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research purposes under agreement from GlaxoSmithKline
Chemical Name:4-Hydroxy-a1-[[[6-(4-phenylbutoxy)hexyl]amino]methyl]-1
,3-benzenedimethanol
Biological Activity:
Potent
and selective β2-adrenoceptor agonist (EC50
= 5.3 nM); bronchodilator. Unlike other β2 agonists, binds to exo-site domain
of β2 receptors, producing a slow onset of action and
prolonged activation.
Johnson et al (1993) The pharmacology of
salmeterol. Life Sci. 52 2131. Ellis et al (1995)
Correlation of cyclic AMP accumulation and relaxant actions of salmeterol and
salbutamol in bovine tracheal smooth muscle. Br.J.Pharmacol. 116
2510. Clarket al (1996) Stable activation and desensitization of
beta 2-adrenergic receptor stimulation of adenylyl cyclase by salmeterol:
evidence for quasi-irreversible binding to an exosite. Mol.Pharmacol. 49
182.
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