Non-Adrenergic Binding Sites for the “α-Antagonist” [³H] Idazoxan in Rabbit Urethral Smooth Muscle

Abstract

In the present study, we have provided evidence that [³H] rauwolscine and [³H] idazoxan bind to different sites in rabbit urethra. The [³H] idazoxan capacity and affinity was 215 ± 14 fmol/mg protein and 1.59 ± 0.16 nM while [³H] rauwolscine binding parameters were 45.9 ± 3.4 fmol/mg protein and 2.39 ± 0.27 nM. [³H] idazoxan specific binding was inhibited only by compounds possessing an imidazoli(di)ne or a guanidinium moiety, while [³H] rauwolscine specific binding was inhibited by phenylethanolamines and classical α-antagonists. [₃H] idazoxan was inhibited by KCI in a competitive and by MnCI₂ in a non-competitive way, while other cations such as Na⁺, Li⁺ and Mg²⁺ did not inhibit [³H] idazoxan binding. Moreover, we investigated the regional distribution of [³H] idazoxan and [³H] rauwolscine along the rabbit urethra using quantitative autoradiography. Analysis of the films revealed a different distribution of these two binding sites on the urethral sections.