Summary
There is conflicting data in the literature as to whether subsensitivity of in-vivo β2-adrenoceptor (β2-AR) responses in patients with asthma is due to an endogenous defect of β2-AR or an effect of exogenous β2-agonist therapy. The purpose of the study was to compare in-vitro parameters of lymphocyte β2-AR function in eight age and sex matched normal [FEV1, 98 (2) % predicted] volunteers and asthmatic [FEV1, 60 (5) % predicted] subjects. The asthmatic group were washed out for 4 weeks by substituting inhaled β2-agonist therapy with ipratropium bromide, in order to exclude possible exogenous effects of β2-agonist exposure. Receptor binding affinity (Kd) and density (Bmax) were evaluated using (-)125I-iodocyanopindolol and maximal cAMP response (Emax) was assayed following stimulation with isoprenaline (10−4M).
No significant differences were found between the normal and asthmatic group for Kd (pmol·l−1): 9.65 vs 10.2, Bmax (fmol/106 cells): 1.9 vs 1.6, or Emax (pmol/106 cells): 4.24 vs 4.85.
Thus, parameters of β2-AR function are unaltered in asthmatic patients who have not been exposed to β2-agonists, suggesting that asthma is not associated with an endogenous defect of β2-AR.
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Newnham, D.M., Coutie, W.J.R., McFarlane, L.C. et al. Comparison of parameters of in vitro lymphocyte β2-adrenoceptor function in normal and asthmatic subjects. Eur J Clin Pharmacol 45, 535–538 (1993). https://doi.org/10.1007/BF00315310
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DOI: https://doi.org/10.1007/BF00315310