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Biomedical subjects

K Go

Publications and source records attributed to K Go.

At least 55 records · Page 3Linked to original sources
PubMed1978

Anti-convulsant effect of phthalazino-2,3b-phthalazine-5(14H),12(7h)-dione (L-5418). I. Behavioral effect.

Since it had been demonstrated that L5418 has an anti-convulsant effect with no relation to its anti-inflammatory properties, comparative studies were carried out with the use of currently available anti-convulsant agents as controls. L-5418 inhibited tonic convulsions induced by maximal electroshock and strychinine in mice and prevented animals from the death sequence. L-5418 had an inhibitory effect on tonic convulsions induced by pentetrazol and N-sulfamoyl-hexahydroazepine (SaH 41-178), but not on clonic convulsions by those compounds at even a high dosage or on clonic convulsions induced by picrotoxin and bemegride. Trimethadione produced an inhibitory effect on both tonic and clonic convulsions. The hypnotic agents, phenobarbital and glutethimide inhibited both convulsions, but a higher dose was required in the case of clonic convulsions. Anti-convulsant agents are classified into three different groups according to their mode of action. L-5418 had the same mode of action as seen with diphenylhydantoin and carbamazepine. As L-5418 did not inhibit tremor induced by tremorine, an anti-Parkinson effect was ruled out. When L-5418 was administered alone, the animals did not lose the righting reflex nor show muscle relaxation observed in inclined screen and rotarod tests. Moreover, the compound had no influence on the aggressive behavior induced by electrical stimulation or olfactory bulb ablation. L-5418 possesses a selective anti-convulsant effect, yet has no sedative, tranquilizing or disturbing effects on movement such as equilibrium disturbance or muscle relaxation. L-5418 may prove useful for grand mal epilepsy as it is less toxic than diphenylhydantoin and carbamazepine.

Aggression↗
PubMed1978

Anti-convulsant effect of phthalazino-[2,3b]-phthalazine-5(14H), 12(7H)-dione (L-5418). II. Electroencephalographic study.

L-5418 has an anti-convulsant effect which is similar to that of diphenylhydantoin. The effects of L-5418 on EEG activity in rabbits with acute and chronic implantation of electrodes were studied in comparison with those of currently available anti-convulsants. Intravenous administration of L-5418 increased a slow-wave sleep pattern in the spontaneous EEG, which was also induced by diphenylhydantoin. With respect to the focal seizure in the cerebral cortex induced by local application of penicillin, L-5418 showed suppressive effects on the frequency and duration of seizure discharge, and on the spread of seizure discharge to other parts of the brain. The efficacy was about twice that of diphenylhydantoin. L-5418 and dephenylhydantoin did not increase the threshold of seizures induced by bemegride while trimethadione raised the threshold. L-5418 also showed suppressive effects twice as active as diphenylhydantoin on after-discharge induced by electrical stimulation of the hippocampus and amygdala. This suppressive effect on after-discharge of the limbic system may be parallel with the suppressive effect on psychomotor seizure. From these results of L-5418 on an experimental model of epilepsy, it is suggested that L-5418 has suppressive effects similar to that of diphenylhydantoin on convulsion and the efficacy proved to be twice that of diphenylhydantoin in the EEG study.

Animals↗
PubMed1977

[Pharmacological studies of ketoprofen (19583RP) III. Anti-inflammatory, analgesic and antipyretic actions in subcutaneous administration (author's transl)].

It has been already reported that ketoprofen (KP) has a potent anti-inflammatory action comparable to indomethacin, but with oral administration, gastric mucous membrane disturbances occur. In the present work, we administered the Na salt of KP (KP-Na) subcutaneously and found that the anti-inflammatory action was more potent in subacute and chronic inflammations than in the acute one. As an acidic compound, KP-Na had a relatively potent analgesic-antipyretic action and a medical efficacy comparable to the usual non-steroidal anti-inflammatory drugs given orally. The efficacy in case of subcutaneous administration was 2 to 3 times stronger over both acute and chronic inflammations than in case of oral administration. On the other hand, the gastric mucous membrane disturbance was decreased to about 1/3 in case of subcutaneous administration, thus the gastric disturbance could be abated and the medical efficacy can be increased when KP-Na is given subcutaneously. As KP-Na was less irritative at the injection site, the compound could be used clinically for a subcutaneous administration.

Animals↗
PubMed1976

[Acute toxicity and the central effect of 1-(m-chlorophenyl)-3-N,N-dimethylcarbamoyl-5-methoxypyrazole (PZ-177)].

In a previous paper, we reported that PZ-177 had potent anti-inflammatory and analgesic activities. In the present work, acute toxicity and action of PZ-177 on the central nervous system were tested in comparison with PZ-222, one of metabolites of PZ-177, and mepirizole. Acute toxicity of PZ-177 was slightly less than that of aminopyrine and the same as that of mepirizole in mice and rats. PZ-177 produced from sedation to loss of righting reflex with the increase of dose. At a low dose with which the righting reflex was hot lost, PZ-177 decreased spontaneous locomotion of mice in the Animex test, produced muscle relaxation in rotarod and inclined screen tests, produced sleeping-pattern in electroencephalogram of rabbit, potentiated hypnosis of barbiturates and exerted an anti-convulsive effect in mice. In these depressive effects on the central nervous system, PZ-222 was very much lower and mepirizole slightly lower than PZ-177. It would thus appear that PZ-177 has more potent analgesic, antipyretic and anti-tussive actions than do PZ-222 and mepirizole.

Acute Disease↗