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PubMed2000

[The roles of estrogen and progestin in epileptogenesis and their mechanisms of action].

Clinical data showed that periodic alterations of estrogen and progestin in some women patients with catamenial epilepsy might affect seizure susceptibility. In the present study, in order to explore the roles of estrogen and progestin in epilepsy and elucidate their mechanisms of action, we utilized animal seizure models induced by intracerebroventricular(i.c.v) coriaria lactone(CL) and intraperitoneal(i.p.) bemegride(Be), studied the effects of estrogen and progestin on central nervous system(CNS) functions in behavior, electrophysiological, cellular, molecular and gene levels by means of neuroelectrophysiology, flow cytometry, high performance liquid chromatography, immunocytochemical and in situ hybridization techniques. From our observation we concluded that ovarian hormones are neuroactive steroids and new neuromodulaters, they could affect the excitability of CNS by regulating immediate early genes, amino acid neurotransmitters and N-methyl-D-aspartate receptor(NMDAR).

Animals↗
PubMed1979

[Two forms of Ca2+-dependent ATPase from sarcoplasmic reticulum].

Two highly purified sarcoplasmic reticulum membrane fractiones differing in their sensitivities to the uncoupling action of caffeine were isolated from white skeletal muscles of the rabbit. The main protein component of both fractions is a catalytical polypeptide of Ca2+-dependent ATPase. Treatment of the caffeine-sensitive reticular fraction by trypsin or DTNB completely removes the effect of caffeine. It was found that similar effects on the caffeine-sensitive reticular fraction are exerted by bemegride, camphor, ethymizole and cordiamine. Isolation of Ca2+-dependent ATPase from both reticular fractions and reconstruction of Ca2+-transporting vesicles were carried out. Ca2+ transport by the vesicles enriched by ATPase from the caffeine-sensitive reticular fraction is uncoupled under the effect of caffeine; however, caffeine has no effect on the vesicles enriched by caffeine-insensitive reticular ATPase. The molecular weight of caffeine-sensitive and caffeine-insensitive ATPases determined in the presence of sedium dodecyl sulfate are found to be identical. Electrophoresis in the presence of digitonin revealed different electrophoretic behaviour of the two forms of ATPase.

Animals↗
PubMedDate not supplied

[Digoxin--an active antiepileptic agent].

A new pathogenetically grounded approach to the treatment of resistant forms of epilepsy is proposed. Digoxin suppresses the activity of experimental epileptogenic foci produced in the hippocampus of animals (frogs and rats) and also convulsions induced by corazol, bemegrid or electroshock. The antiepileptic and anticonvulsant activity of the drug was confirmed during its clinical testing on 20 children with grave forms of epilepsy which were resistant to the known antiepileptic drugs. The positive therapeutic effect was obtained in 42% of the cases.

Anticonvulsants↗
PubMed1987

The guinea-pig isolated atrium as a model system for the central actions of selected CNS stimulant and depressant drugs. Part 1: 3,3-Diakylglutarimide homologues and related drugs.

The 3H-noradrenaline pretreated, spontaneously beating, guinea-pig atrial preparation has been used as a model system to study the presynaptic and postsynaptic actions of selected drugs with stimulant (bemegride, pentylenetetrazol, picrotoxin, strychnine and 4-methyl-4-n-propylpiperidine hydrochloride), depressant (pentobarbitone, hydroxydione, trimethadione, 3-methyl-3-n-alkylglutarimide where alkyl = butyl, amyl or hexyl, 4-methyl-4-n-propylpiperidone-2 hydrochloride, chlordiazepoxide and chlorpromazine) or dual stimulant-depressant (3-methyl-3-n-propylglutarimide and 5-ethyl-5-(1,3-dimethylbutyl) barbiturate and its (+) and (-) enantiomers) actions in the central nervous system of the mouse. 3H-Noradrenaline efflux and force and rate of atrial contraction were used as parameters of atrial function. With the exception of strychnine, picrotoxin and 4-methyl-4-n-propylpiperidine hydrochloride, which appear to act by different central mechanisms, there is good correspondence between the actions of the test drugs on the force of atrial contraction and in the CNS of the mouse. Thus, stimulant drugs increase and depressant drugs decrease the force of atrial contraction, while dual stimulant-depressant drugs in low concentrations increase, and in higher concentrations, decrease the inotropic response. A similarly good correspondence generally exists between mouse and atrium with respect to the relative stimulant and depressant potencies of the test drugs, additive stimulation or depression for pairs of like-acting drugs and 'analepsis' and 'anticonvulsant activity' for drugs with opposed central actions. No such relationships were found using tritium efflux or the chronotropic response as parameters of atrial function. Thus, the guinea-pig atrial preparation appears to be a good model system in which to demonstrate the acute CNS actions and interactions of the majority of the test drugs. Their positive and negative inotropic effects on the atrium have been explained in terms of a membrane phase distribution hypothesis of drug action, and their ability to facilitate or impede, respectively, the movement of Ca2/ across the atrial sarcolemmal membrane. It is proposed that these drugs may act by similar mechanisms at responsive sites in the brainstem reticular formation and related areas in the mouse. These may be primarily excitatory noradrenergic synapses integrated functionally with presynaptic or independent inhibitory GABAergic terminals.

Animals↗
PubMedDate not supplied

[Comparative characteristics of septal "burst" neurons after elimination of afferent effects of the reticular formation in the rabbit].

Comparative analysis of characteristics of rhythmic theta-activity in the neurones of the medial septal nucleus and nucleus of diagonal band was performed in intact rabbits after. i. v. injection of pentobarbital, and in rabbits with chronic lesion of the ascending brain-stem afferent fibers. In both conditions theta-bursts disappeared in some cells with unstable periodic rhythmic modulation; substantial population of the septal units preserved regular burst activity. Main characteristics of theta-bursts were almost identical in both states, their mean frequency decreased to 3.5 Hz. The theta-rhythm in hippocampal EEG was usually absent; but low-frequency rhythmic activity could be evoked by electrical or sensory stimulation as well as by injection of bemegrid or physostigmine. The data show that the ascending brain-stem afferents control: the frequency of the bursts in a population of septal units regarded as bursting pace-maker cells; the total number of the septal cells secondarily (synaptically) involved into rhythmic activity. The effect of pentobarbital upon theta-rhythm results from elimination of these influences upon the septal cells.

Animals↗
PubMed1979

Quantitative evaluation of the actions of anticonvulsants against different chemical convulsants.

Anticonvulsants were tested on mice for their effectiveness against different chemical convulsants. Ethosuximide is very effective against pentylenetetrazol (PTZ), but ineffective against 3-mercaptopropionate (3-MP) which is an inhibitor of gamma-aminobutyrate (GABA) synthesis. Trimethadione, chlordiazepoxide and mesuximide are less effective against 3-MP than against PTZ. The same tendency was apparent, though falling short of statistical significance, with phenobarbital, mephenytoin, carbamazepine and valproic acid, whereas aminooxyacetic acid (AOAA) appeared to be somewhat more effective against 3-MP than against PTZ. Several anticonvulsants were tested also against bicuculline (BIC), picrotoxin (PIC) and bemegride (BEM), and profiles depicting their relative capacities to antagonize the convulsants were constructed. These show major differences and few resemblances. Likewise the convulsants show little resemblance to each other in their patterns of sensitivity to different anticonvulsants. The data do not support the concept that PTZ, BEM, BIC or PIC induce seizures primarily by blockading GABA-mediated inhibition, since their patterns are so unlike that of 3-MP. The profiles of clinically used anticonvulsants suggest that none of those tested acts primarily on the GABA system, since all are so unlike that of AOAA.

Animals↗
PubMed1984

[Intravenous monoanesthesia and antianesthetics in emergency surgery].

Profiles of using the intravenous mononarcosis (sodium hydroxybutyrate, viadryl , ketamin , sombrevin, seduxen) in urgent surgery and traumatology are analyzed. Choice of certain narcotics is motivated for patients with blood loss and shock, intoxication, insufficiency of kidneys, adrenals and liver, cardio-vascular and respiratory disorders. The problem of antinarcotics is considered with reference to the efficiency of specific (bemegride, gutimine , amtizol , cytochrome "C") and nonspecific ( osmodiuretics , infusion media containing thawing water) antinarcotics . A preliminary assessment of the efficiency of different drugs of antinarcotic action is given.

Adult↗
PubMed1983

[Effects of pentylenetetrazol on conflict behavior and interactions with anxiolytics in rats].

Effects of pentylenetetrazol (PTZ) on conflict behavior were studied using a punished water-lick (conflict) paradigm in rats. PTZ (5-20 mg/kg, ip) produced a dose-related enhancement of conflict behavior as demonstrated by a suppression of lick responding in low shock intensity (1.3-2.0 mA). Furthermore, PTZ (2-20 mg/kg, ip) clearly antagonized the release of punished responding induced by diazepam (5 mg/kg, ip), chlordiazepoxide (10 mg/kg i.p.) or meprobamate (75 mg/kg, ip) when a high intensity of shock (2.5 or 3 mA) was used. Bemegride also showed a similar suppressive effect on the anticonflict action of diazepam. However, bicuculline, picrotoxin or strychnine neither enhanced conflict behavior nor inhibited the anticonflict action of diazepam, even in high doses. In addition, PTZ (10 or 20 mg/kg, ip) did not show any significant effect on unpunished drinking or flinch-jump threshold, suggesting that the conflict enhancing action of PTZ may not be due to the secondary action including decrease in drive for drinking or increase in sensitivity to shock. These results suggest that PTZ may exert facilitation of conflict behavior or suppression of the anticonflict action of anxiolytics via an activation of the conflict generating mechanisms.

Animals↗
PubMed1982

Multiple drug training as a method for increasing the specificity of the drug discrimination procedure.

In a two-lever appetitively reinforced bar-pressing task, one group of rats learned a phenobarbital vs. saline discrimination. Groups 2 to 4 were reinforced for pressing one lever when given phenobarbital and for pressing the other level when given saline or any one of three drugs. In Group 2, the other drugs were the stimulants amphetamine, cocaine and bemegride. In Group 3, the other drugs lacked either strong stimulant or depressant effects (fentanyl, nicotine and cyclazocine). In Group 4, the other drugs were the depressants ethanol, chlordiazepoxide and ketamine. All rats learned the required multiple drug (phenobarbital vs. other) discrimination after one to four training sessions per drug. After discrimination training was completed, tests for substitution with various depressant drugs showed that the degree to which these drugs substituted for phenobarbital differed greatly across groups. Substitution was most complete in rats trained with phenobarbital vs. saline and least complete when the other training drugs were depressants. The results indicate that the degree of specificity produced by phenobarbital vs. other drug discrimination training can be systematically altered by varying the drugs included in the other category.

Animals↗
PubMed1982

Interactions of phenytoin with ouabain and other chemical convulsants.

Phenytoin potentiated the convulsive actions of bicuculline and picrotoxin in mice, whereas the action of bemegride was neither potentiated nor antagonized. Seizures induced by intracerebral injection of ouabain were antagonized by phenytoin, as well as by phenobarbital, chlordiazepoxide and valproic acid; trimethadione had a possible small effect, not quite significant at the 5% level; ethosuximide and muscimol did not show significant effects. Seizures induced by intracerebral injection of pentylenetetrazol were antagonized by phenobarbital but not by phenytoin. Tests of phenytoin against other chemical convulsants are reviewed, and it is suggested that phenytoin may be specific for seizures that arise from a derangement of mechanisms involving sodium ions. This strengthens the view that such a derangement is likely in many cases of human epilepsy.

Animals↗
PubMed1980

[Behavioral pharmacology of mianserin hydrochloride, a new antidepressant (author's transl)].

Behavioral pharmacological properties of mianserin (1,2,3,4,10,14b-hexahydro-2-methyldibenzol[c,f]pyrazino [1.2-a]azepine monohydrochloride) were investigated in comparison with imipramine (IMP) and amitriptyline (ATP). Mianserin antagonized reserpine-induced hypothermia but to a much lesser extent than IMP or ATP, and did not block the ptosis evoked by reserpine or tetrabenazine. Amphetamine-induced stereotyped behavior was significantly enhanced by both IMP and ATP, but not by mianserin. Unlike IMP or ATP, haloperidol-induced catalepsy in the rat was not blocked by mianserin. Like IMP or ATP, mianserin did not suppress the convulsions induced by bemegride or strychnine in the mouse, and or emetic action of apomorphine in the dog, while only mianserin did not block the convulsions evoked by electric shocks. Mianserin more strongly potentiated the anesthetic action of thiopental than did IMP. ATP showed strong muscle relaxant action and the impairment of coordinated motor activities both in mice and rats, in the inclinated screen test and rotarod test, while, like IMP, these actions of mianserin were significant only in the rat. Catalepsy was not induced nor was the righting reflex suppressed by mianserin. In the low spinal cat, mianserin did not depress the amplitude of extensor MSR. Moreover, the MSR inhibition induced by conditioning stimulation of ipsilateral cutaneous afferents and the MSR potentiation evoked by conditioning stimulation of contralateral saphenous nerve were unaffected by mianserin. The curious behavior of mice and rats was significantly and dose-dependently suppressed by mianserin, and tended to be suppressed by ATP, while an enhancement was seen with IMP in large doses. Mianserin was the most potent in suppressing the fighting behavior induced by long-term isolation of the mouse, and was the weakest in suppressing electric-stimulation-induced fighting behavior, compared with IMP and ATP. Mianserin showed no significant suppression of the muricide behavior of the olfactory bulbectomized rat, while IMP significantly suppressed it. No significant differences were observed among mianserin, IMP and ATP as to their actions on the conflict behavior and the shuttle-box type conditioned avoidance behavior of the rat. These results indicate that behavioral pharmacological actions of mianserin were not always the same as those of IMP and ATP. Therefore, mianserin may be a new antidepressant with mechanisms of action which differ from that of the usual tricyclic antidepressants.

Agonistic Behavior↗
PubMed1980

[Psycopharmacological and general pharmacological studies of 7-chloro-1-cyclopropylmethyl-1, 3-dihydro-5-(2-fluorophenyl)-2H-1, 4-benzodiazepin-2-one (KB-509) (author's transl)].

KB-509, a new derivative of benzodiazepines, increased locomotor activities of mice in doses of 8-32 mg/kg (p.o.) and a decrease occurred with higher doses. This drug was 3-6 and 1-2 times more potent than diazepam (DZP) and nitrazepam (NZP), respectively, in anticonvulsant (anti-pentylenetetrazol, bemegride, strychnine) activities, antiaggressive activity and potentiation of chlorprothixene-induced hypnosis in mice. On the other hand, KB-509 possessed similar potency to DZP and NZP in muscle relaxant activity in mice and inhibition of flexor in cats, and was markedly weaker than DZP and NZP in causing a loss of righting reflex in mice. In the spontaneous EEG activity, KB-509 induced a drowsy pattern and slightly inhibited arousal response to EEG in rabbits, as did DZP. In particular, KB-509 was more potent than DZP in suppressing the amygdala afterdischarge and had a longer duration of action. KB-509 and DZP slightly depressed body temperature, the cardio-respiratory system and the gastrointestinal tract in high doses. Potentiation of spontaneous motility of the uterus and increase of urine excretion were also observed with high doses. In conclusion, KB-509 is superior to both DZP and NZP in the ratio of anticonvulsant and/or taming activities and muscle relaxant activity, and has a weak central depressant activity.

Animals↗