Isoguvacine hydrochloride
(Synonyms: 异四氢烟酸) 目录号 : GC13567
A GABAA receptor agonist
Cas No.:68547-97-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Kinase experiment: | The assay for 3H-Isoguvacine binding is carried out as follows: membranes suspended in Tris-citrate buffer pH 7.1 are incubated at 4°C for 10 min with 8 nM 3H-Isoguvacine. Identical samples are incubated in the presence of cold 0.5 mM GABA or 10 μM cold isoguvacine. The assay is terminated by centrifugation for 10 min at 4°C in a micro-centrifuge. The supernatants are rapidly aspirated and the surface of the pellets washed (2x) with ice-cold buffer. The pellet is resuspended in I00 μL of 0.1% Triton and placed in a scintillation vial. The assay tube is washed with I00 μL of distilled water and the wash added to the vial along with 10 ml of PCS: xylene (2:1). Counting efficiency is determined to be 40-45% in a Beckman liquid scintillation counter. Specific binding is defined as those radioactive cpm of bound 3H-Isoguvacine that are displaced by excess cold isoguvacine or GABA[1]. |
References: [1]. Morin AM, et al. The binding of 3H-isoguvacine to mouse brain synapticmembranes. Life Sci. 1980 Apr 14;26(15):1239-45. | |
Isoguvacine hydrochloride is a GABA receptor agonist.
Isoguvacine binds to a mouse forebrain synaptic membrane preparation. The specific binding is displaceable by GABA, muscimol and bicuculline but not by picrotoxin or diaminobutyric acid. Kinetic data suggest two binding affinities. Highest levels of binding are observed in the cerebellum, cortex and hippocampus[1]. Isoguvacine binds to membrane preparations of rat forebrain with pharmacological characteristics similar to the postsynaptic GABA recognition site: that it is transported into synaptosomal preparations by an uptake system similar to the high-affinity GABA uptake system; and that recently accumulated isoguvacine is released in a Ca2+-dependent manner and by heteroexchange with external GABA[2]. Isoguvacine at a concentration of 50 μM blocks the seizure like events in 2 out of 6 organotypic hippocampal slice cultures. Isoguvacine inhibits the low magnesium induced seizure like events dose dependently[3].
Reference:
[1]. Morin AM, et al. The binding of 3H-isoguvacine to mouse brain synapticmembranes. Life Sci. 1980 Apr 14;26(15):1239-45.
[2]. White WF, et al. Isoguvacine binding, uptake, and release: relation to the GABA system. J Neurochem. 1983 Jun;40(6):1701-8.
[3]. Wahab A, et al. Effects of gamma-aminobutyric acid (GABA) agonists and a GABA uptake inhibitor on pharmacoresistant seizure like events in organotypic hippocampal slice cultures. Epilepsy Res. 2009 Oct;86(2-3):113-23.
| Cas No. | 68547-97-7 | SDF | |
| 别名 | 异四氢烟酸 | ||
| 化学名 | 1,2,3,6-tetrahydropyridine-4-carboxylic acid hydrochloride | ||
| Canonical SMILES | OC(C1=CCNCC1)=O.Cl | ||
| 分子式 | C6H9NO2.HCl | 分子量 | 163.6 |
| 溶解度 | DMSO: 1 mg/ml,PBS (pH 7.2): 10 mg/ml | 储存条件 | Store at RT |
| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 6.1125 mL | 30.5623 mL | 61.1247 mL |
| 5 mM | 1.2225 mL | 6.1125 mL | 12.2249 mL |
| 10 mM | 0.6112 mL | 3.0562 mL | 6.1125 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 | ||||||||||
计算结果:
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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