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At least 19 recordsLinked to original sources
PubMedDate not supplied

Relative potency of the atropine-like effects of a new parasympatholytic drug, scopolamine-N-(cyclopropyl methyl) bromide and those of hyoscine-N-butyl bromide.

A double-blind crossover trial with a 4-point bioassay was carried out in 8 convalescent in-patients to study the relative potency of scopolamine-N-(cyclopropyl methyl) bromide (DA 3177), a new parasympatholytic drug, administered at doses of 2.5 mg and 5 mg i.v., and hyoscine-N-butyl bromide, administered at doses of 10 mg and 20 mg i.v., in producing atropine-like effects. The results showed that the effects on heart rate and near point of accommodation were slightly less with DA 3177, while its effects on salivary secretion were a little greater than those of hyoscine-N-butyl bromide. It is suggested that study of the pharmacodynamic effects of parasympatholytic drugs is a relatively simple way of predicting which doses should be effective spasmolytically.

Accommodation, Ocular↗
PubMed1975

Comparative studies of parasympatholytic drugs on stomach (double blind test) and analysis of relation between gastric form and tonus.

Effects of 3 kinds of parasympatholytic drugs (timepidiumbromide, hyoscine-N-butylbromide and prifinium-bromide) and placebo (physiological saline solution) on the gastrointestinal tract were evaluated roentgenographically by double blind technique in a total of 101 male human subjects. The results may briefly be summarized as follows: 1. There were significant differences on hypotonic rate being one of the indexes of the gastric tonus between timepidium-bromide and placebo. The effects of 3 experimental drugs were significantly high as compared with that of placebo on peristaltic movement of the stomach. The effect of timepidium-bromide was significantly different from that of placebo on the site of arrival of barium. 2. The comparison of degrees of the gastric tonus between main and control tests revealed that the effect of placebo obtained in the main test was significantly inferior to that of hyoscine-N-butylbromide obtained in the control test, whereas there existed no significant differences of the effects among 3 active drugs. 3. Effects of each drug on the gastric tonus which was scored by hypertonic, normotonic and hypotonic state were evaluated by stratification. The result showed that the effect of timepidium-bromide was significantly greater than that of placebo. 4. All active drugs were not significantly different in terms of 7 observed values each on the gastric form.

Adhesiveness↗
PubMed1975

[Interactions of some parasympatholytics and structurally similar drugs with bovine serum albumin].

The interactions of the parasympatholytic drugs adiphenin, adiphenin H and propanthelin and the structurally related compounds, diphenhydramine, D-propoxyphene and methadone with bovine serum albumin (BSA) are studied by equilibrium dialysis and ultracentrifugation. The results show that BSA has a few binding sites (n less than 10) for the mentioned drugs. The association between the compounds under study and BSA are relatively weak. The binding constants are in the range of 10(3) l/Mol.

Binding Sites↗
PubMed1975

[Studies on the binding of some parasympatholytics to bovine serum albumin/measurement of relaxation times (author's transl)].

The interactions of the parasympatholytic drugs adiphenin, adiphenin H and propantheline and the structurally related compounds diphenhydramine, D-propoxyphene and methadone with bovine serum albumin (BSA) are studied by means of 1H-NMR-spectroscopy. The relaxation rates of essential protons or proton groups of the bound ligands are obtained by a plot of the observed relaxation rates, which are determined from the alterations of the line widths in the presence of BSA, versus the biopolymer concentration. From the stabilization factors R thus obtained it can be concluded that there exist defined but relatively weak associations between these drugs and BSA; both the hydrophobic aryl moieties and the ionized amino groups are involved in these interactions.

Dextropropoxyphene↗
PubMed1979

[Effect of an adrenergic-parasympatholytic aerosol combination on the respiratory function].

The ventilatory and cardiocirculatory effects of salbutamol-ipratropium aerosol were examined in 27 subjects with bronchial obstruction. The activity of the association was compared with that of the two components at therapeutic doses. Then the effects and possible side-effects of the association were assessed at increasing doses. Lastly, the association was compared with its components. The association had the same latency time, but a more prolonged effect (still effective after 120'), when compared with salbutamol. It was decidedly superior to the parasympatholytic. No side-effects of any kind were observed.

Aerosols↗
PubMed1976

The influence of some sympatholytic, parasympatholytic and serotonin-synthesis-inhibiting agents on the ultrastructure of the rabbit pineal organ.

The influence of certain drugs on the ultrastructure of rabbit pinealocytes was studied. The results obtained after administration of p-chlorophenylalanine and p-chloroamphetamine support the hypothesis proposed earlier that the smooth endoplasmic reticulum in the light pinealocytes is involved in indoleamine synthesis. The administration of either one of the sympatholytic agents, 6-hydroxydopamine or alpha-methyl-p-tyrosine, induced typical fine structural changes corresponding to those observed after surgical sympathectomy.

5-Hydroxytryptophan↗
PubMed1977

Parasympatholytic (anticholinergic) esters of the isomeric 2-tropanols. 1. Glycolates.

The 38 esters in Table I were prepared from the four isomeric 2-tropanols and a variety of racemic glycolic acids and their optical isomers. Anticholinergic activity in mice was measured in the peripheral nervous system (mydriasis) and in the central nervous system (anti-tremorine) and compared with that of atropine, scopolamine, and racemic 2-quinuclidinyl benzilate. The results (Table III) showed that several esters (such as 8, 12, 14, and 21) had significantly greater activity in both the peripheral and central nervous systems than did the reference compounds. Esters of (+)-2alpha-tropanol were more potent than those of either its epimer (-)-2beta-tropanol or its optical isomer(-)-2alpha-tropanol. Esters derived from (-)-glycolic acids were uniformly more potent than those from the (+)-glycolic acids. Esters of (+)-2alpha-notropanol and five of its N-substituted derivatives had markedly decreased activity. Peripheral/central activity ratios and time-activity profiles for five active compounds are discussed and compared with those of the reference compounds.

Animals↗
PubMed1977

Functional contribution of autonomic innervation to urethral striated sphincter: studies with parasympathomimetic, parasympatholytic and alpha-adrenergic blocking agents in spinal cord injury and control male subjects.

Mechanisms underlying urethral pressure changes at the external sphincter region after administration of neuropharmacologic agents were investigated with cystosphincterometric studies and electromyography of the external urethral sphincter in adult patients with spinal cord injury and control male subjects. Bethanechol chloride, propantheline or phentolamine were administered to 37 spinal cord injury men and 3 normal controls. After cystectomy 3 additional spinal cord injury patients were subjected to bethanechol studies. The results of these studies suggested that the pressure changes in the external sphincter zone were caused predominantly by the concurrent changes produced in the detrusor and/or the smooth muscle components of the proximal urethra and of the external sphincter zone.

Adolescent↗