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  • 1
    Electronic Resource
    Electronic Resource
    Comparative Studies of the Binding of Dimeric and Monomeric Enkephalins to Neuroblastoma-Glioma NG108–15 Cells (1985)
    Oxford, UK : Blackwell Publishing Ltd
    Journal of neurochemistry 45 (1985), S. 0 
    Details
    ISSN: 1471-4159
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: Abstract: Binding activity of the enkephalin dimer [d-Ala2, Leu5-NH-CH2--]2 (DPE2) to NG108–15 hybrid cells was compared to that of the monomer [d-Ala2, Leu5]enkephalin amide (DALEA). At 25°C, the values of the apparent affinity constant for DPE2, measured to intact and lysed cells and membranes, was 5.0 (±0.09) × 109M−1 for n = 28 experiments, as compared to 0.9 (±0.08) × 109M−1 (n = 16) for DALEA. At 4°C, the binding affinity of DPE2 decreased by 43% and that of DALEA by 33%. An important difference between the binding of DPE2 and DALEA was that, after necessary corrections for difference in maximal “bindability” of the respective tritiated enkephalins, the molar binding capacity for DALEA was twofold higher than for DPE2, although mutual cross-displacement studies indicated that binding occurred to one class of noninteracting homogeneous receptors. The binding capacity for intact and lysed cells and membranes was 20 (±2) × 10−-11M for DPE2 and 43 (±2) × 10−-11M for DALEA. The enkephalin monomers [d-Ala2, d-Leu5]enkephalin (DADLE) and [d-Ala2, Met5]enkephalin amide (DAMEA) showed binding characteristics similar to those of DALEA.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1111/j.1471-4159.1985.tb05480.x
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  • 2
    Electronic Resource
    Electronic Resource
    Opioid receptor binding in rat spinal cord (1987)
    Springer
    Neurochemical research 12 (1987), S. 231-235 
    Details
    ISSN: 1573-6903
    Keywords: Spinal opioid binding
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The interaction of various radioligands with spinal opioid receptors has been characterized under variable experimental conditions. Binding to μ, δ, and κ sites was measured in all (cervical, thoracic, lumbar) segments. The apparent affinity constant (K) of [3H]Ethylketocyclazocine (EKC) was similar in Tris, 2.09 (±1.06)×108 M−1, and phosphate buffer, 2.16 (±0.02)×108 M−1, when its interaction with δ and μ sites was blocked. Without blocking ligands, EKC binding was resolved in two components:K 1=1.01 (±0.21)×109 M−1 andK 2=0.95 (±0.61)×107 M−1. Likewise, the binding of [D-Ala2, MePhe4, Gly(ol)5]enkephalin (DAGO) or [D-Ala2, D-Leu5]-enkephalin (DADLE) alone was represented by a 2-site model. By adjusting the radioligand and receptor concentration or by the addition of blocking ligands, binding was represented by a 1-site model for DAGO,K=4.35 (±1.41)×108 M−1, and DADLE,K=2.44 (±0.08)×108 M−1.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00972131
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  • 3
    Electronic Resource
    Electronic Resource
    The effects of long-term treatment of NG108-15 cells with penta- and tetrapeptide enkephalin dimers on opioid receptor binding and cyclic AMP (cAMP) levels (1987)
    Springer
    Cellular and molecular neurobiology 7 (1987), S. 221-228 
    Details
    ISSN: 1573-6830
    Keywords: opioid receptor down regulation ; adenylate cyclase ; dimeric enkephalins ; chronic treatment
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Summary 1. The effects of chronic treatment with a dimeric or monomeric penta- or tetrapeptide enkephalin analogue on binding and cyclic AMP (cAMP) accumulation in NG108-15 cells have been studied. 2. When the cells were cultured in the presence of 1µmol of a pentapeptide analogue (dimer or monomer) for up to 96 hr, binding was reduced by ⩾90%. 3. In contrast, in the presence of 1µmol of a tetrapeptide analogue (dimer or monomer), binding was reduced by only ⩽30%. 4. The analogues had varying effects on regulation of cAMP formation. Desensitization, indicated by impaired opioid-mediated inhibition of prostaglandin E1 (PGE1)-stimulated cAMP accumulation, was clearly apparent only for cells pretreated with [d-Ala2,d-Leu5]enkephalin (DADLE), while cells pretreated with [d-Ala2,Leu5-NH-CH2-]2 (DPE2) showed minor impairment. 5. Thus, ligand dimerization appeared to have a modulating effect on regulation of adenylate cyclase activity but not to affect opioid-induced down-regulation.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00711556
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  • 4
    Electronic Resource
    Electronic Resource
    Interaction of very low density lipoprotein with chicken oocyte membranes (1985)
    New York, N.Y. : Wiley-Blackwell
    Journal of Cellular Biochemistry 28 (1985), S. 281-288 
    Details
    ISSN: 0730-2312
    Keywords: very low density lipoprotein ; hen ; oocyte membranes ; Life and Medical Sciences ; Cell & Developmental Biology
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Biology , Chemistry and Pharmacology , Medicine
    Notes: The interaction of hen 125I-VLDL (very low density lipoprotein) with chicken oocyte membranes was characterized using a rapid sedimentation assay. Equilibrium and kinetic studies showed an apparent dissociation constant (Kd) 8.7-9.1 × 10-8 M or 43.5-45.5 μg VLDL protein/ml. Binding capacity was 2.0 μg VLDL protein/mg membrane homogenate protein. The apparent rate constants were, k1 = 2.4 × l05 M-1min-1 and k2 = 2.1 × 10-2 min-1. Specific binding required the presence of divalent cations. Whereas binding was completely re-stored after treatment with EDTA by the addition of Mn++, only 60% of binding was restored using Ca++.
    Additional Material: 3 Ill.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/jcb.240280406
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