Agmatine Sulfate
Cat.No:IA4360 Solarbio
CAS:2482-00-0
Storage:Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:≥98%
Appearance:White to off-white Solid
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Agmatine SulfateCAS:2482-00-0
Storage:Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:≥98%
Appearance:White to off-white Solid
Qty:
Size:
CAS | 2482-00-0 |
Name | Agmatine Sulfate |
Molecular Formula | C5H14N4·H2SO4 |
Molecular Weight | 228.27 |
Solubility | Soluble in Water ≥5mg/mL |
Purity | ≥98% |
Appearance | White to off-white Solid |
Storage | Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year |
EC | EINECS 219-617-3 |
MDL | MFCD00013109 |
SMILES | NC(NCCCCN)=N.O=S(O)(O)=O |
Target Point | Imidazoline Receptor,NO Synthase |
Passage | GPCR & G Protein;Neuronal Signaling |
Background | Agmatine Sulfate plays a regulatory role on multiple targets, such as neurotransmitter system, ion channel, nitric oxide synthesis. It is an endogenous agonist and NO synthase inhibitor of imidazoline receptor. |
Biological Activity | Agmatine sulfate在多个靶点上发挥调节作用,如神经递质系统,离子通道,一氧化氮合成。它是 imidazoline receptor 的内源性激动剂和 NO synthase 抑制剂。[1-7] |
In Vitro | 胍丁胺与α2-肾上腺素能和咪唑啉受体结合,并刺激肾上腺嗜铬细胞释放儿茶酚胺。其生物合成酶精氨酸脱羧酶存在于脑中。局部合成的胍丁胺是咪唑啉受体的内源性激动剂,是α2-肾上腺素能受体的非儿茶酚胺配体,可作为神经递质[1]。胍丁胺在大脑中合成,储存在区域选择性神经元的突触小泡中,通过摄取积累,通过去极化释放,并通过农杆菌酶灭活。胍丁胺抑制一氧化氮合酶,并诱导一些肽激素的释放[2]。胍丁胺4-(氨基丁基)胍是通过酶精氨酸脱羧酶使L-精氨酸脱羧而产生的。胍丁胺是所有NOS同工酶的竞争性抑制剂,但不是NO前体。 Ki值约为660μM(NOS I),220μM(NOS II)和7.5 mM(NOS III)[3]。胍丁胺刺激亚硝酸盐产生比内皮细胞形成的基础亚硝酸盐高三倍。胍丁胺从内皮细胞膜中置换[3H] - 脱氮嗪,并且发现其诱导内皮细胞的胞质钙中的瞬变。通过反复接触胍丁胺可以下调瞬变,但不受去甲肾上腺素预处理的影响[4]。 |
In Vivo | 当在强迫游泳测试和小鼠尾部悬浮试验(剂量范围0.01-50mg / kg,ip)中评估时,胍丁胺产生类似抗抑郁药的效果,而没有伴随开放场中移动的变化[5]。在缺血性中风中,胍丁胺可以保护血脑屏障,可以通过使用动态对比增强磁共振成像定量渗透性来体内监测[6]。胍丁胺大大增强了MK-801的抗抑郁样作用,强化了这种化合物调节NMDA受体激活的观点[7]。 |
Animal Experiment | 大鼠:将34只雄性Sprague-Dawley大鼠进行瞬时MCA闭塞90分钟。再灌注后,立即将胍丁胺(100mg / kg)或生理盐水腹膜内注射到胍丁胺处理组(n = 17)或对照组。再灌注后进行MR成像[6]。小鼠:用一系列亚有效剂量的氟西汀(1,2.5和5 mg / kg,po;选择性5-羟色胺再摄取抑制剂),丙咪嗪(0.01,0.05和0.1 mg / kg,po;三环)预处理小鼠。抗抑郁药),安非他酮(0.1,0.5和1 mg / kg,po;对去甲肾上腺素能再摄取具有微妙活性的多巴胺再摄取抑制剂),或MK-801(0.0001,0.0005和0.001 mg / kg,po;非竞争性NMDA受体拮抗剂)并立即之后,给予亚有效剂量的胍丁胺(0.0001mg / kg口服)或赋形剂。 60分钟后,对动物进行行为测试[7]。 |
Data Literature Source | [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 |
Unit | Bottle |
Specification | 100mg |
Remark:These protocols are for reference only. Solarbio does not independently validate these methods.
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