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  • 1
    Electronic Resource
    Electronic Resource
    Human placental transfer of AH 8165 (1975)
    Oxford, UK : Blackwell Publishing Ltd
    Anaesthesia 30 (1975), S. 0 
    Details
    ISSN: 1365-2044
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1111/j.1365-2044.1975.tb00790.x
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  • 2
    Electronic Resource
    Electronic Resource
    5-HT3 Receptors (1990)
    Oxford, UK : Blackwell Publishing Ltd
    Annals of the New York Academy of Sciences 600 (1990), S. 0 
    Details
    ISSN: 1749-6632
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Natural Sciences in General
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1111/j.1749-6632.1990.tb16882.x
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    Paper (German National Licenses)
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  • 3
    Electronic Resource
    Electronic Resource
    Short-lasting, Competitive Neuromuscular Blocking Activity in a Series of Azobis-Arylimidazo-[1,2-a]-Pyridinium Dihalides (1972)
    [s.l.] : Nature Publishing Group
    Nature 238 (1972), S. 354-355 
    Details
    ISSN: 1476-4687
    Source: Nature Archives 1869 - 2009
    Topics: Biology , Chemistry and Pharmacology , Medicine , Natural Sciences in General , Physics
    Notes: [Auszug] Table 1 Paralysing Activities of some Azobis-Arylimidazo-[1,2-a]-Pyridinium Analogues, (+)-Tubocurarine, Succinylcholine, Gallamine and Pancuronium following Intravenous Injection in the Conscious Mouse x- R2 Paralysing activity Acute toxicity AH No. RI R2 ED 50 (95% fid. LD 50 ...
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1038/238354a0
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  • 4
    Electronic Resource
    Electronic Resource
    Identification and distribution of 5-HT 3 receptors in rat brain using radioligand binding (1987)
    [s.l.] : Nature Publishing Group
    Nature 330 (1987), S. 746-748 
    Details
    ISSN: 1476-4687
    Source: Nature Archives 1869 - 2009
    Topics: Biology , Chemistry and Pharmacology , Medicine , Natural Sciences in General , Physics
    Notes: [Auszug] Non-radiolabelled GR65630 (3-(5-methyl-lH-imidazol-4-yl)-1-(1 -methyl-lH-indol-3-yl)-l-propanone) (Fig. la) is approximately 10 times more potent than GR38032 against 5-HT-induced depolarization of the rat isolated vagus nerve2 (pA2 9.9; Schild slope = 1.11, n = 27) and 2-methyl-5-HT-indueed ...
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1038/330746a0
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  • 5
    Electronic Resource
    Electronic Resource
    5-HT 3 receptors mediate inhibition of acetylcholine release in cortical tissue (1989)
    [s.l.] : Nature Publishing Group
    Nature 338 (1989), S. 762-763 
    Details
    ISSN: 1476-4687
    Source: Nature Archives 1869 - 2009
    Topics: Biology , Chemistry and Pharmacology , Medicine , Natural Sciences in General , Physics
    Notes: [Auszug] Release of [3H]acetylcholine from rat entorhinal cortex pre-loaded with [3H] choline was stimulated by potassium. Previous studies have shown that the tritium released is [3H]acetylcholine, and that the release is calcium-dependent13. 5-HT (2 p,M) or the selective 5-HT3 receptor agonist, ...
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1038/338762a0
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  • 6
    Electronic Resource
    Electronic Resource
    [3H] GR67330, a very high affinity ligand for 5-HT3 receptors (1990)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 342 (1990), S. 22-30 
    Details
    ISSN: 1432-1912
    Keywords: 5-HT3 receptors ; Rat brain ; [3H] GR67330 ; 5-HT3 Antagonists ; Rat isolated vagus nerve
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary GR67330 potently inhibited 5-hydroxytryptamine (5-HT)-induced depolarizations of the rat isolated vagus nerve. At the higher concentrations used (0.3 nmol/l–1 nmol/l) this was accompanied by a marked reduction in the maximum response to 5-HT. The calculated pKB value was 10.2. The binding of the tritiated derivative of GR67330 to homogenates of rat entorhinal cortex was examined. Kinetic analysis revealed that specific [3H] GR67330 (0.1 nmol/l) binding was rapid and reversible. Association and dissociation rate constants were 1.48 ± 0.36 × 108 mol/l−1 s−1 and 7.85 ± 0.41 × 10−3 s−1 respectively. Equilibrium saturation analysis revealed specific binding was to a single site (Bmax 22.6±0.21 fmol/mg protein) of high affinity (Kd 0.038±0.003 nmol/l). At low ligand concentrations, specific binding was up to 90% of total binding. If unlabelled GR67330 was used to define non-specific binding two sites were evident (Kd1 0.066 ± 0.007 nmol/l, Kd2 20.1 ± 9.7 nmol/l; Bmax2 31.5 ± 3.2 fmol/mg protein, Bmax2 1110 ± 420 fmol/mg protein). [3H] GR67330 binding was inhibited potently by 5-HT3 antagonists and agonists. Ligands for other 5-HT receptors and other neurotransmitter receptors were either only weakly active or inactive at inhibiting binding. Hill numbers for antagonist inhibition of binding were close to unity, except for quipazine which was significantly greater than one. In common with other 5-HT3 binding studies, all 5-HT3 agonist tested had Hill numbers greater than one (1.51–1.71). GR38032 and GR65630 inhibited a greater proportion of binding than other 5-HT3 antagonists, this additional binding was interpreted as inhibition from a second saturable site unrelated to the 5-HT3 receptor. Homogenates of five areas of rat brain were examined for specific [3H]-GR67330 binding (entorhinal cortex, cingulate cortex, parietal cortex, hippocampus and nucleus accumbens/olfactory tubercle). In each brain area a site of very high affinity was labelled. Drug inhibition profiles were also very similar in each brain area. It is concluded that, because of its high affinity, [3H] GR67330 will be a useful ligand to label 5-HT3 receptors especially in tissues with low receptor densities and to map 5-HT3 receptors autoradiographically.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00178967
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  • 7
    Electronic Resource
    Electronic Resource
    Interactions between 5-HT3 receptors and cerebral dopamine function: implications for the treatment of schizophrenia and psychoactive substance abuse (1993)
    Springer
    Psychopharmacology 112 (1993), S. S68 
    Details
    ISSN: 1432-2072
    Keywords: 5-HT3 ; Receptor ; Dopamine ; Mesolimbic
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract This article reviews current knowledge on the interaction between 5-hydroxytryptamine (5-HT), acting at 5-HT3 receptors in the CNS, and cerebral dopamine systems. Since 1987, a growing body of behavioural, neurochemical and electrophysiological evidence from animal studies has demonstrated a clear role for 5-HT3 receptors in the modulation of activity of mesolimbic and mesocortical dopamine neurones. This evidence has led to the suggestion that 5-HT3 receptor antagonists have potential as novel antipsychotic agents and may also find use in the treatment of psychoactive substance abuse. Data emerging from clinical studies generally support this hypothesis and suggest that 5-HT3 antagonists may prove to be among the first agents available to treat schizophrenia which are not dopamine D2 antagonists and hence lack their side-effect problems.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF02245009
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