Tetraethylammonium transport in renal brush border membrane vesicles of the rabbit.

The mechanisms involved in the transport of tetraethylammonium (TEA) in the rabbit renal brush border were investigated by using membrane vesicles. Transport of [14C]TEA (0.2 mM) was measured by a rapid filtration method. We have reported previously that an imposed pH gradient (pHi = 6, pHo = 7.4) stimulates the uptake of TEA markedly, yielding a transient overshoot of 200% above the equilibrium value. Here we demonstrate that an overshoot of similar magnitude can also be obtained in the presence of indirectly induced proton gradients, via the naturally occurring Na+/H+ exchanger or via the artificial K+/H+ exchanger nigericin. The TEA exchange mechanism is shown to be electroneutral, temperature-dependent and saturable [Km, 0.328 (CL for P less than .05: 0.250-0.425) mM; Vmax, 2.13 (CL for P less than .05: 1.98-2.32) nmole/mg of protein X 15 sec]. Other organic cations interact with this exchange mechanism: mepiperphenidol and morphine both cis-inhibited and trans-stimulated TEA uptake. Quinine, which was the most potent inhibitor of TEA uptake (57% inhibition at 10(-5) M), did not trans-stimulate. The mechanism appears to be specific for organic cations inasmuch as the organic anion p-aminohippurate did not cis-inhibit or trans-stimulate TEA uptake. These results demonstrate the presence of a H+/TEA exchange mechanism in the rabbit renal brush border membrane showing many similarities with that shown to be present in the rat.