Abstract
[ 3H]Idazoxan is a labelled ligand that is frequently used to study α 2-adrenoceptors in the central nervous system. In pig kidney membranes, [ 3H]idazoxan labelled high-affinity binding sites (K d = 1.5 nM) that were not α 2-adrenoptors and which recognized clonidine with low affinity. This new class of binding sites was recognized by amiloride derivatives; however, it is not likely that these sites are the well-known targets of amiloride in the kidney: the Na +/H + exchanger and the epithelium Na + channel. These binding sites may be the normal target of a series of imidazolidines derivatives (guanabenz, guanochlor, guanoxan), which are known for their antihypertensive properties.
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