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      Alpha-Adrenoreceptor-Related Dissociation Constants and Intrinsic Efficacies of Stereoisomers of Epinephrine


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          The α-adrenoreceptor-related dissociation constant and intrinsic efficacy of the stereoisomers of epinephrine were determined on the rabbit aortic strip. (–)-Epinephrine showed higher affinity than (+)-epinephrine or the desoxy analogue epinine. Efficacy of (+)-epinephrine relative to (–)-epinephrine was low (relative efficacy, e<sub>r</sub> = 0.44). Epinine had about the same affinity and efficacy as (+)-epinephrine. When the α-adrenoreceptors were protected against dibenamine by an equimolar concentration of the isomers, (–)-epinephrine was found to be more effective than (+)-epinephrine or epinine. These results suggest that the stereoisomers of catecholamines differ not only in affinity but also in intrinsic efficacy.

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          Author and article information

          J Vasc Res
          Journal of Vascular Research
          S. Karger AG
          19 September 2008
          : 18
          : 4-5
          : 145-152
          College of Pharmacy, The Ohio State University, Columbus, Ohio, USA
          158349 Blood Vessels 1981;18:145–152
          © 1981 S. Karger AG, Basel

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          Pages: 8
          Research Paper


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