Mometasone furoate   中文名称: 糠酸莫米松

糠酸莫米松附着在糖皮质激素受体上，引起受体构象变化，与伴侣分离，受体进入细胞核[1]。糠酸莫米松（0.1-10 μM；LPS 刺激前 2 小时）以浓度依赖性方式显着抑制 J774 巨噬细胞中 LPS 刺激的亚硝酸盐生成，J774 细胞中糠酸莫米松的 IC50 值为 0.00024 μM[1]。糠酸莫米松（0.1-10 μM；LPS 刺激前 2 小时）比 DEX 更强大，它在 0.01 μM 剂量下显着降低 iNOS 表达，而 Dex 在 0.1 μM 剂量下变得活跃。此外，0.01 µM 的 cox-2 蛋白表达抑制率对于糠酸莫米松为 79%，对于 Dex 为 39%[1]。

莫米松会减少大鼠揉鼻的次数，并且在治疗期间观察到这种反应受到抑制。在小鼠中测试的最高剂量下，莫米松 (3 mg/kg) 可抑制气道对雾化醋甲胆碱敏感性的增加。最后一次过敏原激发后一小时给予莫米松，剂量依赖性地抑制过敏原诱导的 Penh 增加，与激发前的治疗方案相比，效力损失约 10 倍。糠酸莫米松（0.02%）和丙酸氟替卡松（0.1%）即使在局部应用后6小时也能显着抑制抗原诱导的鼻摩擦增加，表明这两种药物具有长效作用。糠酸莫米松剂量依赖性地抑制致敏、卵清蛋白攻击小鼠的支气管肺泡灌洗液和肺组织中嗜酸性粒细胞数量的升高。糠酸莫米松 (33 mg/kg) 可将 CD44+ T 辅助细胞（活化/记忆细胞）的百分比降低至在未致敏、卵清蛋白攻击的小鼠中观察到的水平。

Absorption, Distribution and Excretion
The mean time to peak concentration is 1.0 to 2.5 hours. Bioavailability has been reported as <1% but studies of repeat doses of inhaled corticosteroids suggest a bioavailability of 11%. The 0.1% ointment may have a bioavailability of 0.7%.
For an inhaled dose, approximately 74% is excreted in the feces and 8% is excreted in the urine.
Steady state volume of distribution of 152L.
The clearance rate of mometasone furoate is not readily available, though it may be close to 90L/h.

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Metabolism / Metabolites
Metabolism of mometasone furoate is largely performed hepatically by cytochrome P450 3A4 producing a number of metabolites. Some of these metabolites include free mometasone and 6-beta-hydroxy-mometasone furoate.

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Biological Half-Life
The terminal half life of an inhaled dose is approximately 5 hours though it has been reported as 5.8 hours by other sources.

Protein Binding
98% to 99% (in vitro concentration of 5 to 500ng/mL).

[1]. Use of Mometasone furoate in prolonged treatment of experimental spinal cord injury in mice: A comparative study of three different glucocorticoids. Pharmacol Res. 2015 Sep;99:316-28.

[2]. https://go.drugbank.com/drugs/DB14512.

Mometasone furoate is a 2-furoate ester, a steroid ester, an 11beta-hydroxy steroid, a 20-oxo steroid, an organochlorine compound and a 3-oxo-Delta(1),Delta(4)-steroid. It has a role as an anti-inflammatory drug and an anti-allergic agent. It is functionally related to a mometasone.
Mometasone furoate is a corticosteroid drug that can be used for the treatment of asthma, rhinitis, and certain skin conditions. It has a glucocorticoid receptor binding affinity 22 times stronger than [dexamethasone] and higher than many other corticosteroids as well. Mometasone furoate is formulated as a dry powder inhaler, nasal spray, and ointment for its different indications.
Mometasone Furoate is the furoate ester form of mometasone, a synthetic topical glucocorticoid receptor (GR) agonist with anti-inflammatory, anti-pruritic and vasoconstrictive properties. Upon administration, mometasone binds to cytoplasmic GRs and subsequently activates GR-mediated gene expression. This results in the synthesis of certain anti-inflammatory proteins, while inhibiting the synthesis of certain inflammatory mediators. Specifically, mometasone appears to induce phospholipase A2 inhibitory proteins, thereby controlling the release of the inflammatory precursor arachidonic acid from phospholipid membrane by phospholipase A2.
A pregnadienediol derivative ANTI-ALLERGIC AGENT and ANTI-INFLAMMATORY AGENT that is used in the management of ASTHMA and ALLERGIC RHINITIS. It is also used as a topical treatment for skin disorders.
See also: Mometasone (has active moiety); Formoterol fumarate; mometasone furoate (component of); Florfenicol; Mometasone furoate; Terbinafine (component of) ... View More ...

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Drug Indication
Inhaled mometasone furoate is indicated for prophylaxis of asthma in patients ≥4 years. Applied topically as an ointment, mometasone furoate is indicated for symptomatic treatment of dermatitis and pruritis in patients ≥2 years. Mometasone furoate nasal spray is available both over-the-counter (OTC) and by prescription. The OTC nasal spray formulation of mometasone furoate is indicated for the treatment of upper respiratory allergic symptoms (e.g. rhinorrhea, sneezing) in patients ≥2 years of age. The prescription formulation is indicated for the treatment of chronic rhinosinusitis with nasal polyps in patients ≥18 year old and for the and prophylaxis of seasonal allergic rhinitis in patients ≥12 years old. It is also approved in combination with [olopatadine] for the symptomatic treatment of seasonal allergic rhinitis in patients ≥12 years.
FDA Label
Seasonal and perennial allergic rhinitis

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Mechanism of Action
In asthma, mometasone is believed to inhibit mast cells, eosinophils, basophils, and lymphocytes. There is also evidence of inhibition of histamine, leukotrienes, and cytokines. Corticosteroids diffuse across cell membranes into the cytosol of cells where they bind to glucocorticoid receptors to produce their activity. Mometasone furoate has a particularly high receptor affinity compare to other corticosteroids, 22 times higher than that of [dexamethasone]. Mometasone furoate binding to a glucocorticoid receptor causes conformational changes in the receptor, separation from chaperones, and the receptor moves to the nucleus. Once at the nucleus, receptors dimerize and bind to a DNA sequence known as the glucocorticoid response element which either increases expression of anti-inflammatory molecules or inhibits expression of pro-inflammatory molecules (such as interleukins 4 and 5). Mometasone furoate also reduces inflammation by blocking transcription factors such as activator-protein-1 and nuclear factor kappa B (NF-kappaB).

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Pharmacodynamics
Mometasone is a synthetic corticosteroid with an affinity for glucocorticoid receptors 22 times higher than that of [dexamethasone]. Mometasone furoate also has a lower affinity to mineralocorticoid receptors than natural corticosteroids, making it more selective in its action. Mometasone furoate diffuses across cell membranes to activate pathways responsible for reducing inflammation.

C27H30CL2O6

521.43

83919-23-7

Mometasone furoate-d3

441336

White to off-white solid powder

1.4±0.1 g/cm3

655.5±55.0 °C at 760 mmHg

218-220°C

350.2±31.5 °C

0.0±2.1 mmHg at 25°C

1.604

4.27

113.02

1

6

5

35

1020

8

WOFMFGQZHJDGCX-ZULDAHANSA-N

InChI=1S/C27H30Cl2O6/c1-15-11-19-18-7-6-16-12-17(30)8-9-24(16,2)26(18,29)21(31)13-25(19,3)27(15,22(32)14-28)35-23(33)20-5-4-10-34-20/h4-5,8-10,12,15,18-19,21,31H,6-7,11,13-14H2,1-3H3/t15-,18+,19+,21+,24+,25+,26+,27+/m1/s1

(8S,9R,10S,11S,13S,14S,16R,17R)-9-chloro-17-(2-chloroacetyl)-11-hydroxy-10,13,16-trimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-17-yl furan-2-carboxylate

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

配方 1 中的溶解度: ≥ 2.5 mg/mL (4.79 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 2.5 mg/mL (4.79 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL 澄清 DMSO 储备液添加到 900 μL 玉米油中并混合均匀。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。