2-Dialkylaminoalkyl-(dialkylamido)-fluorophosphates: acute toxicities.

Toxicities expressed as LD50 values of 2-dialkylaminoalkyl-(dialkylamid) o-fluorophophates for rats and mice (i. m. administration) were determined. Rats were more sensitive to these compounds than mice: LD50 values varied from 17 to 261 micrograms/kg for rats and from 30.5 to 1222 micrograms/kg for mice, respectively. Different routes of administration in one derivative of this group substituted by methyl groups only were compared. The highest toxicity (lowest LD50 value) in intravenous administration (11 micrograms/kg) and the lowest one in percutaneous (1366 micrograms/kg) were found.

Acute toxicities of 2-dialkylaminoalkyl-(dialkylamido)-fluoro-phosphates.

Toxicities expressed as LD50 values of 2-dialkylaminoalkyl-(dialkylamido)-fluorophosphates for rats and mice (i.m. administration) were determined. Rats were more sensitive to these compounds than mice: LD50 values varied from 17 (rats) to 1222 (mice) micrograms/kg. LD50 values at different routes of administration (i.v., i.m., s.c., p.o. and p.c.) for one derivative of this group, 2-dimethylaminoethyl-(dimethylamido)-fluorophosphate, were determined. Depending on the route of administration, LD50 values varied from 11 (i.v.) to 190 (p.o.) micrograms/kg for rats and from 27.6 (i.v.) to 222 (p.o.) micrograms/kg for mice, respectively. Percutaneous toxicity in rats only (LD50 = 1366 micrograms/kg) was determined.

[Initial experience with the administration of 7-methoxyacrine to patients with psychological disorders]. / První zkusenosti s podáním 7-metoxytakrinu psychicky nemocným.

The cholinomimemtic substance 7-methoxyacrine was administered to eight patients, incl. 5 patients with tardive dyskinesias after neuroleptic drugs. In all patients an europhorizing effect was recorded, all five patients with tardive dyskinesias improved markedly after a single dose, in one female patient after repeated administration symptoms of tardive dyskinesia were eliminated. The incidence of side effects is minimal. Based on our modest experience we consider 7-methoxyacrine an important extension of therapeutic possibilities, in particular in tardive dyskinesias. The authors plan to test 7-methoxyacrine also in other indications, in particular in Alzheimer's disease and in side-effects caused by psychopharmaceutical preparations.

Continual monitoring of the reactivation effect of oximes on blood acetylcholinesterase in the rats poisoned with organophosphates.

Acetylcholinesterase activity in rat blood was continuously monitored following O-ethyl-S-(2-dimethylaminoethyl)-methylphosphonothioate intoxication (p.o.) alone and in combination with atropine and the reactivators trimedoxime, obidoxime and methoxime. Decrease of acetylcholinesterase activity was not influenced by atropine alone but following treatment with a combination of atropine with the reactivators mentioned, an increase (reactivation) of the blood enzyme was demonstrated. This increase was highest for the combination atropine-trimedoxime and the lowest for the combination atropine-obidoxime.