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Agmatine sulfate

CAS No. : 2482-00-0

MCE 站：Agmatine sulfate

产品活性：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。

研究领域：GPCR/G Protein  |  Neuronal Signaling  |  Immunology/Inflammation  |  Metabolic Enzyme/Protease

作用靶点：Imidazoline Receptor  |  NO Synthase  |  Endogenous Metabolite

In Vitro: 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. 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. 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_i values are approximately 660 ?M (NOS I), 220 ?M (NOS II) and 7.5 mM (NOS III). 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.

In Vivo: 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. 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. Agmatine substantially augments the antidepressant-like effect of MK-801, reinforcing the notion that this compound modulates NMDA receptor activation.

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