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(Chest. 1983;83:339-340.)
© 1983 American College of Chest Physicians

Characterization of Central agr-Adrenoceptors Using 3H-Clonidine and Its Derivatives

Bevyn Jarrott Ph.D., Pharm.1; William J. Louis M.D.1; and Roger J. Summers Ph.D., B.Pharm.1

1 From the Clinical Pharmacology and Therapeutics Unit, Department of Medicine, University of Melbourne, (Austin Hospital), Heidelberg, Victoria, Australia

agr-adrenoceptors in brain can be studied readily by radioligand binding techniques. This provides valuable information not only on the distribution of receptors in brain regions, but also on the regulation of receptors. The usefulness of this technique is dependent in part on a radioligand with high specificity for the receptor under study. Our studies have shown that 3H-clonidine does not bind exclusively to agr2-adrenoceptor subtypes, but also interacts with agr1-adrenoceptors. In contrast, 3H-guanfacine labels a high affinity agr2 subtype with good selectivity, but 3H-lofexidine probably labels with both agr2 and agr1-adrenoceptor binding sites.






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Copyright © 1983 by the American College of Chest Physicians.