Changes in the activity of β2-adrenergic receptors of human T-lymphocytes under the effect of salbutamol (a short-acting β2-agonist) have been evaluated with a new modified radioligand method utilizing [125I]cyanopindolol and a specific ligand ICI 118551. In healthy volunteers, the receptor activity decreased after 30 min upon the inhalation of salbutamol and restored to the initial level after 2 h. At the same time, there were changes in the transcription level of the ADRB2 gene, which encodes the protein component of the β2-adrenoreceptor. The dynamics of β2-adrenergic receptor activity of T-lymphocytes after salbutamol treatment in patients with cardiorespiratory pathology significantly differed from that in healthy volunteers.