Lodoxamide tromethamine

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Chemical Structure| 63610-09-3 同义名 : U-42585E; Alomide
CAS号 : 63610-09-3
货号 : A202923
分子式 : C19H28ClN5O12
纯度 : 99%+
分子量 : 553.91
MDL号 : MFCD04112765
存储条件：

Pure form Keep in dark place, inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 18 mg/mL(32.5 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 100 mg/mL(180.53 mM)
动物实验配方：
生物活性
描述 To treat allergic asthma, nonsympathomimetic drugs have been developed that act prophylactically by inhibiting the release of mast cell mediators. Lodoxamide tromethamine is a new drug intended for the prophylaxis of mast cell-mediated allergic disease. In vitro, lodoxamide inhibited compound 48/80-induced histamine release and ionophore-induced 45Ca influx with associated histamine release in purified rat peritoneal mast cells. When given intravenously, orally, or intrabronchially by aerosol, lodoxamide significantly inhibited the increased respiratory frequency and decreased tidal volume induced by antigen challenge in Ascaris-sensitized, anesthetized rhesus monkeys. Doses as low as 1 μg by aerosol 30 min prior to challenge effectively prevented lung function changes induced by allergen. Ten allergen-sensitive asthmatics were pretreated with lodoxamide (0.01, 0.1, or 1.0 mg) or placebo. Pretreatment with lodoxamide offered significant protection against experimental allergen-induced bronchoconstriction. At 0.01 mg, lodoxamide was effective in over half the subjects tested. Administration of lodoxamide by inhalation at doses of 0.1 and 1.0 mg uniformly allowed subjects to tolerate significantly larger doses of inhaled allergen[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.81mL

0.36mL

0.18mL

9.03mL

1.81mL

0.90mL

18.05mL

3.61mL

1.81mL
参考文献

[1]Avunduk AM, Avunduk MC, et al. Mechanisms and comparison of anti-allergic efficacy of topical lodoxamide and cromolyn sodium treatment in vernal keratoconjunctivitis. Ophthalmology. 2000 Jul;107(7):1333-7.

[2]Lee S, Allard TR. Lodoxamide in vernal keratoconjunctivitis. Ann Pharmacother. 1996 May;30(5):535-7.

[3]Watt GD, Bui TC, Bewtra AK, Townley RG. Protective effect opf lodoxamide tromethamine on allergen inhalation challenge. J Allergy Clin Immunol. 1980;66(4):286‐294