SOTERENOL AND RELATED COMPOUNDS:MOLECULAR MODIFICATIONS AND CHANGES IN SELECTIVITY, AFFINITY AND EFFICACY AT β‐ADRENOCEPTORS IN GUINEA‐PIG ATRIA AND TRACHEA

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Abstract
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 pA2 values, but produce marked alterations in pD2 values and in the selectivity of the drugs as agonists at β1‐and β2‐receptors. These results suggest that differences in efficacy rather than affinity determine the nature of the agonistic effects obtained.