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CHARACTERIZATION OF THE RECEPTOR MEDIATING THE ANTI‐ANAPHYLACTIC EFFECTS OF β‐ADRENOCEPTOR AGONISTS IN HUMAN LUNG TISSUE in vitro
Author(s) -
BUTCHERS P.R.,
SKIDMORE I.F.,
VARDEY C.J.,
WHEELDON A.
Publication year - 1980
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.1476-5381.1980.tb10987.x
Subject(s) - practolol , isoprenaline , atenolol , salbutamol , antagonist , receptor , propranolol , endocrinology , chemistry , medicine , pharmacology , terbutaline , biology , stimulation , asthma , blood pressure
1 The rank order of potency of six β‐adrenoceptor agonists as inhibitors of the anaphylactic release of histamine from fragments of passively sensitized human lung in vitro was (‐)‐isoprenaline > (‐)‐adrenaline > (±)‐salbutamol > (‐)‐noradrenaline > R0363 > H133/22. 2 The β‐adrenoceptor antagonists, propranolol, atenolol and H35/25, blocked the response to both (‐)‐isoprenaline and (±)‐salbutamol competively. Each antagonist gave similar pA 2 values with both agonists. pA 2 values were consistenly at the high end of the range expected for interaction at a β 2 ‐adrenoceptor. 3 Practolol did not antagonize isoprenaline in a competitive manner but was a competitive antagonist of salbutamol with a pA 2 at the high end of the range expected for interaction at a β 2 ‐adrenoceptor. 4 Data obtained with agonists are consistent with the receptor being of the β 2 ‐subtype. Data obtained with antagonists indicate a consistently higher affinity for the receptor than observed for the β 2 ‐subtype in other tissues but do not suggest a novel β‐adrenoceptor subtype on the mast cell of the human lung.