Salmeterol xinafoate Chemical Properties

Melting point:

137-138°C

storage temp. 

2-8°C

solubility 

H₂O: slightly soluble

form 

solid

color 

white

Merck 

14,8337

InChIKey

XTZNCVSCVHTPAI-UHFFFAOYSA-N

CAS DataBase Reference

94749-08-3(CAS DataBase Reference)

Safety Information

Hazard Codes 

Xi

Risk Statements 

36/37/38

Safety Statements 

22-24/25-36-26

WGK Germany 

3

RTECS 

QJ1970500

HS Code 

2922504500

MSDS

• Language:English Provider:SigmaAldrich

Salmeterol xinafoate Usage And Synthesis

Description

Salmeterol hydroxynaphthoate is a new long-acting β2-selective adrenoceptor agonist introduced as a bronchodilator for the treatment of reversible airway obstruction in asthma and chronic bronchitis. It has bronchodilatory activity as intense and four times longerlasting than equivalent doses of salbutamol. Salmeterol hydroxynaphthoate is reported to be the first bronchodilator with significant anti-inflammatory activity and hence could complement prophylactic corticosteroid therapy.

Description

Salmeterol is a long-acting β₂-adrenergic receptor agonist (β₂-AR; EC₅₀s = 0.79, 63.1, and 9.4 nM for β₂-, β₁-, and β₃-ARs, respectively). It inhibits electrically-stimulated contraction of isolated guinea pig trachea strips (EC₅₀ = 2.51 nM) and histamine-induced bronchoconstriction in guinea pigs via aerosol administration of doses ranging from 0.12 to 12 mM. Salmeterol binds to an exosite domain of β₂-adrenergic receptors, producing a slow onset of action and prolonged activation. Formulations containing salmeterol have been used in the treatment of asthma, including exercise-induced asthma, and chronic obstructive pulmonary disease.

Chemical Properties

White to Off-White Solid

Originator

Glaxo (United Kingdom)

Uses

A ?-Adrenergic agonist. Structural analog of albuterol

Uses

A β2-Adrenergic agonist. Structural analog of Albuterol (A514500).

Uses

Smooth wheezing anti-inflammatory

Uses

Bronchodilator; Beta2-adrenoceptor agonist

Application

Salmeterol xinafoate is a potent and selective β2-adrenoceptor agonist (EC50 = 5.3 nM) that displays bronchodilator actions. Unlike other β2- adrenoceptor agonists, Salmeterol binds to exo-site domain of β2-AR receptors, producing a slow onset of action and prolonged activation. Clinically used for the treatment of asthma and chronic obstructive pulmonary disease(COPD).

Definition

ChEBI: Salmeterol xinafoate is a naphthoic acid.

brand name

Serevent (GlaxoSmithKline).

Biochem/physiol Actions

β2-adrenoceptor agonist.

storage

Desiccate at RT

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