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  • Electronic Resource  (4)
  • Monoamine Synthesis in Rat Brain  (2)
  • Ataxia  (1)
  • Benzodiazepine receptor agonists  (1)
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  • Electronic Resource  (4)
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  • 1
    Electronic Resource
    Electronic Resource
    Effect of pentobarbitone and diethyl ether on the synthesis of monoamines in rat brain (1974)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 284 (1974), S. 263-277 
    Details
    ISSN: 1432-1912
    Keywords: Diethyl Ether Anaesthesia ; Pentobarbitone Anaesthesia ; Monoamine Synthesis in Rat Brain ; Dopa ; 5-Hydroxytryptophan ; NSD 1015 (3-hydroxybenzylhydrazine HCl)
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Rats were injected i.p. with pentobarbitone sodium 40 mg/kg or were exposed to diethyl ether anaesthesia for 15 to 60 min. Monoamine synthesis in vivo was measured in various brain regions by determining the accumulation of dopa and 5-hydroxytryptophan (5-HTP) during 15 or 30 min after the i.p. injection of NSD 1015 (3-hydroxybenzylhydrazine HCl, 100 mg/kg), an inhibitor of the aromatic amino acid decarboxylase. Pentobarbitone retarded the formation of dopa and 5-HTP by about 25% in most brain regions but had no effect on striatal dopa formation. Ether accelerated the formation of dopa and 5-HTP in most brain regions, the action on striatal dopa being most pronounced (to 250% of control). The effect was generally somewhat less marked during the second than during the first half-hour of anaesthesia. A postanaesthetic inhibition of dopa formation was found in the striatum and of 5-HTP formation in whole brain. If hypothermia was allowed to develop, the stimulating action of ether on dopa and 5-HTP formation tended to be partly antagonized. A complex interaction between NSD 1015 and the hypothermic response to ether was observed.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00500346
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    Paper (German National Licenses)
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  • 2
    Electronic Resource
    Electronic Resource
    ZK 91296, a partial agonist at benzodiazepine receptors (1984)
    Springer
    Psychopharmacology 83 (1984), S. 240-248 
    Details
    ISSN: 1432-2072
    Keywords: Benzodiazepine receptors ; β-Carboline-3-carboxylates ; Anxiety ; Epilepsy ; Ataxia ; Rat ; Mouse
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract ZK 91296 (ethyl 5-benzyloxy-4-methoxymethyl-β-carboline-3-carboxylate) is a potent and selective ligand for benzodiazepine (BZ) receptors. Biochemical investigations indicate that ZK 91296 may be a partial agonist at BZ receptors. Such partial agonism may explain to some extent why ZK 91296 needs higher BZ receptor occupancy than diazepam for the same effect against chemical convulsants and for behavioural effects. The lack of sedatiye effects, and the very potent inhibition of reflex epilepsy, spontaneous epilepsy and DMCM-induced seizures suggest, furthermore, that ZK 91296 may possess pharmacological selectivity for a particular type of BZ receptor interaction, perhaps including topographic as well as receptor subtype differentiation.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00464788
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    Paper (German National Licenses)
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  • 3
    Electronic Resource
    Electronic Resource
    Evaluation of the β-carboline ZK 93 426 as a benzodiazepine receptor antagonist (1984)
    Springer
    Psychopharmacology 83 (1984), S. 249-256 
    Details
    ISSN: 1432-2072
    Keywords: ZK 93426 ; Ro 15-1788 ; CGS 8216 ; Benzodiazepine receptor agonists ; Benzodiazepine receptor antagonist ; Benzodiazepine receptor inverse agonist ; Rat ; Mouse
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract We describe here biochemical and pharmacological effects of the β-carboline ZK 93426, a new and potent benzodiazepine (BZ) receptor antagonist. ZK 93426 was compared with Ro 15-1788 and CGS 8216, two compounds previously described as BZ receptor antagonists. Certain effects of ZK 93426, Ro 15-1788 and CGS 8216 were quite similar (e.g., 3H-FNM displacement, “GABA ratio”, “photo-shift”). In most pharmacological tests ZK 93426 and Ro 15-1788 lacked overt effects; Ro 15-1788 was a weak agonist in some paradigms, while ZK 93426 exhibited a potent proconflict effect but also a weak anticonvulsant effect. This interesting finding with ZK 93426 suggests that BZ receptor ligands may possess differential efficacy at BZ receptor subtypes. In contrast, CGS 8216 exhibited potent proconvulsant effects in several paradigms in addition to proconflict and pentylenetetrazol generalizing effects. ZK 93426, Ro 15-1788 and CGS 8216 were almost equally potent as antagonists of the effects of BZ receptor agonists, such as diazepam and lorazepam. However, ZK 93426 was the most potent inhibitor of the convulsions produced by the BZ receptor inverse agonist DMCM.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00464789
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    Paper (German National Licenses)
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  • 4
    Electronic Resource
    Electronic Resource
    Influence of l-3-methoxytyrosine on monoamine synthesis in rat brain (1975)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 290 (1975), S. 347-356 
    Details
    ISSN: 1432-1912
    Keywords: l-3-Methoxytyrosine ; Monoamine Synthesis in Rat Brain ; Dopa ; 5-Hydroxytryptophan ; NSD 1015 (3-Hydroxybenzylhydrazine HCl)
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Rats were injected i.p. with l-3-methoxytyrosine, 100 or 300 mg/kg. One h later brain, liver, heart and blood plama were analyzed for catecholamines and their precursors. In brain Dopa as well as dopamine and noradrenaline levels were unchanged, while demethylation of l-3-methoxytyrosine might have occurred in peripheral organs since Dopa levels in liver and dopamine in heart were elevated. 3-Methoxytyramine could not be detected in brain and liver after treatment with l-3-methoxytyrosine. Monoamine synthesis in vivo was measured in whole brain by determining the accumulation of Dopa and 5-hydroxytryptophan 30 min after the i.p. injection of NSD 1015 (3-hydroxybenzylhydrazine HCl, 100 mg/kg), an inhibitor of the aromatic amino acid decarboxylase. l-3-Methoxytyrosine attenuated the formation of Dopa and 5-hydroxytryptophan by about 25% in brain tissue. The effect was paralleled by a decrease in the brain concentration of tryptophan.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00499948
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    Paper (German National Licenses)
    Fulltext
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