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药品详细

Spaglumic Acid(Spaglumic酸)

化学结构式图
中文名
Spaglumic酸
英文名
Spaglumic Acid
分子式
C11H16N2O8
化学名
(2R)-2-[(3S)-3-carboxy-3-acetamidopropanamido]pentanedioic acid
分子量
Average: 304.2533
Monoisotopic: 304.090665498
CAS号
4910-46-7
ATC分类
R01A 未知;S01G 解充血药及抗过敏药
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Spaglumic acid is the β-aspartyl isoform of N-Acetyl-l-aspartylglutamate (isospaglumic Acid is N-(N-Acetyl-l-α-aspartyl)-l-glutamic acid). In eye drops, spaglumic acid is either a magnesium or sodium salt of N-Acetyl-l-aspartylglutamate. Spaglumic acid is a mast cell stabilizer. Thus it is used in allergic conditions such as allergic conjunctivitis. Specifically spaglumic acid is approved in Portugal under the brand name Naabak and in Greece under the brand name Naaxia for use in patients with allergic conjunctivitis.

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    参考
    Synthesis Reference

    Reddy AV, Ravindranath B: Synthesis of alpha-, beta- and cyclic spaglumic acids. Int J Pept Protein Res. 1992 Nov;40(5):472-6.
    General Reference
    1. Sala-Rabanal M, Loo DD, Hirayama BA, Turk E, Wright EM: Molecular interactions between dipeptides, drugs and the human intestinal H+ -oligopeptide cotransporter hPEPT1. J Physiol. 2006 Jul 1;574(Pt 1):149-66. Epub 2006 Apr 20. Pubmed
    2. Sanchis-Merino ME, Montero JA, Ruiz-Moreno JM, Rodriguez AE, Pastor S: Comparative efficacy of topical antihistamines in an animal model of early phase allergic conjunctivitis. Exp Eye Res. 2008 May;86(5):791-7. doi: 10.1016/j.exer.2008.02.007. Epub 2008 Mar 4. Pubmed
    3. Purello D’Ambrosio F, Gangemi S, Ricciardi L, Cuzzocrea S, Di Lorenzo G: Lodoxamide versus spaglumic acid: a comparative double-blind trial on patients suffering from seasonal allergic conjunctivitis induced by Parietaria pollen. Allergol Immunopathol (Madr). 1997 Sep-Oct;25(5):233-7. Pubmed
    剂型
    规格
    化合物类型
    Type small molecule
    Classes Not Available
    Substructures Not Available
    适应症
    药理
    Indication Used in patients with allergic conjunctivitis.
    Pharmacodynamics Not Available
    Mechanism of action Spaglumic acid is a mast cell stabilizer. Mast cells are involved in producing an allergic response by releasing inflammatory mediators such as histamine. Mast cell stablizers block the release of histamine and other mediators by inhibiting mast cell degranulation, which is the process of releasing these mediators. Inhibition occurs through inhibition of specific calcium channels to stabilize the mast cell and prevent degranulation.
    Absorption Not Available
    Volume of distribution Not Available
    Protein binding Not Available
    Metabolism
    Not Available
    Route of elimination Not Available
    Half life Not Available
    Clearance Not Available
    Toxicity Not Available
    Affected organisms
    • Humans and other mammals
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties Not Available
    Predicted Properties
    Property Value Source
    water solubility 3.22e+00 g/l ALOGPS
    logP -1.1 ALOGPS
    logP -2.3 ChemAxon
    logS -2 ALOGPS
    pKa (strongest acidic) 3.01 ChemAxon
    pKa (strongest basic) -1.5 ChemAxon
    physiological charge -3 ChemAxon
    hydrogen acceptor count 8 ChemAxon
    hydrogen donor count 5 ChemAxon
    polar surface area 170.1 ChemAxon
    rotatable bond count 9 ChemAxon
    refractivity 64.06 ChemAxon
    polarizability 26.96 ChemAxon
    药物相互作用
    食物相互作用
    • No food effects were found.

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