Abstract
Because of the lack of direct measurement of sympathetic activity, lymphocytes (LY) which contain the same β-adrenoceptor (R)-subtype as the bronchial tree have been introduced as an easy available in vitro model to study β-adrenoceptors (R). Although widely used in prevention of bronchial asthma the mode of action of most antiasthmatic drugs, including prednisolone (PRED), sodium comoglycate (SCG) and ketotifen (KET) remains to be obscure. Since some of these drugs have been reported to influence the adrenergic system in different tissues we have investigated the effects of fenoterol (FENO), PRED, SCG and KET on R of LY. Number and affinity have been quantitatively determined by binding with the radioligand 125[I]-Cyanopindolol.- FENO(4×0.4mg per inhal./d) down regulated the number of R to 40%. PRED (2mg/kg/d) and SCG (4×2mg per inhal./d) were able to prevent this down regulation.In addition PRED increased the basal number of R, whereas SCG did not. A one week treatment with KET (0.2 mg/kg/d) had no influence on R. Since down regulation produced by β-sympathomimetics is suggested to be due to an internalisation of the drug-R-complex from the cell surface into the cytoplasma PRED and SCG may evoke some of their effects by inhibiting this process.PRED may have a further different mode of action, perhaps on the R-synthesis.
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Reinhardt, D., Ludwig, J. ANTIASTHMATIC DRUGS AND THEIR EFFECTS ON β-ADRENOCEPTORS OP LYMPHOCYTES FROM ASTHMATIC CHILDREN. Pediatr Res 19, 1122 (1985). https://doi.org/10.1203/00006450-198510000-00294
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DOI: https://doi.org/10.1203/00006450-198510000-00294