Effects of antiepileptic drugs on various components (TF: tonic extension of forelimb, TH: tonic extension of hindlimb and CL: clonic convulsions or MCL: myoclonus) of maximal seizures induced by electroshock or pentylenetetrazol in mice were examined in order to classify these drugs. In addition, experiment was conducted similarly on the new anti-convulsant agent, 3-sulfamoylmethyl-1,2-benzisoxazole (AD-810), in order to assess this compound on the basis of the results with clinically useful antiepileptic drugs. From the results obtained in the present study, irrespective of the method, i.e. chemically or electrically induced seizures, anticonvulsant drugs tested can be classified into four main groups; 1) drugs (trimethadione, ethosuximide, nitrazepam, diazepam, erthotoin and metharbital) with an effect to antagonize all the whole seizure components. (TF, TH and CL or MCL) in an almost same antagonism, 2) drugs (phenacemide, dipropylacetate, pheneturide, acetylpheneturide and phenobarbital) which inhibit all forms of seizures at relatively dissociated doses for the prevention of each component of seizures, 3) drugs (diphenylhydantoin and carbamazepine) which selectively abolish both components (TF and TH) of tonic seizures, and 4) drugs (acetazolamide, sulthiame and primidone) exclusively blocking TH of tonic seizures. AD-810 demonstrated an antagonistic effect on tonic seizures but no on clonic ones with the same manner as seen with diphenylhydantoin and carbamazepine.

01 Jan 1963·Japanese Journal of Pharmacology

THE ANTICONVULSANT ACTIVITY OF ETHYL α-PHENYLBUTYROYL ALLOPHANATE (P-5257)

Article

Author: Kiyoshi Tsutsui ; Shinsuke Ose ; Yoshinobu Masuda ; Keiji Nakamura ; Katsuyoshi Nakatsuji ; Katsuro Fujimoto ; Kuniaki O'hashi

The anticonvulsant activity of Et α-phenylbutyrylallophanate (P-5257) and of its derivatives was studied in exptl. animals.P-5257 showed the lowest toxicity in mice and rats among the antiepileptics tested.P-5257 modified the spontaneous behavior of the animals at high doses.Its neurotoxicity was the lowest among phenurone derivatives P-5257 suppressed both elec. and Metrazol shocks in mice and rats, and these effects resembled those of phenurone, pheneturide, crampol, and phenobarbital.Neither development of tolerance nor a withdrawal effect in mice was observed during the daily administration of P-5257 for 3 weeks.The fact that the compound did not potentiate the hypnotic activity of barbiturate in mice was unique and differed from phenurone derivatives and other antiepileptics tested.In unanesthetized cats, the compound produced no effect on the spontaneous electroencephalogram, reticular arousal threshold, and pallidal seizure thresholds.No apparent blocking effect by the compound on either the cholinergic or adrenergic systems was observed in unanesthetized spinal or nembutalized cats.Subchronic toxicological studies on P-5257 indicated no significant effect upon growth rate, blood and urine analysis, and the tissues of rats and mice, while phenurone caused a slight decrease in growth rate, mild leukopenia, proteinuria, mild nephrosis, and slight pyknotic fatty liver with heteromorphous cytoplasm.The relation between anticonvulsant activity and chem. structure of allophanate derivatives is discussed.

01 Apr 1962·No to shinkei = Brain and nerve

[Clinical experiences with Crampol, a new anti-convulsant].

Article

Author: MORISADA, H ; KOSAKA, M ; KOBAYASHI, J ; FUJITA, S

100 Deals associated with Acetylpheneturide

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KEGG	Wiki	ATC	Drug Bank
D01409	-	N03A	-

R&D Status

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Indication	Country/Location	Organization	Date
Autonomic seizure	JP	Sumitomo Pharma Co., Ltd.	06 Apr 1962
Epilepsy, Temporal Lobe	JP	Sumitomo Pharma Co., Ltd.	06 Apr 1962
Epilepsy, Tonic-Clonic	JP	Sumitomo Pharma Co., Ltd.	06 Apr 1962

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