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Salmeterol: a potent and long‐acting inhibitor of inflammatory mediator release from human lung
Author(s) -
Butchers P.R.,
Vardey C.J.,
Johnson M.
Publication year - 1991
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1991.tb12487.x
Subject(s) - salmeterol , histamine , salbutamol , pharmacology , leukotriene , leukotriene d4 , chemistry , isoprenaline , agonist , propranolol , leukotriene c4 , ic50 , endocrinology , medicine , receptor , in vitro , asthma , biochemistry , stimulation
1 The effects of salmeterol, a novel long‐acting β 2 ‐adrenoceptor agonist, have been investigated on antigen‐induced mediator release from passively sensitized fragments of human lung in vitro.2 Salmeterol was a potent inhibitor of the release of histamine (–log IC 50 = 8.54), leukotriene C 4 (LTC 4 )/LTD 4 (–log IC 50 = 9.07) and prostaglandin D 2 (–log IC 50 = 8.81). It was slightly less potent (1–3 fold) than isoprenaline, but significantly more potent (10–35 fold) than salbutamol. 3 Propranolol competitively antagonized the inhibitory effects of salmeterol on histamine release (pA 2 = 8.41) and LTC 4 /LTD 4 release, (pA 2 = 8.40) indicating an action via β‐adrenoceptors. 4 The inhibitory effects of isoprenaline (20 n m ) and salbutamol (200 n m ) were removed after washing the lung tissue for 2 h and 4 h respectively. In contrast, the inhibitory effects of salmeterol (40 n m ) were much longer‐lasting, and were still evident after 20 h. 5 Salmeterol therefore exhibits potent and persistent inhibition of anaphylactic mediator release from human lung. This anti‐inflammatory effect may be important for the therapeutic potential of salmeterol in the treatment of bronchial asthma.