Characteristics of (3H)E-643-binding to alpha adrenoceptors.

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Abstract
Radiolabeled E-643, a newly developed antihypertensive compound, bound specifically to a preparation obtained from rat brain with a maximum of 85 f[femto]mol of binding sites per mg protein and a Kd of 0.59 nM. Prazosin markedly inhibited the binding, while yohimbine and clonidine were only weak inhibitors. Other characteristics of the binding of [3H]E-643 to the brain and its specific binding to preparations of peripheral rat organs were also studied. [3H]E-643 may be useful for labeling .alpha.1-adrenoceptors.