Adrenergic mimetics have many varied pharmacological applications, thus the quest for selective and efficacious ligands. Provided that a reasonable receptor model can be constructed which mimics the key interactions between a ligand and its biological receptor, molecular modelling offers the potential for rational drug design. The beta 2-adrenergic receptor models reviewed in this article have increased in sophistication, in line with more information becoming available about the residues involved in ligand binding, as well as the topography of the receptor.