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      Variable Receptor Affinity and Tissue Sensitivity

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          Vascular smooth muscle sensitivity to norepinephrine (NE), measured by contractile responses in vitro, varied in different arteries of the rabbit and also in the same vessels in other species. There was a good correlation between variation in the affinity of NE for the α<sub>1</sub>-adrenoceptor and tissue sensitivity. The variation was continuous and probably not indicative of different receptor subtypes. Solubilization of α<sub>1</sub>-adrenoceptors from the membrane changed the affinity for specific ligands while reconstitution restored it. Taken together, these results suggest the presence of a factor(s) within the receptor microenvironment capable of modulating affinity and hence tissue sensitivity to NE. In some blood vessels, receptor number was correlated significantly with affinity of the α<sub>1</sub>-adrenoceptor for NE also. In general, the contribution of receptor number was considerably less than the affinity for NE.

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          Author and article information

          J Vasc Res
          Journal of Vascular Research
          S. Karger AG
          23 September 2008
          : 28
          : 1-3
          : 115-121
          Department of Pharmacology, University of Vermont, College of Medicine, Burlington, Vt., USA
          158850 Blood Vessels 1991;28:115–121
          © 1991 S. Karger AG, Basel

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          Page count
          Pages: 7
          Signal Recognition and Transduction in Vascular Smooth Muscle


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