Characterization of imidazoline-guanidinium receptive sites in renal medulla from human kidney.

Previous studies showed that alpha 2-adrenergic receptors and imidazoline-guanidinium receptive sites (IGRS) are colocalized in rabbit and human renal proximal tubule. In the present study we investigated the localization of these two binding sites in the renal medulla from human kidney. Binding studies performed with [3H]idazoxan (IGRS ligand) and [3H]rauwolscine (alpha 2-adrenergic ligand) showed that, in membrane preparations from renal medulla, the density of IGRS was 3.6-fold higher than that of alpha 2-adrenergic receptors (134 +/- 7 v 37 +/- 5 fmol/mg protein, respectively). These data indicate that imidazoline, guanidinium, and oxazoline derivatives could induce their therapeutic effects through the interaction with IGRS and/or alpha 2-adrenergic receptors located not only in the renal proximal tubule but also in other segments of the nephron.