硫酸胍基丁胺 T4808

Product Introduction
Bioactivity


英文名: Agmatine sulfate

描述: Agmatine sulfate (Agmatine sulfate salt) 是咪唑啉受体的内源性激动剂和一氧化氮合酶抑制剂。它靶向神经递质系统，离子通道和一氧化氮合成。

体外活性: 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 a 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 cell membranes 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].

体内活性: 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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : Insoluble
H2O : 10 mM


关键字: Endogenous Metabolite | Agmatine | Agmatine sulfate | Nitric oxide synthases | NO Synthase | Inhibitor | Imidazoline Receptor | Agmatine Sulfate | inhibit | NOS

相关产品: BU 226 hydrochloride | Idazoxan hydrochloride | Harmane | Rilmenidine hemifumarate | BU 224 hydrochloride | Moxonidine | 2-BFI hydrochloride | Rilmenidine Phosphate | Allantoin | CR4056

相关库: Anti-Tumor Natural Product Library | Human Endogenous Metabolite Library | Bioactive Compounds Library Max | Inhibitor Library | Human Endogenous Metabolite Compound Library Plus | Natural Product Library for HTS | Endocrinology-Hormone Compound Library | Gut Microbial Metabolite Library | RO5 Drug-like Natural Product Library | NO PAINS Compound Library

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