Edwards R M, Trizna W, Stack E J
Department of Renal Pharmacology, SmithKline Beecham Pharmaceuticals, King of Prussia, PA 19406-0939, USA.
Eur J Pharmacol. 1998 Mar 19;345(2):229-32. doi: 10.1016/s0014-2999(98)00090-9.
[125I]Endothelin-1 bound with high affinity to a single site on both brush border membranes (Kd=192+/-26 pM. Bmax=314+/-49 fmol/mg) and basolateral membranes (Kd=94.7+/-3.4 pM, Bmax=612+/-107 fmol/mg) isolated from rat renal cortex. Competition binding experiments using subtype selective ligands revealed that the proportion of ET(B) to ET(A) receptors was 80:20 and 60:40 in the brush border membrane and the basolateral membrane, respectively. The results demonstrate that endothelin-1 binds to brush border membranes, and that endothelin ET(B) receptors may be involved in the previously described effects of endothelin-1 on brush border membrane Na+ transport.