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  • 1
    ISSN: 1432-2072
    Keywords: β-Carbolines ; Dimethyltryptamine (DMT) ; Ethnopharmacology ; Harmala alkaloids ; Human platelets ; 5-Hydroxytryptamine ; Psychedelic
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The binding of [3H]citalopram to the platelet 5-hydroxytryptamine (5-HT) transporter was measured in a group of healthy male drinkers ofayahuasca, a psychoactive sacrament indigenous to Amazonia, and a group healthy male controls. An increased number of binding sites (Bmax) in the platelets of ayahuasca drinkers was found, while the dissociation constant (Kd) remained the same for both groups. If indicative of neuronal 5-HT uptake activity, these results would suggest a decreased concentration of extracellular 5-HT, or a response to increased production and release of 5-HT. Such changes in 5-HT synaptic activity, in this case, should not be misinterpreted as an indication of developing neurological or psychiatric illness.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1432-2072
    Keywords: 5-Substituted N,N-Dimethyltryptamines, α-Methyltryptamine, and Gramines ; Monoamine Oxidase Inhibitors ; Psychopharmacology
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Three series of derivatives of N,N-dimethyltryptamine, α-methyltryptamine and gramine bearing substituents of varying electronic nature on the C-5 position were tested for acute toxicity, effect on barbiturate sleeping time, antireserpine effect, swim maze, variable interval conditioned behavior, and inhibition of monoamine oxidase. No correlation could be made between the electronic effects and their pharmacological activities. It was thus suggested that there exist different pharmacological receptors for the tryptamines and gramines.
    Type of Medium: Electronic Resource
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  • 3
    ISSN: 1432-1912
    Keywords: Ro 5-4864 ; PK 11 195 ; Chronic treatment ; Behavior withdrawal ; GABAA and benzodiazepine receptors
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Rats were twice daily (2 × 10 mg/kg, i.p.) treated for three weeks with the peripheral benzodiazepine (BZ) receptor ligands Ro 5-4864 (4′-chlorodiazepam) and PK 11 195 (1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinoline-carboxamide). After the first injection there were no differences between the drug-treated and control animals in behavioral tests. After 10 days treatment, the number of sniffings was increased in Ro 5-4864-treated rats. After the last injection, sniffings and ambulations were decreased in PK 11 195-treated animals. The number of rearings and groomings remained unchanged throughout the treatment, and there were no changes in the results in the elevated plus-maze test. Apparently these compounds are devoid of anxiolytic and anxiogenic effects at moderate doses. The effect of 72 a h withdrawal from the above mentioned chronic treatment on peripheral and central BZ receptors as well as on GABAA receptors was studied with receptor binding techniques using 3H-Ro 5-4864, 3H-flumazenil and 3H-muscimol, respectively, as ligands. The number of GABAA and central BZ receptors was lower after Ro 5-4864 treatment, as was the effect of progesterone-induced stimulation of 3H-muscimol binding. The number of peripheral BZ receptors was decreased after Ro 5-4864 and PK 11 195 treatments in the olfactory bulb but not in the cerebral cortex. The chronic treatment with peripheral BZ receptor ligands ] Ro 5-4864 and PK 11 195 produced only little behavioral effects. Ro 5-4864, often presented as an agonist of peripheral BZ receptors, was behaviorally inactive. PK 11 195, often considered to be an antagonist of Ro 5-4864 developed a small sedative action during chronic treatment. The withdrawal from chronic treatment with these ligands similarly affected peripheral BZ receptors but only Ro 5-4864 affected GABAA/BZ receptor complex in the CNS. The present data support the idea that Ro 5-4864 has independent of peripheral BZ receptors effects on GABA, receptors while PK 11 195 is rather a partial agonist than antagonist of peripheral BZ receptors.
    Type of Medium: Electronic Resource
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  • 4
    Electronic Resource
    Electronic Resource
    Chichester : Wiley-Blackwell
    Biological Mass Spectrometry 7 (1980), S. 549-552 
    ISSN: 1052-9306
    Keywords: Chemistry ; Analytical Chemistry and Spectroscopy
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: A sensitive and specific method is described for the determination of 1,2,3,4-tetrahydro-β-carboline in human plasma, based on selected ion monitoring gas chromatography mass spectrometry and employing a deuterium analogue as internal standard. The identification of 1,2,3,4-tetrahydro-β-carboline is based on monitoring ions m/z 143, 171,199 and 368 for the heptafluorobutyryl derivative of 1,2,3,4-tetrahydro-β-carboline or the normal mass spectrum. For quantitation the ratio of ions m/z 368/370 was used. The mean of 1,2,3,4-tetrahydro-β-carboline level in human plasma (n = 10) was 8.78± 1.94 ng ml-1 and 5.68±1.34 ng in platelets corresponding 1 ml of platelet rich plasma.
    Additional Material: 4 Ill.
    Type of Medium: Electronic Resource
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  • 5
    Electronic Resource
    Electronic Resource
    Chichester : Wiley-Blackwell
    Biological Mass Spectrometry 7 (1980), S. 553-555 
    ISSN: 1052-9306
    Keywords: Chemistry ; Analytical Chemistry and Spectroscopy
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: 1-Methyl-1,2,3,4-tetrahydro-β-carboline (tetrahydroharman) has been quantified in human platelets and plasma following acute intake of ethanol using a selective ion monitoring method. It was not possible to detect this compound before ethanol intake.
    Additional Material: 3 Ill.
    Type of Medium: Electronic Resource
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