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1Author    Mario Suwalsky3, Carlos Schneider3, Fernando Villenab, Beryl Norrisb, HernanC. Árdenasb, Francisco Cuevasc, CarlosP. SotomayorcRequires cookie*
 Title    Dibucaine-Induced Modification of Sodium Transport in Toad Skin and of Model Membrane Structures  
 Abstract    The interaction of the local anesthetic dibucaine with the isolated toad skin and membrane models is described. The latter consisted of human erythrocytes, isolated unsealed human erythrocyte membranes (IUM), large unilamellar vesicles (LUV) of dimyristoylphosphati-dylcholine (DMPC) and phospholipid multilayers built-up of DMPC and dimyristoylphos-phatidylethanolamine (D M PE), representative of phospholipid classes located in the outer and inner monolayers of the human erythrocyte membrane, respectively. Results indicate a significant decrease in the potential difference (PD) and in the short-circuit current (Isc) after the application of dibucaine in toad skin, which may be interpreted as reflecting inhibition of the active transport of ions. This finding might be explained on the basis of the results ob­ tained from fluorescence spectroscopy and X-ray diffraction studies on membrane models. In fact, dibucaine induced structural perturbations in IUM, DMPC LUV and phospholipid multilayers. Scanning electron microscopy revealed that dibucaine induced erythrocyte sto-matocytosis. According to the bilayer couple hypothesis an echinocytic type of shape change would have been expected given the preferential interaction of dibucaine with DMPC. Al­ though it is still premature to define the molecular mechanism of action of dibucaine, the experimental results confirm the important role played by the phospholipid bilayers in the association of the anesthetic with cell membranes. 
  Reference    Z. Naturforsch. 56c, 614 (2001); received January 29/March 8 2001 
  Published    2001 
  Keywords    Local Anesthetic, Dibucaine, Membrane 
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 TEI-XML for    default:Reihe_C/56/ZNC-2001-56c-0614.pdf 
 Identifier    ZNC-2001-56c-0614 
 Volume    56 
2Author    Ping-Lu LiRequires cookie*
 Title    Cytotoxicity of Cobra (Naja naja kaouthia) Venom on Rabbit Red Blood Cells and S-180 Tumor Cells in the Presence of Tetracaine, Lidocaine and Procaine  
 Abstract    The cytocidal action of Naja naja kaouthia venom on rabbit red blood cells and S-180 tumor cells treated with local anesthetics (tetracaine, lidocaine and procaine) were studied. The S-180 cells were more sensitive to the venom than the red blood cells which required albumin for ef­ ficient hemolysis in the 10 minute assay. All three local anesthetics at lower concentrations protected both cell types against venom hemolysis. At higher concentrations the local anesthetics enhanced the cell lysis to 100%. The effectiveness of the local anesthetics for both the inhibition and enhancement phases of cytotoxicity was tetracaine > lidocaine > procaine. This is the same order as their anesthetic effectiveness, lipid solubility and their protein binding. 
  Reference    Z. Naturforsch. 35c, 268 (1980); received October 8 1979 
  Published    1980 
  Keywords    Local Anesthetics, Cobra Venom, Cytotoxicity, Erythrocytes, Tumor Cells 
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 TEI-XML for    default:Reihe_C/35/ZNC-1980-35c-0268.pdf 
 Identifier    ZNC-1980-35c-0268 
 Volume    35 
3Author    V. Kettmann, J. SivýRequires cookie*
 Title    A Receptor Interaction Model for Phenylcarbamate Local Anesthetics  
 Abstract    We report here a molecular modeling study of selected conformationally constrained phenylcarbamate local anesthetics in relation to the available pharmacological data that enabled us to develop a receptor-interaction model for this class of drugs. The validity of the model was confirmed on other semirigid analogues prepared for this study. The results suggest that the phenyl ring is most likely involved in a stacking interaction with a complementary receptor site and the tertiary ammonium group is capable of both hydrogen bonding and lipophilic interactions. 
  Reference    Z. Naturforsch. 50c, 708—714 (1995); received May 22/June 17 1995 
  Published    1995 
  Keywords    Local Anesthetics, Phenylcarbamates, Molecular Modeling, Receptor Model 
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 TEI-XML for    default:Reihe_C/50/ZNC-1995-50c-0708.pdf 
 Identifier    ZNC-1995-50c-0708 
 Volume    50 
4Author    GabrieleG. Ünther, Henrik LaaschRequires cookie*
 Title    Local Anesthetic Binding to Thylakoid Membranes. Relation to Inhibition of Light-Induced Membrane Energization and Photophosphorylation  
 Abstract    The association o f the lipophilic tertiary amine and local anesthetic dibucaine with osm oti-cally shocked chloroplasts o f Spinacia oleracea L. cv. M onatol was investigated. Dibucaine, known as an effective inhibitor o f thylakoid membrane energization and A TP synthesis, ex­ hibited three distinct binding classes with chloroplasts: partitioning in the lipid phase o f the membranes, electrostatic screening o f negative electrical charges on the thylakoid surface and light-induced association o f an as yet unknown nature. Evidence is presented that the mecha­ nism o f inhibition o f the transthylakoid pH gradient, ApH, by dibucaine is distinct from 'clas­ sical' amine-type uncoupling: The inhibitory effect o f dibucaine on ApH was independent o f the initial strength o f ApH. Light-induced dibucaine binding was independent o f the volum e o f the intrathylakoid space and o f the strength o f ApH as varied by medium pH. Judged from a comparison o f the data on dibucaine binding and on inhibition o f ApH and photophosphory­ lation, dibucaine bound via partitioning in the membrane lipid phase is responsible for the un-coupler-like effects o f the local anesthetic. A mechanism for the inhibition o f thylakoid energi­ zation by local anesthetic amines is discussed. 
  Reference    Z. Naturforsch. 46c, 79—8 (1991); received September 21 1990 
  Published    1991 
  Keywords    Chloroplast, Local Anesthetic, Dibucaine, Uncoupling, Photophosphorylation, Amine Bind­ ing 
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 TEI-XML for    default:Reihe_C/46/ZNC-1991-46c-0079.pdf 
 Identifier    ZNC-1991-46c-0079 
 Volume    46 
5Author    Henrik LaaschRequires cookie*
 Title    Maintenance of Photophosphorylation Despite Inhibition of the Transthylakoid pH Gradient by Tetracaine  
 Abstract    The inhibition o f the transthylakoid pH gradient, ApH, and o f photophosphorylation by the local anesthetic tetracaine was investigated with isolated chloroplasts from Spinacia olera-cea L. Tetracaine strongly inhibited ApH in the presence o f low salt concentrations. In the presence o f high salt concentrations, the inhibition o f ApH was much smaller. This effect o f salt concentration was observed only when both, cation and anion were easily membrane permeable. It was concluded that the effect o f salts on ApH inhibition was excerted on the inside o f the thylakoid membrane. The rate o f photophosphorylation, Vv, driven by the PS I-dependent artificial proton carrier phenazine methosulfate decreased with ApH in the presence o f both, high and low salt concentrations. In contrast, Vp driven by the endogenous proton pumps o f PS II + I-dependent linear electron flow was largely independent o f ApH changes in the presence o f low salt concentration. It appeared that energy coupling during linear electron transport, in contrast to artificially produced PS I-dependent coupling, may be localized to membrane-bound proton dom ains which are not accessible to the employed indicators o f ApH. The data were discussed with respect to recent hypotheses on localized energy coupling in chloroplasts. 
  Reference    Z. Naturforsch. 47c, 717 (1992); received June 26 1991/February 17 1992 
  Published    1992 
  Keywords    Photophosphorylation, Energy Coupling, Local Anesthetic, Tetracaine, Salt Concentrations, Localized Protons 
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 TEI-XML for    default:Reihe_C/47/ZNC-1992-47c-0717.pdf 
 Identifier    ZNC-1992-47c-0717 
 Volume    47