel object recognition test.[5]
Reference:
[1]. Arriza, J.L., Fairman, W.A., Wadiche, J.I., et al. Functional comparisons of three glutamate transporter subtypes cloned from human motor cortex. J. Neurosci. 14(9), 5559-5569 (1994).
[2]. Gasull-Camós, J., Tarrés-Gatius, M., Artigas, F., et al. Glial GLT-1 blockade in infralimbic cortex as a new strategy to evoke rapid antidepressant-like effects in rats. Transl. Psychiatry 7(2), e1038 (2017).
[3]. Gasull-Camós, J., Martínez-Torres, S., Tarrés-Gatius, M., et al. Serotonergic mechanisms involved in antidepressant-like responses evoked by GLT-1 blockade in rat infralimbic cortex. Neuropharmacology 139, 41-51 (2018).
[4]. John, C.S., Smith, K.L., Van't Veer, A., et al. Blockade of astrocytic glutamate uptake in the prefrontal cortex induces anhedonia. Neuropsychopharmacology 37(11), 2467-2475 (2012).
[5]. Tian, S.-W., Yu, X.-D., Cen, L., et al. Glutamate transporter GLT1 inhibitor dihydrokainic acid impairs novel object recognition memory performance in mice. Physiol. Behav. 199, 28-32 (2019).
Cas No. | 52497-36-6 | SDF | |
别名 | 2-羧基-4-异丙基-3-吡咯烷乙酸,DHK | ||
化学名 | (2S,3S,4R)-3-(carboxymethyl)-4-isopropylpyrrolidine-2-carboxylic acid | ||
Canonical SMILES | OC([C@H]1NC[C@H](C(C)C)[C@@H]1CC(O)=O)=O | ||
分子式 | C10H17NO4 | 分子量 | 215.25 |
溶解度 | H2O : 5 mg/mL (23.23 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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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 | 4.6458 mL | 23.2288 mL | 46.4576 mL |
5 mM | 0.9292 mL | 4.6458 mL | 9.2915 mL |
10 mM | 0.4646 mL | 2.3229 mL | 4.6458 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 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
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工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
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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