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  • 3H-nicotine  (1)
  • Acetylcholine  (1)
  • 1
    ISSN: 1432-1912
    Schlagwort(e): Acetylcholine ; Nicotine ; Cytisine ; d-Tubocurarine
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Summary Nicotine 1.8×10−5–1.8×10−4 mol/l enhanced the spontaneous3H-efflux from guinea-pig cortical slices preloaded with3H-choline and perfused in the presence of hemicholinium (HC-3). The facilitation of tritium outflow was prevented by tetrodotoxin 5×10−7 mol/l and byd-tubocurarine 4.5×10−6 mol/l. Nicotine 1.8×10−6–1.8×10−4 mol/l, and the agonist cytisine 5×10−7–5×10−5 mol/l increased, in a concentration-dependent way,3H-efflux from electrically-stimulated slices (0.2 Hz). The concentration-response curves of both drugs were parallelly shifted to the right byd-tubocurarine 4.5×10−6 mol/l. The EC50 values (i.e. the concentrations required to cause a 50% increase in the S2/S1 ratio) changed for nicotine from 5.58×10−5 to 4.34×10−4 and for cytisine from 6.3×10−6 to 2.75×10−4 mol/l in the absence and in the presence of the antagonist, respectively. In the range of 0.2–2 Hz the magnitude of the effect of nicotine was inversely related to the rate of stimulation. The response to nicotine was subject to rapidly developing tachyphylaxis; it was resistant to atropine. It is concluded that nicotine and cytisine facilitate3H-efflux from the cholinergic nerve endings of guinea-pig cerebral cortex. This effect involves sodium-dependent mechanisms and is due to an interaction of the drugs with receptors showing affinity ford-tubocurarine.
    Materialart: Digitale Medien
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
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  • 2
    ISSN: 1435-1463
    Schlagwort(e): Human thalamus ; nicotinic receptors ; receptor subtypes ; autoradiography ; 3H-ACh ; 3H-nicotine
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract Nicotinic cholinergic receptors in human thalamus were measured using (−)3H-nicotine (20 nM) and3H-acetylcholine (3H-ACh) (20 nM) as radioligands. The specific binding for3H-nicotine to homogenates of thalamus was 51.6±8.3 pmol/g protein and for3H-ACh 18.6±1.9pmol/g protein. Receptor autoradiography indicated a high labelling of both3H-Nicotine and3H-ACh in the antero-ventral nucleus of thalamus and dorso-medial nucleus of thalamus, while the labelling was lower in the postero-lateral nucleus of thalamus and in the postero-lateral ventral nucleus of thalamus. Quantitative measurement of the3H-nicotine autoradiograms showed highest labelling in the anteroventral nucleus of thalamus (17.34±0.76pmol/g tissue). This study indicates a heterogenous distribution of high-affinity nicotinic receptors in the human thalamus.
    Materialart: Digitale Medien
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
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