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  • 1
    Electronic Resource
    Electronic Resource
    Are benzodiazepines GABA antagonists? (1977)
    [s.l.] : Nature Publishing Group
    Nature 269 (1977), S. 72-73 
    Details
    ISSN: 1476-4687
    Source: Nature Archives 1869 - 2009
    Topics: Biology , Chemistry and Pharmacology , Medicine , Natural Sciences in General , Physics
    Notes: [Auszug] The experiments were performed on seven adult rabbits anaesthetised with hexobarbitone sodium and artificially ventilated. Microiontophoresis and recording was from five to seven barrelled micropipettes of 4-6 jim overall tip diameter. The central recording barrel was filled with 2M NaCl and only ...
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1038/269072a0
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  • 2
    Electronic Resource
    Electronic Resource
    Effect of substances modifyingγ-aminobutyric acid metabolism on recovery cycles of the interzonal response of the cat motor cortex (1975)
    Springer
    Bulletin of experimental biology and medicine 79 (1975), S. 154-157 
    Details
    ISSN: 1573-8221
    Keywords: γ-aminobutyric acid (GABA) ; interzonal cortical response ; GABA-ergic brain structures ; cholinergic brain structures
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Abstract The effect of thiosemicarbazide (TSC), depakin and bicuculline on recovery cycles of the interzonal response of the motor cortex was investigated in unanesthetized, curarized cats. Substances modifying the metabolism of γ-aminobutyric acid (GABA) selectively influence the facilitation of this response (with intervals of 20–100 msec between stimuli). After injection of TSC, which lowers the GABA content in the brain, and of bicuculline, which specifically blocks GABA-ergic synapses, facilitation is increased, but after injection of depakin, which increases the GABA concentration, and after intraventricular injection of GABA facilitation is reduced. Caffeine and bemegride increase the amplitude of both conditioning and test responses but have no selective action on facilitation of the test response. Benactyzine and arecoline, substances exciting cholingergic structures, likewise had no selective effect on the recovery cycles. It is suggested that the facilitation described above is the result of interaction between systems of recurrent excitation and inhibition. GABA plays an important role in the regulation of this interaction.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00808864
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  • 3
    Electronic Resource
    Electronic Resource
    Antagonism between sodium hydroxybutyrate and some effects of aminohydroxyacetic acid (1975)
    Springer
    Bulletin of experimental biology and medicine 79 (1975), S. 542-544 
    Details
    ISSN: 1573-8221
    Keywords: GABA ; aminohydroxyacetic acid ; sodium hydroxybutyrate ; convulsive states
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Abstract In agreement with data in the literature, a protective effect of aminohydroxyacetic acid (AHAA) was observed as an inhibitor of 4-aminobutyrate:2-oxoglutarate-aminotransferase (GABA-T) in convulsions induced in mice by thiosemicarbazide (TSC), a glutamate decarboxylase inhibitor. A similar but somewhat weaker action was exhibited by sodium hydroxybutyrate (NaHB). Meanwhile, combined administration of NaHB with AHAA reduced the intensity of its anticonvulsant effect with respect to TSC and reduced the accumulation of GABA in the brain characteristic of the action of AHAA. Competition between AHAA, NaHB, and GABA as structurally closely similar compounds for GABA-T or the GABA-ergic receptor is postulated.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00800497
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  • 4
    Electronic Resource
    Electronic Resource
    Antagonistic effect of bicuculline and thiosemicarbazide on the tranquilizing action of diazepam (1977)
    Springer
    Bulletin of experimental biology and medicine 83 (1977), S. 332-334 
    Details
    ISSN: 1573-8221
    Keywords: diazepam ; bicuculline ; γ-aminobutyric acid ; thiosemicarbazide
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Abstract Bicuculline, a specific blocking agent of GABA-ergic receptors, in doses of 0.5 and 1 mg/kg (subcutaneously); and thiosemicarbazide, which inhibits GABA (γ-aminobutyric acid) synthesis in the brain, in doses of 5 and 8 mg/kg (subcutaneously); are antagonists of diazepam and weaken its tranquilizing action during conflict behavior in experimental rats. Bicuculline exhibits stronger antagonism toward diazepam than thiosemicarbazide. The results are evidence that GABA-ergic mechanisms may participate in the tranquilizing action of the benzodiazepines.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00799353
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  • 5
    Electronic Resource
    Electronic Resource
    Cortical inhibition processes and the anticonvulsant action of benzodiazepine derivatives (1977)
    Springer
    Bulletin of experimental biology and medicine 84 (1977), S. 1429-1432 
    Details
    ISSN: 1573-8221
    Keywords: interzonal cortical response ; benzodiazepine derivatives
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Abstract A comparative study of the effect of various benzodiazepine derivatives (clonazepam, lorazepam, diazepam, and medazepam) on the recovery cycle of the interzonal response in the motor cortex of unanesthetized immobilized cats showed that these substances selectively depress the testing potential within the interval of 20–100 msec between conditioning and testing stimuli, evidence of the potentiation of GABA-ergic inhibition in the cortex. Clear correlation was shown between the degree of protective action of the various benzodiazepine derivatives against convulsions due to GABA deficiency and their ability to induce depression of the test response. It is suggested that the GABA-positive action of the benzodiazepines plays a significant role in the mechanism of their anticonvulsant activity.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00801114
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  • 6
    Electronic Resource
    Electronic Resource
    Effect of cesium, lithium, and rubidium on some actions of morphine (1978)
    Springer
    Bulletin of experimental biology and medicine 86 (1978), S. 883-885 
    Details
    ISSN: 1573-8221
    Keywords: lithium ; cesium ; rubidium ; dependence on morphine
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Abstract The effect of cesium, lithium, and rubidium chlorides on the analgesic action of morphine (in the vocalization test) and on the course of dependence on it (by the “two bottle” test) was investigated. The chlorides were shown to reduce both the threshold of the pain response and the duration of analgesia produced by morphine. Cesium chloride was most active in this respect. All the compounds studied reduced the coefficient of morphine preference. The greatest effect was observed with cesium chloride, which reduced the preference coefficient to one-fortieth of the control level.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00801299
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  • 7
    Electronic Resource
    Electronic Resource
    Role of cholinergic mechanisms in the mechanism of action of bicuculline (1978)
    Springer
    Bulletin of experimental biology and medicine 86 (1978), S. 1048-1050 
    Details
    ISSN: 1573-8221
    Keywords: bicuculline ; cholinergic mechanisms ; GABA ; convulsions ; recovery cycle
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Abstract The hypothesis of a possible role of cholinergic structures in the mechanism of the action of bicuculline was tested by screening and electrophysiological methods. Neither muscarinic (M-) nor nicotinic (N-) cholinolytics (benactyzine, atropine, aprophen,* and pediphen†) abolished convulsions produced in mice by bicuculline. Meanwhile substances inducing the accumulation of γ-aminobutyric acid (GABA) in the brain, such as aminohydroxyacetic acid (AHAA) and depakine, had a well marked protective action against bicuculline convulsions. The electrophysiological experiments also showed that the M-cholinolytic benactyzine does not abolish the effects of bicuculline. Bicuculline was shown to reduce the depression of the test response in the recovery cycle of the primary response of the rat sensomotor cortex when intervals between stimuli measured 40–125 msec, whereas benactyzine reduced the late facilitation of the test response when intervals between stimuli measured 150–300 msec. No interaction could be found between benactyzine and bicuculline by this test. It was concluded from these results that the effects of bicuculline are produced by blockade of postsynaptic GABA receptors and are not connected with the activity of cholinergic structures.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00799587
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  • 8
    Electronic Resource
    Electronic Resource
    Mechanism of the anticonvulsant action of diazepam (1975)
    Springer
    Bulletin of experimental biology and medicine 79 (1975), S. 270-273 
    Details
    ISSN: 1573-8221
    Keywords: paroxysmal states ; thiosemicarbazide ; γ-aminobutyric acid (GABA) ; anticonvulsants (diazepam) ; brain mitochondria
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Abstract Diazepam is highly effective in the prevention of convulsions induced by thiosemicarbazide (TSC), i.e., due to γ-aminobutyric acid (GABA) deficiency. Electrophysiological experiments to record the recovery cycle of the interzonal response of the cat motor cortex showed that diazepam reduces the amplitude of the test response, indicating the strengthening of inhibition. This test revealed antagonism of diazepam to bicuculline, specifically blocking GABA-ergic receptors, and to TSC. Diazepam was shown to be capable of increasing the GABA concentration in the brain by inhibiting the activity of GABA transaminase in the mitochondrial fraction of brain tissue.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00804212
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  • 9
    Electronic Resource
    Electronic Resource
    Increased sensitivity of rabbit sensomotor cortical neurons to gaba produced by diazepam (microiontophoretic investigation) (1976)
    Springer
    Bulletin of experimental biology and medicine 82 (1976), S. 1808-1811 
    Details
    ISSN: 1573-8221
    Keywords: diazepam ; γ-aminobutyric acid ; glycine ; glutamate ; acetylcholine ; microiontophoresis ; sensomotor cortex
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Abstract Changes produced by diazepam in the effects of γ-aminobutyric acid (GABA), applied microiontophoretically to neurons of the rabbit sensomotor cortex, were investigated. Diazepam was shown to strengthen the inhibitory action of GABA on spontaneous unit activity and to prolong the effect of GABA on the duration of the inhibitory pause in unit responses to afferent stimulation and to direct cortical stimulation. Diazepam did not change unit responses to microiontophoretically applied glycine, glutamate, or acetylcholine. It is suggested that diazepam increases the sensitivity of the receptors of the postsynaptic membrane of neurons to GABA.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00785702
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  • 10
    Electronic Resource
    Electronic Resource
    The GABA-ergic mechanism of the effect of diazepam on cortical neurons (1976)
    Springer
    Bulletin of experimental biology and medicine 82 (1976), S. 1343-1346 
    Details
    ISSN: 1573-8221
    Keywords: cerebral cortex ; evoked and spontaneous unit activity ; diazepam ; GABA
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Abstract The effect of diazepam, depakine thiosemicarbazide (TSC), and bicuculline on unit activity of the sensomotor cortex arising spontaneously and evoked by sciatic nerve stimulation was studied in unanesthetized, immobilized albino rats. Diazepam was shown to strengthen the inhibitory effects, i.e., to reduce the frequency of spontaneous discharges and to prolong postactivation depression of unit activity (the inhibitory pause). Depakine which increases the brain GABA concentration, had a similar action. Bicuculline, which blocks GABA-ergic receptors, and TSC, which reduces its concentration, had the opposite action and weakened inhibition. A two-way antagonism also was found between diazepam and bicuculline as regards their effect on unit activity. The results confirm the earlier hypothesis that diazepam can potentiate the effect of GABA on cortical neurons.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00799470
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