[Pharmacologic profile of dithiadenoxide, a potential non-sedating H1-antihistaminic]

Dithiadenoxide, a product of metabolic S-oxidation of the H1-antihistaminic agent dithiaden (bisulepin, Dithiaden), is also an effective histaminic H1-antagonist in pharmacological experiments in in vivo conditions. In contrast to dithiaden, dithiadenoxide exerts a demonstrable inhibitory action as much as the subtoxic or sublethal dosage in experiments in mice and rats. Its acute toxicity in mice and guinea-pigs substantially decreases; acute toxicological findings in rats are not unambiguous. Other experimental findings demonstrate higher selectivity of pharmacological effects of dithiadenoxide.