A β2-AR agonist; selectively binds to β1- over β2-ARs (Kds = 2.9 and 113 nM

Arformoterol (tartrate) – 50 mg

Brand:
Cayman
CAS:
200815-49-2
Storage:
-20
UN-No:
Non-Hazardous - /

Aformoterol is the (R,R)-enantiomer of the β2-adrenergic receptor (β2-AR) agonist formoterol (Item No. 15584).{43065} It selectively binds to β1- over β2-ARs (Kds = 2.9 and 113 nM, respectively) as well as β3-adrenergic, B2 bradykinin, neurokinin 1 (NK1) and NK2 receptors when used at concentrations up to 3 μM. Aformoterol induces cAMP accumulation in cultured human bronchial epithelial cells. Ex vivo, aformoterol (0.01-1,000 nM) induces dose-dependent relaxation of guinea pig tracheal strips precontracted with carbamoylcholine (Item No. 14486), ovalbumin, or histamine (pD2s = 8.4, 9.5, and 9.5, respectively). In vivo, aformoterol reverses histamine- and ovalbumin-induced bronchoconstriction in guinea pigs (ED50s = 1 and 40 nmol/kg, respectively). Formulations containing aformoterol have been used in the treatment of chronic obstructive pulmonary disease (COPD).  

 

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Description

A β2-AR agonist; selectively binds to β1- over β2-ARs (Kds = 2.9 and 113 nM, respectively) as well as β3-adrenergic, B2 bradykinin, NK1 and NK2 receptors up to 3 μM; induces cAMP accumulation in cultured human bronchial epithelial cells; relaxes guinea pig tracheal strips precontracted with carbamoylcholine, ovalbumin, or histamine (pD2s = 8.4, 9.5, and 9.5, respectively); reverses histamine- and ovalbumin-induced bronchoconstriction in guinea pigs (ED50s = 1 and 40 nmol/kg, respectively)

Formal name: N-[2-hydroxy-5-[(1R)-1-hydroxy-2-[[(1R)-2-(4-methoxyphenyl)-1-methylethyl]amino]ethyl]phenyl]-formamide, (2R,3R)-2,3-dihydroxybutanedioate

Synonyms:  (R,R)-Formoterol

Molecular weight: 494.5

CAS: 200815-49-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Cardiovascular System|Cardiovascular Diseases||Research Area|Cardiovascular System|Heart|Arrhythmia

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