Agmatine sulfate
(Synonyms: 胍基丁胺；硫酸胍基丁胺；硫酸鲱精胺；胍基丁胺硫酸盐) 目录号 : GC16831
A polyamine metabolite
Cas No.:2482-00-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Animal experiment: | Rats: Thirty-four male Sprague-Dawley rats are subjected to transient MCA occlusion for 90 minutes. Immediately after reperfusion, agmatine (100 mg/kg) or normal saline is injected intraperitoneally into the agmatine-treated group (n= 17) or the control group, respectively. MR imaging is performed after reperfusion[6]. Mice: Mice are pretreated with a range of sub-effective doses of either fluoxetine (1, 2.5 and 5 mg/kg, p.o.; a selective serotonin reuptake inhibitor), imipramine (0.01, 0.05 and 0.1 mg/kg, p.o.; a tricyclic antidepressant), bupropion (0.1, 0.5 and 1 mg/kg, p.o.; dopamine reuptake inhibitor with subtle activity on noradrenergic reuptake), or MK-801 (0.0001, 0.0005 and 0.001 mg/kg, p.o.; noncompetitive NMDA receptor antagonist) and immediately after, a sub-effective dose of either agmatine (0.0001 mg/kg p.o.) or vehicle is administered. After 60 min, the animals are subjected to behavioral testing[7]. |
References: [1]. Li G, et al. Agmatine: an endogenous clonidine-displacing substance in the brain. Science. 1994 Feb 18;263(5149):966-9. | |
Agmatine sulfate exerts modulatory action at multiple molecular targets, such as neurotransmitter systems, ion channels and nitric oxide synthesis. It is an endogenous agonist at imidazoline receptor and a NO synthase inhibitor.
Agmatine binds to alpha 2-adrenergic and imidazoline receptors and stimulates release of catecholamines from adrenal chromaffin cells. Its biosynthetic enzyme, arginine decarboxylase, is present in brain. Agmatine, locally synthesized, is an endogenous agonist at imidazoline receptors, a noncatecholamine ligand at alpha 2-adrenergic receptors and may act as a neurotransmitter[1]. Agmatine is synthesized in the brain, stored in synaptic vesicles in regionally selective neurons, accumulated by uptake, released by depolarization, and inactivated by agmatinase. Agmatine inhibits nitric oxide synthase, and induces the release of some peptide hormones[2]. Agmatine, 4-(aminobutyl)guanidine, is produced by decarboxylation of L-arginine by the enzyme arginine decarboxylase. Agmatine is a competitive inhibitor of all NOS isoenzymes but not an NO precursor. Ki values are approximately 660 µM (NOS I), 220 µM (NOS II) and 7.5 mM (NOS III)[3]. Agmatine stimulates nitrite production three-fold above basal nitrite formation by endothelial cells. Agmatine displaces [3H]-idazoxan from endothelial cellmembranes and is found to induce transients in the cytosolic calcium of endothelial cells. The transients could be downregulated by repeated exposure to agmatine but are not affected by pretreatment with norepinephrine[4].
Agmatine produces an antidepressant-like effect when assessed in the forced swimming test and in the tail suspension test in mice (dose range 0.01-50 mg/kg, i.p.), without accompanying changes in ambulation in an open-field[5]. In ischemic stroke, agmatine protects the blood-brain barrier, which can be monitored in vivo by quantification of permeability by using dynamic contrast-enhanced MR imaging[6]. Agmatine substantially augments the antidepressant-like effect of MK-801, reinforcing the notion that this compound modulates NMDA receptor activation[7].
References:
[1]. Li G, et al. Agmatine: an endogenous clonidine-displacing substance in the brain. Science. 1994 Feb 18;263(5149):966-9.
[2]. Reis DJ, et al. Is agmatine a novel neurotransmitter in brain Trends Pharmacol Sci. 2000 May;21(5):187-93.
[3]. Galea E, et al. Inhibition of mammalian nitric oxide synthases by agmatine, an endogenouspolyamine formed by decarboxylation of arginine. Biochem J. 1996 May 15;316 ( Pt 1):247-9.
[4]. Morrissey JJ, et al. Agmatine activation of nitric oxide synthase in endothelial cells. Proc Assoc Am Physicians. 1997 Jan;109(1):51-7.
[5]. Zomkowski AD, et al. Agmatine produces antidepressant-like effects in two models of depression in mice. Neuroreport. 2002 Mar 25;13(4):387-91.
[6]. Ahn SS, et al. Effects of agmatine on blood-brain barrier stabilization assessed by permeability MRI in a rat model of transient cerebral ischemia. AJNR Am J Neuroradiol. 2015 Feb;36(2):283-8.
[7]. Neis VB, et al. Agmatine enhances antidepressant potency of MK-801 and conventional antidepressants in mice. Pharmacol Biochem Behav. 2015 Mar;130:9-14.
| Cas No. | 2482-00-0 | SDF | |
| 别名 | 胍基丁胺；硫酸胍基丁胺；硫酸鲱精胺；胍基丁胺硫酸盐 | ||
| 化学名 | 2-(4-aminobutyl)guanidine sulfate | ||
| Canonical SMILES | OS(O)(=O)=O.NCCCC/N=C(N)/N | ||
| 分子式 | C5H14N4.H2SO4 | 分子量 | 228.27 |
| 溶解度 | 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 | 4.3808 mL | 21.9039 mL | 43.8078 mL |
| 5 mM | 0.8762 mL | 4.3808 mL | 8.7616 mL |
| 10 mM | 0.4381 mL | 2.1904 mL | 4.3808 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。