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At least 127 records · Page 7Linked to original sources
PubMed1982

Comparative studies of cerebral vasodilators on relaxation activities in isolated basilar, mesenteric and pulmonary arteries of rabbits.

Effects of cerebral vasodilators such as bencyclane, cinnarizine, and papaverine were comparatively studied using helically cut basilar and superior mesenteric arteries and radial muscle preparations of pulmonary arteries with the sympathetic nerve isolated from rabbits. The order of relaxation activities on high K+-induced contractures was cinnarizine>bencyclane>papaverine in basilar strips and cinnarizine>papaverine>bencyclane in mesenteric strips. Relaxation responses of basilar strips to cinnarizine and bencyclane were faster and more marked than those seen in mesenteric strips. Responses to papaverine were equipotent in both preparations. The action of cinnarizine alone was irreversible. In mesenteric strips, the order of the sensitivity of contractile responses to cumulatively applied biogenic amines was serotonin>noradrenaline>histamine. Cinnarizine produced an antihistaminergic action, while bencyclane produced an antiserotonergic action. In pulmonary arteries, 6 x 10(-6) g/ml papaverine inhibited contractile responses to 2, 5, and 25 Hz nerve stimulation in a frequency-independent manner together with inhibition of responses to noradrenaline. Bencyclane at 6 x 10(-6) and 10(-5) g/ml selectively inhibited in a dose-dependent manner contractile responses only to 25 Hz without inhibition of responses to noradrenaline. These results were discussed in comparison with findings of the cerebral vasodilators obtained using other experimental techniques. Spiral strips of basilar arteries from rabbits in combination with peripheral arteries may be used as a simple quantitative, and reproducible screening method in a preclinical stage for drug evaluation of cerebral vasodilators.

Animals↗
PubMed1977

[The effect of fludilat on carbohydrate metabolism].

Fludilat (bencyclane-hydrogen-fumarate) increases the O2 consumption and CO2 production of a 10% bovine lens homogenate. An increase of the glucose substrate supply of the homogenate from 25 mM to 37 mM enlarges the above mentioned effects. Investigations on the content of ATP, ADP and AMP show that bencyclane is able to stabilize the physiologic distribution pattern of the three free adenine nucleotides. Changes of the distribution pattern pointing to disturbances of the energy metabolism could in part be normalized by incubation with the addition of bencyclane. This is not only true for lens homogenates but also for whole bovine lenses. Investigations with the enzymes fumarase and malatedehydrogenase indicate that the fumaric acid rest of bencyclane may serve as a substrate for these enzymes in the same way as fumarate. The Km-values found are identical.

Adenosine Diphosphate↗
PubMed1978

[Primary shape change of platelets in vitro (author's transl)].

Studies with interference contrast microscopy reveal that platelets undergo a typical shape change within 30--60' after venepuncture, i.e. swelling, formation of large tentacles, tiny protrusions and vesicles at the platelet surface. This "shape change" can be observed in citrated blood and PRP, heparinized blood and EDTA-blood as well. It is enhanced by low incubation temperatures (4 degrees C, 10 degrees C) and delayed at 37 degrees C as compared with room temperature. An increased number of primarily shape changed platelets is found if platelets are strongly mechanically irritated at blood sampling. The shape change is partly reversible in vitro, it is completely or almost completely reversible in vivo. Some antiaggregating agents inhibit the in vitro shape change at varying degrees (Bencyclan, SH 869 greater than ASA greater than D-Propranolol). The shape change is partly inhibited after oral or i.v. administration of ASA. A typical transformation of platelets into "spheric" forms can be observed following the addition of Bencyclan, SH 869 and D-Propranolol to PRP in vitro. The spontaneous "primary shape change" which occurs in PRP or blood after blood sampling is probably different from the secondary ADP-induced shape change. The primary shape change may influence the results of different platelet function and aggregating tests. The shape change kinetics of "healthy" subjects and patients with Hodgkin's disease differ significantly. The described method may gain more clinical interest in the future.

Aspirin↗
PubMed1986

Effects of cerebro-protective agents on enzyme activities of rat primary glial cultures and rat cerebral cortex.

The effects of different cerebro-protective agents on selected key enzymes of the energy metabolism of rat primary glial cultures and rat cerebral cortex were studied. As indicators for the capacity of the most important pathways of energy metabolism the following enzyme activities were determined: hexokinase (HK), phosphofructokinase (PFK), pyruvate kinase (PK), lactate dehydrogenase (LDH), glucose-6-phosphate dehydrogenase (G-6-P-DH), malate dehydrogenase (MDH), glutamate dehydrogenase (GDH), and cytochrome-c-reductase (CCR). After a one week growth period, rat glial cultures were incubated for 3 or 4 weeks with the substances to be tested. Bencyclane (5 X 10(-5) mol/l) increased the activities of HK, G-6-P-DH, and LDH, whereas PFK and CCR were reduced. Pyritinol (10(-4) mol/l) led to a higher G-6-P-DH activity, simultaneously lowering the values for PFK, CCR, PK, LDH, and MDH. Under the influence of an extract of the leaves of Ginkgo bilobae (EGB; 100 mg/l) PFK, LDH, and MDH activities were reduced. All these alterations in enzyme activities went along with simultaneous reductions in protein content, therefore not allowing to exclude toxic effects with regard to the doses used. Moreover, direct interference with the analytical procedure was demonstrable for bencyclane and EGB. Piracetam (10(-3) mol/l), flunarizine (10(-6) mol/l), dihydroergocristine (5 X 10(-6) mol/l), and nicergoline (5 X 10(-6) mol/l) failed to induce any alteration in the employed doses. The most striking effects were obtained with meclofenoxate which was tested at 10(-3) and 10(-4) mol/l. The higher dose caused an elevation of HK, PFK, CCR, G-6-P-DH, GDH and MDH activities, while slightly reducing PK. With the lower dose of meclofenoxate CCR and G-6-P-DH activities were increased. Short-term incubation of the cultures with 10(-3) mol/l meclofenoxate for 24 hr led to an increase in LDH, G-6-P-DH, and GDH activities. Chronic incubation with meclofenoxate (10(-3) mol/l) followed by 48 hr deprivation of the drug resulted in elevated HK, PFK, CCR, G-6-P-DH, GDH, and MDH activities. These changes were accompanied by alterations in related metabolite levels. These include elevations in the concentration of creatine phosphate and fructose-1,6-bisphosphate, whereas glucose-6-phosphate levels were reduced. After one week of meclofenoxate deprivation the activities of CCR and G-6-P-DH were still elevated. The metabolites of meclofenoxate dimethylaminoethanol (DMAE; 10(-3) mol/l) and p-chlorophenoxyacetic acid (10(-3) mol/l) were also investigated.(ABSTRACT TRUNCATED AT 400 WORDS)

2,4-Dichlorophenoxyacetic Acid↗
PubMed1988

Slow channel inhibitor effects on brain function: tolerance to severe hypoxia in the rat.

1. The protective effects of ten slow channel inhibitor drugs against severe progressive hypoxia were investigated in rats breathing spontaneously during light anaesthesia. Respiration, heart rate, electrocorticogram (ECoG) and/or electroencephalogram (EEG) were recorded. 2. Tolerance times were monitored from hypoxia onset until cessation of respiration, ECoG, EEG synchronization, and 'background-EEG'. Drugs were administered i.v. 5 min before the onset of hypoxia. 3. Verapamil, gallopamil, and nimodipine resulted in a significant increase of tolerance times; fendiline and bepridil showed a small increase (not significant); bencyclan and prenylamine were ineffective; cinnarizine and diltiazem slightly reduced tolerance times as did flunarizine at low doses. 4. At protective doses, verapamil, gallopamil, and nimodipine significantly raised the respiration rate but had little or no cardiac depressor effects. Bencyclan showed ventilatory drive but cardiocirculatory depression. A clear-cut ventilatory drive did not occur with the other ineffective slow channel inhibitors. 5. It is suggested that the protective actions observed were not due to slow channel inhibition per se, nor to spasmolytic potency or increased cerebral blood flow. Ventilatory drive associated with other cardiopulmonary actions which secondarily raise the brain oxygen supply are likely to be responsible for this effect.

Animals↗
PubMed1978

[Myotropic spasmolysis in the treatment of ureteric colics (author's transl)].

The effectiveness of parasympathicolytic drugs in the treatment of ureteric colics is doubtful. Bencyclane is a new myotropic substance. Its spasmolytic effect on smooth muscle is five times stronger than that of papaverine. The results of the clinical use of Bencyclane in cases of ureteric colic are described and discussed.

Bencyclane↗
PubMed1992

Influence of deproteinized hemodialysate on rest pain and walking distance in the presence of peripheral chronic arterial occlusive disease.

In a controlled and randomized single-blind study (blind observer) the clinical efficacy of intra-arterial therapy with a metabolically active deproteinized dialysate from calf blood has been tested against a vasodilating and hemorheologically active reference substance (bencyclan). Over a period of four weeks 28 patients each received 20 intra-arterial infusions of the deproteinized hemodialysate 20% for infusion. The reference group with 30 patients was treated with 250 mg bencyclan in 250 mL saline 0.9%. As for the target criteria, rest pain and consumption of analgesics, the hemodialysate treatment proved superior to the therapy with the reference substance. Both preparations induced to a small extent pain-free walking distances: hemodialysate group, 29.2 +/- 14.6 m; reference group, 25.8 +/- 18.7 m (group difference not significant).

Animals↗