Montelukast sodium
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Montelukast sodium 속성
- 녹는점
- 115 °C(dec.)
- 저장 조건
- 2-8°C
- 용해도
- DMSO: 60°C에서 ≥8mg/mL
- 물리적 상태
- 가루
- 색상
- 흰색에서 황갈색까지
- optical activity
- [α]/D +90 to +106° in methanol (c=1)
- Merck
- 14,6258
- BCS Class
- 1
- 안정성
- 제공된 대로 구매일로부터 1년 동안 안정적입니다. DMSO, 증류수 또는 에탄올 용액은 -20°C에서 최대 1개월 동안 보관할 수 있습니다.
- InChIKey
- LBFBRXGCXUHRJY-HKHDRNBDSA-M
안전
- 위험 및 안전 성명
- 위험 및 사전주의 사항 (GHS)
Montelukast sodium C화학적 특성, 용도, 생산
개요
Montelukast was launched as Singulair in Mexico and Finland for the management of mild to moderate asthma inadequately controlled by inhaled corticosteroids and short-acting beta2-agonists. Montelukast can be obtained by an seven-step synthesis from 3-[2(E)-(7-chloroquinolin-2-yl)vinyl] benzaldehyde. Montelukast is a potent, selective and orally active antagonist of the CysLT1 (formerly called LTD4) receptor, thus blocking the effects of the cysteinyl leukotrienes LTC4, LTD4 and LTE4 on microvascular permeability and the activation of eosinophils. Montelukast represents the third molecule of this class which has been approved in asthma after pranlukast (1995) and zafirlukast (1996). Montelukast has been studied extensively in placebo-controlled clinical trials, in mildly or severe asthmatic patients challenged with LTD4 or exercise. A variety of acute bronchoconstricting challenges were inhibited or attenuated with all doses used. Montelukast demonstrated clinically significant improvements in the parameters of asthma control associated with an appreciable improvement in quality of life., reducing days with asthma exacerbations and allowing significant tapering of corticosteroids. Montelukast is well-tolerated and only needs to be administered once a day.화학적 성질
White or almost white, hygroscopic powder.용도
Montelukast sodium is a potent and highly selective CysLT1 receptor antagonist, without demonstrated CysLT2 activity. It is used to prevent wheezing, difficulty breathing, chest tightness, and coughing caused by asthma in adults and children 12 months of age and older. Montelukast is also used to prevent bronchospasm (breathing difficulties) during exercise in adults and children 6 years of age and older.주요 응용
Montelukast sodium hydrate has been used as a positive control drug to study the protective effects of Gumiganghwal-tang aqueous extract (GGTA) against airway inflammation and pulmonary fibrosis.정의
ChEBI: Montelukast sodium is an organic sodium salt. It contains a montelukast(1-). It is a drug used to treat symptoms of asthma, such as trouble breathing, tight chest, wheezing, coughing, and runny nose. Montelukast sodium blocks the action of a substance that causes airways in the lungs to narrow and causes other symptoms of asthma. It is a type of leukotriene receptor antagonist and a type of antiasthmatic agent. Also called Singulair.Indications
Montelukast sodium is an orally active selective leukotriene receptor antagonist that can specifically inhibit the cysteinyl leukotriene receptor. It was successfully developed by the Merck Company (German) and had entered into market in Canada, Finland, and Mexican in 1997. It is suitable for the prevention and long-term treatment of adults and children asthma, including the prevention of daytime and nighttime asthma symptoms, the treatment of asthma patients who are aspirin-sensitive and prevention of exercise-induced bronchial contraction, it can also be used to relieve the seasonal allergic rhinitis symptoms of 15 year-old or over 15 year-old patients whose symptoms are invalid and intolerant to other treatment.부작용
Common side effects of montelukast include upper respiratory infection, fever, headache, sore throat, cough, stomach pain, diarrhea, earache or ear infection, flu, runny nose, and sinus infection.www.mayoclinic.org
Mode of action
Montelukast selectively and competitively blocks the cysteinyl leukotriene 1 (CysLT1) receptor, preventing binding of the inflammatory mediator leukotriene D4 (LTD4).참고 문헌
1) Lynch?et al.?(1999),?Characterization of the human cysteinyl leukotriene CysLT1 receptor; Nature,?399?789 DOI:10.1038/216582) Jones?et al. (1995),?Pharmacology of montelukast sodium (Singulair), a potent and selective leukotriene D4 receptor antagonist; Can. J. Physiol. Pharmacol.,?73?191 DOI:10.1139/Y95-028
3) Reiss?et al.?(1998),?Montelukast, a once-daily leukotriene receptor antagonist, in the treatment of chronic asthma: a multicenter, randomized, double-blind trial. Montelukast Clinical Research Study Group; Arch. Intern. Med.,?158?1213 DOI:10.1001/ARCHINTE.158.11.1213
4) Zhao?et al.?(2011),?Montelukast, a cysteinyl leukotriene receptor-1 antagonist, attenuates chronic brain injury after focal cerebral ischaemia in mice and rats; J. Pharm. Pharmacol.,?63?550 DOI:10.1111/j.2042-7158.2010.01238.x
5) Lenz?et al.?(2014),?Cysteinyl leukotriene receptor (CysLT) antagonists decrease pentylenetetrazol-induced seizures and blood-brain barrier dysfunction; Neuroscience,?277?859 DOI:10.1016/j.neuroscience.2014.07.058
6) Huber?et al.?(2011)?Inhibition of leukotriene receptors boosts neural progenitor proliferation; Cell Physiol. Biochem.,?28?793 DOI:10.1159/000335793
Montelukast sodium 준비 용품 및 원자재
원자재
메틸마그네슘 염화물
Borane-tetrahydrofuran complex
염화 티오닐
Diethyl 1,1-cyclopropanedicarboxylate
P-클로로아닐린
사염화-1,4-벤조퀴논
사이안화 나트륨
Vinylmagnesium bromide
메탄설포닐 클로라이드
트리에틸아민
N,N-다이아이소프로필에틸아민
테트라뷰틸암모늄 클로라이드
크로톤알데하이드
methyl 2-(2-iodophenyl)propanoate
포타슘터셔리부톡사이드
아세트산 팔라듐 (II)
세륨(III) 클로라이드
MONTELUKAST
준비 용품
Montelukast sodium 공급 업체
글로벌( 742)공급 업체
공급자 | 전화 | 이메일 | 국가 | 제품 수 | 이점 |
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Jinan Jianfeng Chemical Co., Ltd | +8615562555968 |
info@pharmachemm.com | China | 243 | 58 |
Hebei Mojin Biotechnology Co., Ltd | +8613288715578 |
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XI'AN TIANGUANGYUAN BIOTECH CO., LTD. | +86-029-86333380 18829239519 |
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Hebei Guanlang Biotechnology Co,.LTD | +8619930503252 |
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admin@hbdangtong.com | China | 983 | 58 |
Henan Bao Enluo International TradeCo.,LTD | +86-17331933971 +86-17331933971 |
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Sigma Audley | +86-18336680971 +86-18126314766 |
nova@sh-teruiop.com | China | 491 | 58 |
Shaanxi TNJONE Pharmaceutical Co., Ltd | +8618740459177 |
sarah@tnjone.com | China | 1143 | 58 |
Hebei Ganmiao New material Technology Co., LTD | +86-17332992504 +86-17332992504 |
sales8@hbganmiao.com | China | 300 | 58 |
Capot Chemical Co.,Ltd. | 571-85586718 +8613336195806 |
sales@capotchem.com | China | 29798 | 60 |