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SOTERENOL AND RELATED COMPOUNDS:MOLECULAR MODIFICATIONS AND CHANGES IN SELECTIVITY, AFFINITY AND EFFICACY AT β‐ADRENOCEPTORS IN GUINEA‐PIG ATRIA AND TRACHEA
Author(s) -
Malta E.,
Raper C.
Publication year - 1977
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.1440-1681.1977.tb02680.x
Subject(s) - selectivity , agonistic behaviour , guinea pig , chemistry , receptor , intrinsic activity , pharmacology , amine gas treating , adrenergic receptor , stereochemistry , structure–activity relationship , medicine , endocrinology , agonist , biochemistry , biology , in vitro , organic chemistry , psychiatry , catalysis , aggression
SUMMARY 1. Beta‐adrenoreceptor agonistic and antagonistic actions of soterenol and structurally‐related compounds have been assessed in guinea‐pig atrial and tracheal preparations. 2. Changes in the nature and position of the ring substituents affect the type of response obtained (agonistic and/or antagonistic) and the P1/P2‐adrenoceptor selectivity of the compounds. 3. Changes in amine substitution produce little change in pA 2 values, but produce marked alterations in pD 2 values and in the selectivity of the drugs as agonists at β 1 ‐and β 2 ‐receptors. These results suggest that differences in efficacy rather than affinity determine the nature of the agonistic effects obtained.