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      Affinities of Adrenergic Drugs for α 2-Adrenoceptors in Dog Saphenous Vein in Comparison with Those in Rat Brain or Human Platelets

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          The affinities of drugs for the postsynaptic α<sub>2</sub>-adrenoceptors in the dog saphenous vein were examined and compared with those in human platelets or in rat brain. The pA<sub>2</sub> or pD<sub>2</sub> values in the vein were determined in the presence of phenoxybenzamine. The pKi values (dissociation constant) of drugs for binding to α<sub>2</sub>-adrenoceptors in human platelets or in rat brain were determined by radioligand binding assay using <sup>3</sup>H-yohimbine (YOH) or <sup>3</sup>Hclonidine (CLO) as ligands. The binding of agonists to <sup>3</sup>H-YOH binding sites was carried out in the presence of GTP. The pA<sub>2</sub> or pD<sub>2</sub> values in the vein had a good correlation with pKi values for YOH sites but not with those for CLO sites in rat brain. The pKi values for YOH sites in human platelets had a good correlation with those for YOH sites in the brain or with pA<sub>2</sub> or pD<sub>2</sub> values in the vein. These results suggested that the affinities of adrenergic drugs for postsynaptic α<sub>2</sub>-adrenoceptors in the dog saphenous vein are similar to those in brain and in platelets, and it is probable that the adrenergic drugs produce their α<sub>2</sub>-adrenoceptor-mediated effects on vascular tissues primarily through binding to a low-affinity form of the α<sub>2</sub>-adrenoceptors.

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          Author and article information

          J Vasc Res
          Journal of Vascular Research
          S. Karger AG
          23 September 2008
          : 22
          : 3
          : 127-138
          Department of Pharmacology, Hamamatsu University School of Medicine, Hamamatsu, Japan
          158590 Blood Vessels 1985;22:127–138
          © 1985 S. Karger AG, Basel

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          Pages: 12
          Research Paper


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