Characterization of [3H]losartan receptors in isolated rat glomeruli.

[3H]Losartan bound specifically to isolated rat glomeruli. Scatchard analysis revealed a single class of losartan binding sites with an apparent dissociation constant (KD) of 6.2 nM and a density of receptor sites (Bmax) of 1.2 pmol/mg protein. In comparison, [3H][Sar1,Ala8]angiotensin II binding sites exhibited the same KD value (4.3 nM), but a considerably lower Bmax (52 fmol/mg protein). Moreover whereas [125I][Sar1,Ala8]angiotensin II was almost equally displaced by angiotensin II, [Sar1,Ala8] angiotensin II and losartan, [3H]losartan was potently displaced by losartan only. Finally, [125I][Sar1,Ala8]angiotensin II but not [3H]losartan binding sites were sensitive to guanosine triphosphate (GTP) gamma S and Dithiothreitol. These data, together with the recent demonstration of intrinsic effects of losartan, support the view that [3H]losartan does not label only the angiotensin II type 1 receptor (AT1).