PHARMACOLOGICAL STUDIES ON 6-AMINO-2-FLUOROMETHYL-3-(O-TOLYL)-4(3H)-QUINAZOLINONE (AFLOQUALONE), A NEW CENTRALLY ACTING MUSCLE RELAXANT (I)

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Neuropharmacological actions of afloqualone were studied in experimental animals. The dose ratio of loss of righting reflex/muscle relaxant activity of afloqualone in mice was larger than those of tolperisone, mephenesin, and chlormezanone. Afloqualone, like tolperisone, mephenesin, and diazepam, inhibited the ipsilateral flexor reflex, but not the patellar reflex. In decerebrate cats, the inhibitory activities of afloqualone and tolperisone on the polysynaptic spinal reflex were reduced to about 1/5 as compared with those in intact preparations, though the activities of diazepam and mephenesin were almost equal in the both preparations. In spinal preparation, the inhibitory activities of afloqualone, tolperisone, and mephenesin were almost equal to those in decerebrate preparations whereas that of diazepam was reduced to about 1/10 as compared with that in decerebrate preparation. Afloqualone and tolperisone inhibited not only the efferent γ-discharges but also the increment and decrement of patellar reflex by stimulation of the lateral and medial reticular formation. These results suggest that the mode of action of afloqualone is different from the actions of mephenesin, chlormezanone, and diazepam. However, afloqualone, unlike tolperisone, showed no influence on the neuro-muscular transmission and inhibited little the muscle spindle discharges.
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