Asthma is a significant health problem worldwide with a prevalence that continues to rise and for which there is no cure. Animal models have been used for decades to investigate the cause and cures of asthma, and while they do not always mimic many of the facets of this syndrome, mechanistic animal studies are still nevertheless very useful. Animal studies with beta-agonists suggest much broader and perhaps more important roles for beta-agonists since beta-agonists reduce aspects of inflammation and may affect structural remodeling. Studies using enantiomers of beta-agonists provide a confusing picture of the degree and mechanism of the deleterious effects of racemic mixtures and/or the S-enantiomer or other classes of beta-agonists. Neural mechanisms are implicated. The future holds a promise of even more insight into the mechanisms of the acute and chronic role of the beta-adrenoceptor, asthma therapeutics, in particular, beta-agonists that will lead to a better understanding of the pathogenesis and treatment of asthma.