Cation sensitivity of [125I]heat binding to alpha 1-adrenoceptors in rat cerebral cortex membranes.

The alpha 1-adrenoceptor antagonist 2-[beta-(4-hydroxyphenyl)-ethylaminomethyl] tetralone (HEAT) was radiolabeled with 125I and purified to the maximal specific radioactivity of 2200 Ci/mmol. [125 I]HEAT selectively labels alpha 1-adrenoceptors (KD approximately 0.1 nM at 30 degrees C) in rat cerebral cortex membranes. Divalent cations stimulated [125 I]HEAT binding to the alpha 1-adrenoceptors. The rank order of potencies was Ni2+ greater than Mn2+ greater than Mg2+ greater than Ca2+ approximately Sr2+. The effect of Mg2+ was mainly on the Bmax of the alpha I-adrenoceptors. Monovalent cations also stimulated [125I]HEAT binding. Maximal stimulation (up to 3-fold) was seen with Na+ (optimal concentration at approximately 150 mM). Li+ and NH4+ were less effective whereas K+ was ineffective. The stimulation of [125I]HEAT binding to alpha I-adrenoceptors by Na+ was temperature-dependent.