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1 Research Division, Mount Laboratories, Inc., New Brunswick, New Jersey
2,2-Diethyl-1,3-propanediol, called DEP, possesses very strong antagonistic properties to the convulsant and lethal effects of pentamethylenetetrazol (Metrazol), strychnine and Picrotoxin. These antagonistic effects occur with doses which do not possess hypnotic or anesthetic action. DEP can be effectively administered enterally or parenterally. The duration of action of the drug is short.
DEP does not affect spinal reflexes and has little action on the spinal cord. It exerts its action by a depressant effect on the forebrain and midbrain.
Evidence has been obtained which indicates that DEP is in part conjugated in the body as an ether type glucuronide. Another portion is oxidized to
,
-diethyl hydracrylic acid, a new, previously undescribed compound. Diethyl malonic acid could not be recovered from the urine of patients receiving the drug.
Several 2-substituted-1,3-propanediols possess anticonvulsant activity of a similar order to that of DEP. None of the compounds is appreciably longer acting.
The diacetate of DEP has a less intense but more prolonged action than the parent compound. Other esters of DEP show no advantages over the parent compound.
Submitted on April 28, 1950