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AGONISTIC AND ANTAGONISTIC ACTIONS OF 3,4‐DmYDROXY‐SUBSTITUTED PHENOXYPROPANOLAMINES DM GUINEA‐PIG ATRIA AND TRACHEA
Author(s) -
Keh G. S.,
Raper C.,
Dowd H.
Publication year - 1978
Publication title -
clinical and experimental pharmacology and physiology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.752
H-Index - 103
eISSN - 1440-1681
pISSN - 0305-1870
DOI - 10.1111/j.1440-1681.1978.tb00689.x
Subject(s) - potency , agonistic behaviour , carbachol , isoprenaline , chemistry , guinea pig , stereochemistry , agonist , pharmacology , receptor , endocrinology , medicine , ic50 , biology , biochemistry , stimulation , in vitro , psychiatry , aggression
SUMMARY 1. Racemic mixtures of noradrenaline, adrenaline, isoprenaline, N‐r‐butylnor‐adrenaline and their corresponding derivatives containing an oxymethylene (OM) link between the phenyl ring and ethanolamine side‐chain have been tested for their effects on β‐adrenoceptors in isolated guinea‐pig atrial and tracheal preparations. 2.In atrial and in spontaneously contracted tracheal preparations both the parent catecholamines and their corresponding OM‐derivatives had a similar order of potency as 0‐receptor agonists. 3.In carbachol‐stimulated tracheal preparations the OM‐derivatives were shown to have partial agonistic actions. 4.As in other phenylethanolamines and phenoxypropanolamines, both the agonistic and antagonistic potency of the OM‐derivatives increased with increasing amine substitution.