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At least 145 records · Page 8Linked to original sources
PubMed1979

The metabolism of benzyclane [1-benzyl-1-(3-N,N-dimethylaminopropoxy)cycloheptane] in rat and man.

1. Two metabolites, isolated from the urine of rats dosed with bencyclane fumarate, were characterized as cis-1-benzyl-1-(3-N,N-dimethylaminopropoxy)-4-hydroxycycloheptane (metabolite I) and 1-benzyl-1-(3-N,N-dimethylaminopropoxy)-4-oxocycloheptane (metabolite II). 2. Bencyclane and the two metabolites were determined in the urine of rats and volunteers by g.l.c. Metabolite I was a major metabolite in men, being excreted in urine to the extent of 23.5% dose in the first 24 h.

Animals↗
PubMed1979

Effect of mepacrine on gastric motility in the rat.

Mepacrine given orally to rats inhibits gastric motility; its blocking effect is comparable to that of chloroquine, papaverine, and drotaverine, but less expressed than that of bencyclane. Similarly as the delayed gastric emptying induced by chloroquine, the effect of mepacrine is antagonized by acetyl-beta-methylcholine in a dose-related fashion, while that of papaverine, drotaverine, and bencyclane remains unchanged after treatment with the cholinomimetic drug.

Administration, Oral↗
PubMed1976

[Is a medical treatment of glaucomatous field defects possible? Results of a double blind study (author's transl)].

46 patients with field defects due to simple glaucoma were treated with beta-Acetyldigoxin (given as "Placebo") or with beta-acetyldigoxin and Bencyclan (given as Verum) in tablets over 6 months, under strict double-blind conditions and after the elimination of the learning effect of perimetry. 56 out of the 69 eyes which could be evaluated, showed no change of the field during that period, in spite of increasing field defects during the preceeding months in some of them. A deterioration of the field was observed in 3 eyes treated with placebo, 10 eyes became better, one with placebo and 9 with Verum. Digitalis can evidently stop a deterioration and, in exceptional cases, even enlarge the field. Bencyclan with digitalis was found to have a definitely better effect and enlarged field in 9 out of 41 eyes which were treated with the drug, probably by the change of viscosity of the blood perhaps in addition to vasodilation and a better action of the heart. The effect is statistically-significant (p less than 5%).

Bencyclane↗
PubMed1976

Differentiation of intestinal smooth muscle relaxation caused by drugs that inhibit phosphodiesterase.

In this study a number of chemically unrelated smooth muscle relaxants were tested: a) for potency of phosphodiesterase (PDE)-inhibition, using guinea pig colon-PDE and rat erythrocyte-PDE, b) for potency and duration of relaxation of the isolated guinea-pig colon, c) for their interaction with NH4Cl and orciprenaline as well as with "high calcium". Compared with the spasmolytic effect inhibition of guinea pig colon-PDE or rat erythrocyte-PDE was strong for papaverine and some other relaxants but was low or virtually absent with verapamil, hexobendine and bencyclane. The spasmolytic effect of some PDE-inhibitors was found diminished by the PDE-activator NH4Cl. Most of these drugs enhanced the relaxant effect of the "cyclase activator" orciprenaline; the latter are designated A-type drugs. Verapamil, bencyclane, hexobendine and M 13 did not show this type of interaction with NH4Cl and orciprenaline; they are designated B-type drugs. With A-type drugs--but not with B-type drugs--a highly significant correlation was observed between potency of relaxation and inhibition of colon-PDE (r = 0.85) as well as rat erythrocyte-PDE (r = 0.77). The spasmolytic action of aminophylline and papaverine (A-type drugs) was not inhibited by elevation of extracellular calcium to 9 mM, whereas relaxation induced by verapamil and hexobendine (B-type drugs) at 1.8 mM calcium was found abolished by 9 mM calcium. It is concluded that A-type drugs relax guinea-pig colon by inhibition of PDE and accumulation of cAMP, and that B-type drugs in all probability act by (a) cAMP-independent mechanism(s).

3',5'-Cyclic-AMP Phosphodiesterases↗
PubMed1976

The influence of platelet aggregation inhibitors on metastasis formation in mice (3LL).

Platelets were suggested to play a specific role in the haematogenous spread of experimental tumours. To test this hypothesis mice were treated with various inhibitors or platelet function (acetyl-salicylic acid, RA 233, bencyclan-, cyproheptadine). The effect of treatment on the development of lung colonies after i.v. tumour cell injection as well as on the formation of spontaneous metastases from the solid Lewis-lung carcinoma was evaluated. A significant increase of lung colonies after pretreatment with the platelet aggregation inhibitors was found. The effect of long term treatment on spontaneous metastasis formation gave equivocal results. The present investigations do not support the importance of the integrity of platelet function as a prerequisite for metastasis formation.

Animals↗
PubMed1977

Studies on the "vascular labeling" phenomenon in the iris and the ciliary body of the rat after intravenous injection of colloidal carbon.

The occurrence of carbon deposits after intravenous injection of colloidal carbon (vascular labeling phenomenon) in the iris and the ciliary body of the rat eye was studied by vital microscopy, unstained perfused mount preparations, and by electron microscopy. Generally in the untouched eye the vascular labeling phenomenon is either absent or appears only in the form of finest granular deposits in some capillaries and venules of the iris and the ciliary body. A decrease of intraocular pressure by paracentesis causes a certain blackening phenomenon, which prefers the capillaries and the venules of the iris and the capillaries in the ciliary processes. This effect is intensified by a further decrease of the intraocular pressure to -30 mm Hg. Predominantly the deposits are found stronger in the ciliary region than in the iris. Increase of the intraocular pressure of up to 30 mm Hg diminishes the blackening phenomenon. After administration of the vasodilator bencyclane into the anterior chamber the vascular labeling phenomenon shows a clear graduation of carbon affinity depending upon the concentration of the drug: The capillaries and venules are exclusively blackened at low concentrations, additionally the collecting venules and arterioles are influenced at medium and high doses. By electron microscopy an intraluminal as well as an intramural (subendothelial) deposition of carbon, partly accompanied with signs of hemoconcentration, can be seen. Extravascular position of carbon material is seldom observed and restricted to a state of abnormally high vascular permeability. The observations give evidence for a 'gradient of permeability' between the different types of vessels of the terminal anterior uveal vascular system and also permit the assumption that the vessels of the ciliary processes are more permeable than those of the iris.

Animals↗
PubMed1978

[Blood rheology in chronic arterial occlusive disease as influenced by vasodilators (author's transl)].

Increased blood and plasma viscosity was found in patients with chronic arterial occlusion in comparison with healthy probands. The measurements were done at high and low shear rates. Parenteral pentoxifylline (Trental) lowered blood and plasma viscosity of patients significantly, especially when measured at low shear rates. Application of bencyclane (Fludilat) produced variable results. A definite connection between rheological changes and alterations of the protein fractions in plasma could not be established.

Arterial Occlusive Diseases↗
PubMed1977

Rheological changes in the blood of patients with chronic arterial occlusive disease after the administration of vasoactive drugs.

Patients with chronic arterial occlusive disease were found to have higher blood and plasma viscosity levels than healthy controls. Measurements were taken at high and low shear rates. Blood and plasma viscosity in these patients was significantly reduced following parental administration of pentoxifyline, and this effect was particularly pronounced at low shear rates. The changes recorded after administriation of bencyclane did not follow a consistent pattern. There was no significant correlation between the rheological changes measured and changes in plasma protein fractions.

Arterial Occlusive Diseases↗
PubMed1988

Calcium antagonists as a peripherally acting labyrinthine suppressant in humans.

A total of 908 patients with peripheral vestibular disorders were treated with calcium antagonists for periods of 10 to 120 days in a series of controlled clinical trials using a placebo or other medication for comparison. The cumulative analysis of the results indicates that cinnarizine, flunarizine and bencyclan have produced good clinical results, particularly in patients with vascular problems. A comparison between different doses used in different trials revealed a correlation of good clinical results to smaller doses of some of these medications.

Bencyclane↗
PubMed1977

[Influence of vasoactive substances on blood sugar and serum insulin in normal and diabetic carbohydrate metabolism (author's transl)].

The effect of the following vasoactive substances, which are used in the treatment of peripheral arterial occlusive diseases, was investigated in a randomized study in 36 patients with normal and 52 patients with diabetic carbohydrate metabolism by intravenous infusion on the behaviour of blood sugar and serum insulin (IMI) during simultaneous oral glucose tolerance tests (100 g oligosaccharides). The substances used and the doses given were as follows: protein-free calf-blood extract (Actihaemyl, 0,5 ml per kg body weight), bencyclane (Fludilat, 200 mg), naftidrofuryl (Dusodril, 200 mg, pentoxifyllin (Trenal, 200 mg). The results obtained with the simultaneous treatment and oral glucose tolerance test were compared with a second OGTT carried out at an interval of 3-4 days under the same conditions but without administration of the substances (in a cross-over procedure) and the results of these experiments were compared with those obtained from an untreated control group. In subjects with a diabetic metabolic state, Actihaemyl led to a significant reduction of the blood sugar after oral glucose load (p less than 0,05) without producing any change in serum insulin. The same behaviour was exhibited by Fludilat for the total area integral and by Trental for the first 60 min after the oral glucose load. The change in the blood sugar behaviour was only significantly different from the untreated controls with Actihaemyl (p less than 0,05). In subjects with a normal metabolic state neither blood sugar nor serum insulin (IMI) were altered by any of the substances investigated.

Actihaemyl↗
PubMed1982

Heterogeneity of biochemical actions among vasodilators.

Thirty-four vasodilators were screened in several in vitro biochemical assays related to smooth muscle excitation-contraction coupling, binding to beta 1-,beta 2-, and alpha-adrenergic receptors, inhibition of phosphodiesterase activity, and antagonism of calcium accumulation. Isoproterenol and perhexiline only exhibited binding to beta-adrenergic sites. Ergocryptine, tolazoline, and amotriphene only bound to alpha-adrenergic receptors. Leniquinsin, papaverine, proquazone, dioxyline, hoquizil, quazodine, and theophylline were active only as phosphodiesterase inhibitors. Isoxsuprine, nylidrin, and bencyclane bound to alpha- and beta-receptors. Pentoxifylline bound to beta 1-sites and inhibited phosphodiesterase. Cyclandelate bound to beta 2-sites and blocked calcium accumulation. Cinnarizine and flunarizine antagonized calcium accumulation and bound to alpha-sites. Prazosin bound to alpha-sites and inhibited phosphodiesterase. Ethaverine and dipyridamole were inhibitors of phosphodiesterase and calcium accumulation. Nafronyl bound to beta 2- and alpha-sites and antagonized calcium accumulation. Mebeverine bound to beta 2- and alpha-receptors and inhibited phosphodiesterase activity and calcium accumulation. Verapamil bound to alpha-sites, and blocked phosphodiesterase and calcium accumulation. Quinazosin bound to beta 2- and alpha-receptors and antagonized both phosphodiesterase activity and calcium accumulation. Vasodilators that were inactive in all assays included niacin, nicotinyl alcohol, inositol nicotinate, amyl nitrite, sodium nitroprusside, diazoxide, hydralazine, and protoveratrine. Vasodilators should not be considered as a single drug class since they act on various mechanisms related to coupling of neuronal excitation to muscular contractility.

3',5'-Cyclic-AMP Phosphodiesterases↗
PubMed1988

Screening procedure for the detection of alkanolamine antihistamines and their metabolites in urine using computerized gas chromatography-mass spectrometry.

A gas chromatographic-mass spectrometric screening procedure for the detection of the following alkanolamine antihistamines and their metabolites in urine after acid hydrolysis and acetylation is described: bencyclane, carbinoxamine, chlorbenzoxamine, chlorphenoxamine, clemastine, diphenhydramine, diphenylpyraline, doxylamine, mecloxamine, medrylamine, orphenadrine and phenyltoloxamine. The acetylated extract was analysed by computerized gas chromatography-mass spectrometry. An on-line computer allows rapid detection using ion chromatography with the ions m/z 58, 139, 165, 167, 179, 182, 218 and 260. The identity of positive signals in the reconstructed ion chromatograms was confirmed by a comparison of the stored full mass spectra with the reference spectra. Possible interferences with related compounds that yield the same hydrolysis products or metabolites are discussed. The ion chromatograms, reference mass spectra and gas chromatographic retention indices (OV-101) are documented. The procedure presented is integrated in a general screening procedure (general unknown analysis) for several groups of drugs.

Acetylation↗
PubMed1980

Effects of vasodilator drugs, alkaline phosphatase, and cyclic AMP-dependent protein kinase on the 45calcium uptake of sarcolemmal microsomes from human umbilical arteries.

1 A microsomal fraction was prepared from human umbilical arteries by differential centrifugation. The preparation was capable of an oxalate-stimulated Ca2+ uptake at a mean rate of 0.74 nmol Ca2+ mg-1 protein min-1 which could be inhibited by a Ca2+ ionophore, A 23 187, and by Tween 80. 2 The rate of Ca2+ uptake in the fraction obtained by density gradient fractionation paralleled 5'-nucleotidase activity suggesting that vesicles of predominantly sarcolemmal origin were responsible for the microsomal Ca2+ uptake. 3 Cyclic adenosine 3',5'-monophosphate-dependent protein kinase enhanced membrane phosphorylation but did not affect Ca2+ uptake. Preincubation with alkaline phosphatase reduced membrane phosphorylation to a greater extent than Ca2+ uptake. These data are not in favour of a close correlation between Ca2+ uptake and phosphorylation. 4 None of 15 vasodilator drugs (bencyclane, carbocromen, diazoxide, dilazep, hydralazine, indapamide, isosorbide dinitrate, methyl-isobutyl-xanthine, minoxidil, naftidrofuryl, nitroglycerine, prenylamine, sodium nitroprusside, tetracaine, and verapamil) had any effect on Ca2+ uptake at 10(-5) M. This suggests that vasodilator drugs do not act by a direct influence on the Ca2+ pumps of vascular smooth muscle cells.

Alkaline Phosphatase↗
PubMedDate not supplied

Usefulness of the measurement of plasma beta-thromboglobulin (beta-TG) in cerebrovascular disease.

The plasma concentration of the platelet-specific protein beta-thromboglobulin (beta-TG) was measured in 39 normal subjects and 568 patients of neurological diseases. The beta-TG RIA commercially available KIT was also evaluated. Abnormally high plasma levels of beta-TG were demonstrated in groups of ischemic or obstructive cerebrovascular diseases as compared with that of normal subjects. The highest concentrations were found in 8 patients with Moya-Moya disease, (mean concentration of beta-TG was 204.4 ng/ml), completed stroke at an acute stage was next (mean beta-TG level was 194.8 +/- 70.8 ng/ml). On the other hand, many hemorrhagic cerebro-vascular diseases or other neurological diseases such as brain tumors, hydrocephalus, etc. do not show elevated beta-TG levels. In many patients with ischemic or obstructive cerebro-vascular diseases treated with anti-platelet drugs such as Aspirin, Dipyridamole, Bencyclane or Ticlopidine, a significant fall in plasma concentration of beta-TG was chronologically demonstrated. The measurement of plasma beta-TG concentration may be useful not only in the diagnosis of ischemic or obstructive cerebro-vascular disorders but also in judging the efficacy of anti-platelet therapies and prognosis.

Adolescent↗
PubMed1986

[Effects of 4-(o-benzylphenoxy)-N-methylbutylamine hydrochloride (MCI-2016, bifemelane hydrochloride) on coagulation, fibrinolysis, hemolysis, hemorheological properties and platelet aggregation].

MCI-2016 showed little influence on coagulation (APTT) and fibrinolysis (plasma clot lysis activated by urokinase) at doses (concentrations) as high as 300 mg/kg, p.o. or 8.6 X 10(-4) M. Hemolytic action of MCI-2016 was only observed at the concentrations above 2 mM. The drug also showed no influence on blood glucose level (30-300 mg/kg, p.o.). Effects of MCI-2016 on hemorheological properties were studied either in vitro or ex vivo. Above the doses (concentrations) of 100 mg/kg, p.o. and 10 microM, MCI-2016 suppressed the mechanical hemolysis and accelerated the membrane filtration rate. These effects of MCI-2016 were superior to those of cinepazide, Ca-hopantenate, meclofenoxate and pentoxyfylline. MCI-2016 also inhibited platelet aggregation induced by collagen with the IC 50 of 35 to 60 microM (rabbit and human platelets). Secondary aggregations of ADP and epinephrine were also inhibited by MCI-2016. As for reference drugs, bencyclane showed inhibitory patterns similar to MCI-2016. Other drugs examined exhibited little effect. In summary, it may be suggested that MCI-2016 exhibits beneficial influences in the clinical fields of cerebrovascular diseases.

Animals↗
PubMed1976

[The influence of a therapy with vasodilating agents on the sleep EEG of patients with cerebral circulatory disturbances. Results of a double blind study (author's transl)].

In 30 patients (24 men, 6 women) aged from 30-74 years and suffering from ischemic lesions in the cerebral hemispheres all-night EEG recordings before and after a 3 weeks' treatment with vasodilating drugs were carried out. At the same time the development of the clinico-neurological and psychoorganic symptomatology, also using test psychological methods, were studied. The drugs--10 patients received 50 mg raubasin, 6 patients 500 mg bencyclan and the others a salt solution--were administered i.v. Under the treatment no change in the primary sleep EEG findings could be observed, whereas there was an improvement of the clinico-neurological and psychoorganic symptomatology in the drug as well as in the placebo group. The lack of improvement in mood and state of well-being is discussed in its relationship to the sleep behaviour.

Adult↗
PubMed1986

[Effects of drugs on the upper urinary tract of the human].

The effects and the possible mode of action of some drugs were studied in isolated preparations of the human upper urinary tract. Norepinephrine, histamine and serotonin had excitatory effects, whereas isoprenaline had inhibitory effects on smooth muscle activity. Norepinephrine induced different types of mechanical activity in different tissues of the human upper urinary tract suggesting different and separate coupling mechanism between the receptors involved and the calcium pools responsible for initiation of contraction. Acetylcholine had only little effects on smooth muscle activity even in high concentrations. Contractions which were triggered by action potentials or depolarizing extracellular potassium concentrations were highly sensitive to calcium channel blockers. Other drugs with relaxing properties such as papaverine, bencyclane, flavoxate or pitofenone seem to have effects on different calcium activation or calcium storing mechanisms.

Calcium↗
PubMed1989

[The effect of vasodilators on isolated smooth muscle].

Bencyclane (Fludilat), Metamizol (Novalgetol) and Xanthinol nicotinate (Complamin) and their combination were considered as relaxators of smooth muscle. The smooth muscles were isolated from stomach, urinary bladder, oesophagus, vas deferens and aorta of rats. The electrical stimulations induced contractions. The mixture of vasodilators decreased the tonus and induced contractions. The single vasodilators increased tonus and induced spasm sometimes.

Animals↗