아포모테롤

아포모테롤
아포모테롤 구조식 이미지
카스 번호:
67346-49-0
한글명:
아포모테롤
동의어(한글):
아포모테롤
상품명:
(R,R)-Formoterol
동의어(영문):
Arformoterol;(R,R)-Formoterol;Arformoterol 13D3;Formoterol Impurity 10;(R,R)-Formoterol (Arformoterol);(-)-FORMOTEROL; ARFORMOTEROL; FORMOTEROL;Formoterol Impurity 10((R,R)-Formoterol)(Arformoterol);4-[(1R)-2-[[(1R)-2-(4-Methoxyphenyl)-1-methylethyl]amino]-1-hydroxyethyl]-2-(formylamino)phenol;N-[2-Hydroxy-5-[(1R)-1-hydroxy-2-[[(αR)-α-methyl-4-methoxyphenethyl]amino]ethyl]phenyl]formamide;N-[2-hydroxy-5-[(1R)-1-hydroxy-2-[[(2R)-1-(4-methoxyphenyl)propan-2-yl]amino]ethyl]phenyl]formamide
CBNumber:
CB81237087
분자식:
C19H24N2O4
포뮬러 무게:
344.4
MOL 파일:
67346-49-0.mol

아포모테롤 속성

녹는점
73-75 °C
끓는 점
603.2±55.0 °C(Predicted)
밀도
1.233±0.06 g/cm3(Predicted)
용해도
25℃: DMSO
물리적 상태
가루
산도 계수 (pKa)
8.95±0.50(Predicted)

안전

아포모테롤 C화학적 특성, 용도, 생산

개요

Arformoterol, a selective long-acting b2-agonist, was launched as an inhalation solution for treatment of bronchoconstriction associated with COPD. It is the active (R,R)-enantiomer of the previously marketed b2-agonist formoterol, which is registered as a racemic mixture. Similar to other b2-agonists, the mechanism of action of formoterol and arformoterol involves activation of adenyl cyclase, leading to increased production of cyclic adenosine monophosphate (cAMP) via ATP. Increased levels of intracellular cAMP result in relaxation of the bronchial smooth muscle, and also prevent mast cells from releasing inflammatory mediators. Arformoterol has high binding affinity for the human b2 receptor (Kd 2.9 nM) and approximately 39-fold selectivity over the b1 receptor (Kd 113 nM). It is W1,000 times more potent b2 ligand than the corresponding (S,S)-enantiomer (Kd 3100 nM), and twice as potent as racemic formoterol (Kd 5.2 nM). Additionally, arformoterol acts as a full or nearly full agonist of the b2 receptor, whereas the (S,S)-enantiomer acts as an inverse agonist. Therefore, the (R,R)-enantiomer may account exclusively for the activation of b2 receptors by the racemic mixture.

용도

(R,R)-Formoterol (Arformoterol) (CAS# 67346-49-0) is aused in the methods for treating chronic obstructive pulmonary disease by administration of a bronchodilator using a nebulizer.

정의

ChEBI: An N-[2-hydroxy-5-(1-hydroxy-2-{[1-(4-methoxyphenyl)propan-2-yl]amino}ethyl)phenyl]formamide in which both of the stereocentres have R configuration. The active enantiomer of formoterol, it is administered by inhalation generally as the tartrate salt) as a direct-acting sympathomimetic and bronchodilator for the treatment of chronic obstructive pulmonary disease (any progressive respiratory disease that makes it harder to breathe over time, such as chronic bronchitis and emphysema).

아포모테롤 준비 용품 및 원자재

원자재

준비 용품


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