5,5-ジエチル-2,3,5,6-テトラヒドロ-4H-1,3-オキサジン-2,4-ジオン

EFFECTS OF ANTIEPILEPTIC DRUGS ADMINISTERED 1-4 DAYS BEFORE ON CONVULSANT EFFECTS OF DIOXONE WERE STUDIED IN MICE. METHYLPHENOBARBITAL, PRIMIDONE & METHOIN ENHANCED THE EFFECT WHEN GIVEN 2 DAYS PRIOR TO DIOXONE ADMINISTRATION. SODIUM PHENYTOIN HAD AN ANTICONVULSANT EFFECT IN THE FIRST 2 DAYS & AFTER 4 DAYS THE DOSAGE OF DIOXONE NECESSARY TO INDUCE CONVULSIONS IN 50 OF THE ANIMALS WAS DIMINISHED.

THE HYPNOTICS, PENTOBARBITONE SODIUM & HYDROXYDIONE WERE TITRATED BY DIETHADIONE USING HYPNOSIS IN 50 MICE AS THE TITRATION END-POINT. ANTAGONISM OF HYPNOSIS BY DIETHADIONE MAY BE COMPETITIVE OR NONCOMPETITIVE.

THE QUANTITY OF HYPNOTIC, AMYLOBARBITONE SODIUM, REQUIRED TO MAINTAIN THE TITRATION END-POINT HYPNOSIS IN 50 MICE IN PRESENCE OF INCREASING DOSES OF ANALEPTICS SUCH AS BEMEGRIDE, DIETHADIONE, PICROTOXIN, PENTYLENETETRAZOLE, & BETA-SPIROCYCLOPENTANEGLUTARIMIDE WAS STUDIED. WITH THE EXCEPTION OF PICROTOXIN, TITRATION CURVES SHOWED A REVERSAL IN SLOPE AT THE HIGHEST DOSES, & DIETHADIONE ENHANCED THE DEPRESSANT ACTION OF THE HYPNOTIC. THESE ANALEPTICS & THE HYPNOTIC PROBABLY ALL ACT AT THE SAME EXCITATORY SYNAPSES, THE FORMER AS AGONISTS & THE LATTER AS COMPETITIVE OR NONCOMPETITIVE ANTAGONIST.

MEDICATION: CNS STIMULANT

ANALEPTIC AGENT

TESTA ET AL, J ORG CHEM 24, 1928 (1959); BRITISH PATENT 855,244 (1960 TO LEPETIT, SPA).

PROBABLY BY REACTION OF ALPHA,ALPHA-DIETHYL-BETA-CARBAMOYLOXYPROPIONIC ACID WITH THIONYL CHLORIDE FOLLOWED BY REACTION WITH PYRIDINE