Comparative beta-adrenoceptor blocking effects of propranolol, bisoprolol, atenolol, acebutolol and diacetolol on the human isolated bronchus.
Five beta-adrenoceptor blockers, propranolol, acebutolol, diacebutolol, atenolol and bisoprolol, were tested for their antagonistic effect against isoprenaline on human isolated bronchi. The results showed (1) that only propranolol exerted a competitive antagonistic effect against isoprenaline (pA2 = 9.40 +/- 0.22, n = 7) whereas the other drugs did not, and (2) that, in the presence of beta-adrenoceptor blockers in the plasma concentrations reported after a single usual therapeutic dose, the doses of isoprenaline giving the same bronchodilator effect must be multiplied by 32.6, 5.51, 4.63, 2.82 and 1.95 respectively with propranolol, diacetolol, acebutolol, atenolol, and bisoprolol. It was concluded that (1) atenolol and bisoprolol were the least potent drugs at bronchial level in therapeutic plasma concentrations and (2) that tests performed on the human isolated bronchus might be a useful screening procedure for new drugs with potential activity on the airways.
Naline
E
E
Laboratoire de Pharmacologie, Faculté de Médecine Paris-Ouest, France.
Sarria
B
B
Ertzbischoff
O
O
Ozanne
P
P
Advenier
C
C
D000319:Adrenergic beta-Antagonists / Q000494:pharmacology*; D001980:Bronchi / Q000187:drug effects; D006801:Humans; D066298:In Vitro Techniques; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects*
D000319:Adrenergic beta-Antagonists