Agmatine sulfate exerts modulatory action at multiple molecular targets, such as neurotransmitter systems, ion channels and nitric oxide synthesis. It is an endogenous agonist atimidazoline receptorand aNO synthaseinhibitor.

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. K_ivalues 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 monitoredin vivoby 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].

228.27

Solid

C₅H₁₆N₄O₄S

2482-00-0

胍基丁胺；硫酸胍基丁胺；硫酸鲱精胺；胍基丁胺硫酸盐

• Others

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

H₂O : ≥ 100 mg/mL(438.08 mM)

DMSO : 1 mg/mL(4.38 mM;ultrasonic and warming and heat to 80℃)

*"≥" means soluble, but saturation unknown.

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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： PBS

  Solubility: 25 mg/mL (109.52 mM); Clear solution; Need ultrasonic and warming