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  • 1
    Electronic Resource
    Electronic Resource
    s.l. : American Chemical Society
    Macromolecules 11 (1978), S. 369-373 
    ISSN: 1520-5835
    Source: ACS Legacy Archives
    Topics: Chemistry and Pharmacology , Physics
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    s.l. : American Chemical Society
    Industrial and engineering chemistry 19 (1980), S. 587-592 
    Source: ACS Legacy Archives
    Topics: Chemistry and Pharmacology , Process Engineering, Biotechnology, Nutrition Technology
    Type of Medium: Electronic Resource
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  • 3
    Electronic Resource
    Electronic Resource
    Amsterdam : Elsevier
    Biochimica et Biophysica Acta (BBA)/Lipids and Lipid Metabolism 1168 (1993), S. 340-347 
    ISSN: 0005-2760
    Keywords: (Rat) ; Cholesterol metabolism ; Etofibrate ; Free fatty acid ; Glycerol ; HMG-CoA reductase ; Triacylglycerol
    Source: Elsevier Journal Backfiles on ScienceDirect 1907 - 2002
    Topics: Biology , Chemistry and Pharmacology , Medicine , Physics
    Type of Medium: Electronic Resource
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  • 4
    Electronic Resource
    Electronic Resource
    Amsterdam : Elsevier
    Biochimica et Biophysica Acta (BBA)/Lipids and Lipid Metabolism 963 (1988), S. 42-52 
    ISSN: 0005-2760
    Keywords: (Rat) ; Etofibrate ; Free fatty acid metabolism ; Glycerol metabolism ; Triacylglycerol metabolism
    Source: Elsevier Journal Backfiles on ScienceDirect 1907 - 2002
    Topics: Biology , Chemistry and Pharmacology , Medicine , Physics
    Type of Medium: Electronic Resource
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  • 5
    ISSN: 1435-1463
    Keywords: Catalepsy ; haloperidol ; locomotion ; reserpine ; α-methyl-ptyrosine ; rotation ; substantia nigra lesion ; amantadine ; memantine ; MK-801 ; NMDA receptor antagonism ; plasma levels ; brain levels
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Amantadine (25, 50, 100 mg/kg), memantine (5, 10, 20 mg/kg) and MK-801 (0.05, 0.1, 0.2 mg/kg), all having NMDA channel blocking properties, were compared in three tests used for screening of antiparkinsonian agents in rats, namely: haloperidol-induced catalepsy, locomotor activity in monoamine depleted rats and rotation in rats with a unilateral substantia nigra lesion. Additionally, plasma levels of amantadine and memantine were assessed to gain an insight into the concentration ranges achieved at behaviorally active doses. Amantadine and (+)-MK-801 produced dosedependent inhibition of haloperidol-induced catalepsy while memantine was less efficacious producing clear-cut anticataleptic action at a dose of 10 mg/kg only but failing at 20 mg/kg due to myorelaxant activity. All agents attenuated sedation in monoamine depleted rats with amantadine being the least and MK-801 being the most effective. The same rank order of efficacy was seen in inducing ipsilateral rotations in rats after a substantia nigra lesion. On the basis of the present study and published data, it can be assumed that the doses of amantadine, memantine and MK-801 showing antiparkinsonian-like activity in animals result in plasma levels leading to NMDA antagonism. However, in the haloperidol-induced catalepsy test the efficacy of amantadine was higher than memantine, while the opposite was true for rotation and reserpine-induced sedation indicating pharmacodynamic differences between both agents.
    Type of Medium: Electronic Resource
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  • 6
    ISSN: 1438-2199
    Keywords: Keywords: Amino acids ; N-Methyl-D-aspartate ; Uncompetitive antagonist ; Memantine ; MRZ 2/579
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary. There is general agreement that moderate affinity uncompetitive NMDA receptor antagonists combine good efficacy and tolerability in animal models of disturbances in glutamatergic transmission. There are several theories on which properties are important for this profile including 1, rapid access to the channel at the start of pathological overactivity 2, rapid, voltage-dependent relief of blockade during physiological synaptic activation and 3, partial untrapping. Merz has developed a series of novel uncompetitive NMDA receptor antagonists based on the cyclohexane structure. In cultured hippocampal neurones MRZ 2/579 (1-amino-1,3,3,5,5-pentamethyl-cyclohexane) shows similar blocking kinetics to memantine (Kon 10.7 * 104 M−1 sec−1, Koff 0.20 sec−1 at −70 mV) and binds at the same depth in the NMDA receptor channel (δ = 0.8). The potency of MRZ 2/579 assessed as Kd = Koff/Kon = 1.87 μM agrees well with the IC50 of 1.29 μM against steady-state currents in cultured hippocampal neurones (at −70 mV) and with the Ki in [3H]-MK-801 binding of 0.65 μM. MRZ 2/579 protected cultured cortical neurones against glutamate toxicity with an IC50 of 2.16 μM and was also effective in protecting hippocampal slices against hypoxia / hypoglycaemia-induced reduction of fEPSP amplitude in CA1 with an EC50 of 7.01 μM. MRZ 2/579 has similar potency and bio-availability to memantine in vivo assessed using microdialysis, microiontophoresis and MES-induced seizures. Initial characterization in animal models provides strong support for the assump-tion that MRZ 2/579 could be a useful therapeutic in morphine/alcohol dependence, inhibition of morphine tolerance, chronic pain and as a neuroprotective agent.
    Type of Medium: Electronic Resource
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  • 7
    Electronic Resource
    Electronic Resource
    Springer
    Amino acids 19 (2000), S. 167-172 
    ISSN: 1438-2199
    Keywords: Keywords: Amino acids ; NMDA ; Channel blockers ; Memantine
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary. The previous overviews provided the basis for better therapeutic efficacy/tolerability of low to moderate affinity NMDA channel blockers. This prediction finds support in in vitro studies comparing protective and plasticity impairing effects (therapeutic vs. side-effect) of memantine and (+)MK-801. In fact it turned out that memantine had a far better therapeutic index. But can it be confirmed in the in vivo situation?
    Type of Medium: Electronic Resource
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  • 8
    ISSN: 1438-2199
    Keywords: NMDA receptors ; Glutamate ; Behaviour ; MRZ 2/570 ; MRZ 2/576 ; L-701,324
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary It is not clear what therapeutic application is most likely for agents blocking glycine site of the NMDA receptors (glycineB). Majority of the studies to date used either glycineB antagonists with doubtful brain penetration or partial agonists. Following systemic administration to rats of our newly developed glycmeB antagonists (MRZ 2/570; 2/571 and 2/576) and L-701,324 (MSD) as a reference agent the following behavioural effects were observed: weak (if any) antiparkinsonian-like effects, lack of anxiolytic activity, inhibition of physical and motivational aspects of morphine dependence and neuroprotective activity in global ischaemia. The side effects include: sedation, ataxia, and myorelaxation. We detected neither vacuolisation in the cingulate cortex nor impairment of pre-pulse inhibition indicating lack of psychotomimetic potential.
    Type of Medium: Electronic Resource
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  • 9
    Electronic Resource
    Electronic Resource
    Springer
    Knee surgery, sports traumatology, arthroscopy 1 (1993), S. 97-99 
    ISSN: 1433-7347
    Keywords: Shoulder instability ; Overhead sports ; Impingement syndrome ; Rotator cuff ; Schultergelenksinstabilität ; Uberkopfsport ; Impingement-Syndrom ; Rotatorenmanschette
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine , Sports Science
    Description / Table of Contents: Zusammenfassung Als Instabilitäts-Impingement wird eine funktionelle Schädigung der Rotatorenmanschette im Subacromialraum bezeichnet, als deren Ursache eine Schultergelenksinstabilität angesehen wird. Die genannte Erkrankung tritt häufig bei denjenigen Sportarten auf, die mit wiederholten Überkopfbewegungen in Abduktion/Außenrotation einhergehen. Dies ist bei Wurfsportarten wie z. B. Handball oder Speerwurf, Schlagsportarten wie Tennis oder Badminton oder auch Gewichtheben und Schwimmen der Fall. Bei den Patienten, bei denen die konservative Behandlung in Form von muskulärer Stabilisierung versagt, ist die operative Therapie — ventrale Stabilisierung, ggf. Erweiterung des Subacromialraumes and Revision der Rotatorenmanschette — indiziert. In der Zeit von Oktober 1988 bis April 1992 wurden in unserer Klinik 66 Schultergelenke bei 64 Leistungssportlern aus den o. g Sportarten mit Instabilitäts-Impingement der Schulter nach Versagen einer konservativen Therapie einer operativen Behandlung unterzogen. Die Erfolgsrate der operativen Behandlung des Instabilitäts-Impingements der Schulter liegt bei nahezu 90%.
    Notes: Abstract An impingement of the rotator cuff can be caused by chronic anterior instability of the shoulder joint. This particular disease is often found in athletes engaged in overhead motion in abduction/external rotation of the arm, such as in ball sports like volleyball or European handball, racket sports like tennis or badminton, or swimming. For those patients that cannot be cured by conservative treatment such as muscular stabilization, surgical treatment is indicated: anterior reconstruction of the capsule and/or the glenoid labrum, and in addition — if necessary — subacromial decompression and revision of the rotator cuff. Between October 1988 and April 1992, we operated on 66 shoulders in 64 top athletes suffering from chronic anterior or multidirectional instability of the shoulder joint that had caused an impingement syndrome of the rotator cuff. In all cases, the athlete was unaware of the instability. Conservative treatment had been unsuccessful. Surgical treatment was successful in close to 90% of the athletes.
    Type of Medium: Electronic Resource
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  • 10
    ISSN: 1438-2199
    Keywords: NMDA receptors ; Glycine site ; Antagonists ; Partial agonists ; Desensitisation ; Subtypes
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Glycine is a co-agonist at NMDA receptors and it's presence is a prerequisite for channel activation by glutamate or NMDA. Physiological concentrations reduce one form of NMDA receptor-desensitization. Interactions between the glycineB site and other domains of the NMDA receptor are complex and include the glutamate, Mg+ and polyamines sites. Glycine shows different affinities at various NMDA receptor subtypes probably via to allosteric interactions between NMDA2 subunits and the glycine recognition site on the NMDAR1 subunit. There is still some debate whether the glycineB site is saturatedin vivo but it seems likely that this depends on regional differences in receptor subtype expression, local glycine or D-serene concentrations and the expression of specific glycine transporters. GlycineB antagonists and partial agonists have been reported to have good therapeutic indices as neuroprotective agents against focal ischaemia and trauma, anti-epileptics, anxiolytics, anti-psychotomimetics and in models of chronic pain. They clearly lack two potentially serious side effects classically associated with NMDA receptor blockade, namely neurodegenerative changes in the cingulate/retrosplenial cortex and psychotomimetic-like effects. This improved therapeutic profile may be partially due to the ability of full glycineB antagonists to reveal Gycne-sensitive desensitization and possibly also via functional and/or regional NMDA receptor subtype selectivity.
    Type of Medium: Electronic Resource
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