Expression of three human β‐adrenergic‐receptor subtypes in transfected chinese hamster ovary cells

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Abstract
The genes coding for three pharmacologically distinct subtypes of human β‐adrenergic receptors (β1AR, β2AR and β3AR) were transfected for expression in Chinese hamster ovary (CHO) cells. Stable cell lines expressing each receptor were analyzed by ligand binding, adenylate cyclase activation and photoaffinity labeling, and compared to βAR subtypes observed in previously described tissues, primary cultures and transfected cell lines. Each of the three receptor subtypes displayed saturable [125I]iodocyanopindolol‐binding activity. They showed the characteristic rank order of potencies for five agonists, determined by measuring the accumulation of intracellular cAMP. These recombinant cell lines express a homogeneous population of receptors and display the known pharmacological properties of β1AR and β2AR, in human tissues. It is therefore likely that the pattern of ligand binding and adenylate cyclase activation, mediated by the new β3AR in CHO cells, also reflects the yet‐undetermined pharmacological profile in humans.