ラットの脳波および行動に及ぼす4-(p-chlorobenzyl)-2-[N-methylperhydroazepinyl-(4)]-1-(2H)-phthalazinone hydrochloride(Azelastine)の影響

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The effect of azelastine, a new anti-allergic agent which possesses a variety of anti-allergic effects in addition to its H<SUB>1</SUB>-blocking action, on the central nervous system was studied by observing the changes in EEG and behavioral state in unanesthetized rats. Certain H1-receptor antagonists such as promethazine, diphenhydramine, and homochlorcyclizine induced the drowsy pattern in EEGs at doses less than 5mg/kg. The pattern is characterized by high voltage and slow waves and is not interrupted by auditory stimulation. At 5mg/kg both promethazine and diphenhydramine blocked the EEG arousal response induced by electrical stimulation of the midbrain reticular formation (0.5 msec, 4V, 100 Hz for 5 sec). Diphenhydramine also diminished the photic driving responses significantly. Even at 10mg/kg (iv), azelastine had little EEG effect and did not prevent the EEG arousal responses provoked by both auditory and reticular stimulations. Further, the photic driving response was not inhibited at all by the same dosage of azelastine.
一般社団法人日本臨床薬理学会の論文