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PubMed1983

[Synthesis and pharmacological properties of alkyl esters of various DL-omega-phenylamino acids].

The synthesis of some branched-chain and n-alkyl ester hydrochlorides of DL-2-phenylglycine, DL-3-phenyl-3-aminopropionic acid, DL-4-phenyl-4-aminobutyric acid, DL-phenylalanine and DL-4-phenyl-2-aminobutyric acid is described. For 28 alkyl esters of these DL-amino acids, the pharmacological data about the antagonism against spasms induced by barium chloride, histamine and acetylcholine in the guinea-pig ileum in vitro, as well as about the acute toxicity of intraperitoneally administered doses in the mouse, are reported. Empirical structure-activity relationships established for 36 compounds of this group of substances are discussed. It was found that the maxima of the four actions mentioned depended upon the length of the carbon chain in the molecule. In contrast, no clear-cut branching effect was observed. With reference to toxicity, DL-4-phenyl-2-aminobutyric acid n-octyl ester hydrochloride has been found to be the most favourable spasmolytic agent among the compounds under investigation.

Amino Acids↗
PubMed1983

[Synthesis and spectrum of pharmacologic action of aryl-arylamino- and aryl-aryliminoacetonitriles].

Aminoacetonitriles were synthetized from arylaldehyde, arylamine and cyanhydrogene. Their dehydrogenation led to the iminoderivatives. The compounds were evaluated for spasmolytic activity in vitro. Some aryl-arylaminoacetonitriles showed significant inhibition of the histamine-induced contraction in guinea-pig ileum and acetylcholine-induced contraction in rat ileum. Structure-activity relationships are discussed.

Acetonitriles↗
PubMed1983

[Clinical trial of febuprol, a new substance with choleretic activity. Study of efficacy and tolerability].

In a clinical trial, performed according to new criteria of the AMG (Arzneimittelgesetz) 1976, a new choleretic monosubstance 3-n-butoxy-1-phenoxy-2-propanol (code number: K 10.033, H 33, febuprol, Valbil) has been tested. The clinical investigations conducted on 712 healthy volunteers and patients within a period of 4 years showed that Valbil is an effective and safe drug. Besides the choleretic properties, febuprol has some additional spasmolytic and lipid lowering effects.

1-Propanol↗
PubMed1982

[Reactivity of the respiratory tract in healthy humans and with beta-adrenergic blockade].

Airway resistance, FEV 1.0 and lung volumes were measured in 11 normal subjects before and after voluntary hyperventilation and after inhalation of salbutamol and hyperventilation. The measurements were repeated the following day two hours after taking 40 mg propranolol. Under propranolol there is only a minimal increase in inspiratory and expiratory resistance and no change in bronchoconstriction induced by hyperventilation, but the spasmolytic effect of salbutamol is reduced. Blockade of beta-receptors is without influence on airway irritability in subjects without bronchial asthma or chronic asthmatic bronchitis. Blockade of beta-receptors can however reduce the effect of beta-2-receptor stimulants.

Adult↗
PubMed1982

[Current status of drug therapy in male fertility disorders].

Recent advances in the medical treatment of male fertility disturbances by specific and empirical approaches are discussed. Specific approaches follow a pathophysiological concept and require critical patient selection. In contrast, empirical approaches do not allow patient selection, and a predictability of the success is not possible. Therefore, the response of the patients towards one of the available medical compounds has to be checked on an individual basis. Specific treatment includes replacement therapy of hormone-deficient men by human gonadotropins, inhibition of hyperprolactinemia by bromocriptine, antibiotic-antiinflammatory therapy of male genital tract infections and immunosuppressive treatment in cases of autoantibodies against spermatozoa. In addition, special medical approaches are available for disturbances of sperm transport and the retrograde ejaculation using sympathicomimetic or anticholinergic agents. Empirical treatment comprises the use of antiestrogens, human gonadotropins, androgens, kininogenases, and methylxanthines. As supporting therapy psychopharmacological compounds and spasmolytic agents should be mentioned here. The overall result of treatment is moderate. However, considering all possibilities of treatment conception rates between 30% and 50% will be obtained which differ from the spontaneous conception rates of between 10% and 20%.

Androgens↗
PubMed1983

Synthesis of perhydro-1,4-thiazepines, of expected pharmacological activity. Part III. 4-(2-hydroxyethyl)-perhydro-1,4-thiazepine esters.

New esters, derivatives or the title aminoalcohol, were obtained by three classical methods in the reaction of 4-(2-hydroxyethyl)-perhydro-1,4-thiazepine (HEPT) with chlorides (method a), acid potassium salts (method b), and sodium HEPT salts with acid chlorides (method c). Compounds 3 and 5 have weak spasmolytic properties; 5 in a dose of approx. 50 mg/kg strongly depressed the central nervous system.

Animals↗
PubMed1982

[Therapy of acute spastic pain of the biliary and urinary tracts with rociverine].

105 patients with either biliary colics (54) or ureteral colics (51) were treated with rociverine, a new antispastic drug, at a dose of 20 mg iv. The drug showed a rapid and effective spasmolytic activity (total disappearance of painful symptoms in 89% of patients with biliary colic and in 92% of patients with ureteral colic).

Adolescent↗
PubMed1982

Biological properties of 3-benzyl-1,2-benzisothiazole compounds.

By reaction of 3-chloro-1,2-benzisothiazole with phenylacetonitrile, 3-benzyl-1,2-benzisothiazole derivatives can be obtained. These compounds seem to mimic the benzylisoquinoline structure so they can exhibit spasmolytic activities. Both antimuscarinic and direct muscle-relaxant properties have been found with N,N-dimethyl-3-phenyl-3-(1,2-benzisothiazol-3-yl) propylamine hydrochloride.

Acetylcholine↗
PubMed1980

[Pharmacology of N-(2-imidazolin-2-yl)-N-(4-indanyl)amino (indanazoline), a new vasoconstrictive imidazoline compound].

In animal experiments the new imidazoline derivative N-(2-imidazolin-2-yl)-N-(4-indanyl)amine (indanazoline, E-VA-16, as monohydrochloride active substance of Farial) is characterized by a pronounced vasoconstrictive action after local or intravenous application. This is due to a direct action of the compound on alpha-adrenergic receptors. When applied systemically E-VA-16 being a peripherally acting alpha-sympathomimetic induces a rise in blood pressure and a reduction of heart rate and exerts antiphlogistic, spasmolytic, hyperglycemic and diuretic actions. When given by the intranasal route the substance influences blood pressure and heart rate only at concentrations considerably higher than those intended for use in therapy. After enteral administration the effective doses also markedly exceed the single therapeutic doses. There was no evidence of side-effects restricting the use of the drug as compared to other imidazoline derivatives. Studies on the isolated perfused rabbit ear, however, indicated a broader therapeutic range in local application.

Anesthetics, Local↗
PubMed1981

The effects of proxazole on renal function in chronic renal failure.

3-alpha-Phenyl-propyl-5-beta-diethylaminoethyl-1,2,3-oxadiazole (proxazole), a spasmolytic papaverine-like agent, was i.v. administered to 13 patients with chronic renal failure (mean creatinine clearance 46.4 ml/min/1.73 m2), but did not improve renal plasma flow (p-aminohippurate clearance) or glomerular filtration rate (inulin clearance), nor did this agent prevent or modify nor-adrenaline induced renal ischemia. The oral administration of 400 mg proxazole (5.2--6.5 mg/kg/day) for a period of at least 90 days did not improve renal function in 11 patients with chronic renal failure. It is concluded that both i.v. and p.o. administration of proxazole in the dosages used is ineffective in improving renal function in patients with chronic renal failure.

Administration, Oral↗
PubMed1980

Preclinical pharmacologic investigations on a new group of acridine derivatives with oncostatic activity. I. Acute and subchronic action.

The influence of l-nitro-9-/2-dihydroxyethylamino-ethylamino-/-acridine (C-835) and l-nitro-9/3-izopropylaminopropylamino/-acridine (C-846) on the basic functions of animal organism in acute and subchronic experiments was studied. Both compounds displayed distinct all-biologic activity. Their toxicity (LD50) in mice was contained in milligramme interval (i.v.), while LD50 administered into the stomach was several dozen times higher. Even administration in protective phosphate buffer, which provides the most neutral pH, produced quite strong local irritant action. The range between LD50 and LD10 was relatively small, which proved relatively small tolerance factor. Both preparations injected intravenously in the doses starting from several mg/kg had hypotensic influence due to their affinity with the myocardium, the parasymphatetic system and the vascular system. The preparations acted spasmolytically on intestine muscles both in vivo and in vitro in a number of animal species. Central action showed clear stimulating component in a behavioric test. The effect of the compounds in interaction to hypnotic and convulsant drugs was equivocal and dependent on the dose and the reference-preparation. The examined compounds did not influence reproduction processes and did not display the teratogenic action. They impaired only the speed of growth of the newborns. The effect of both examined compounds was qualitatively and quantitatively similar.

Aminacrine↗
PubMedDate not supplied

Synthesis and biological properties of pyrazo-[3,4-B]-pyridine derivatives. II.

By aminoalkylation with diethylaminoethyl chloride of 3-hydroxypyrazo-[3,4-b]-pyridine 1 and its phenyl derivative 2 as well as 3-aminopyrazo-[3,4-b]-pyridine 7 and its phenyl derivative 8, basic ethers 5, 6 and aminoalkanoloamines 9 and 10 have been obtained. Compounds 5, 6 and 10 increased coronary blood flow of the isolated cat heart. At the concentration of 5 +/- 2 mg/ml shoved spasmolytic activity.

Animals↗
PubMed1978

The effect of intravenously administered proxyphylline and Baralgin on the contraction of the human gallbladder.

In subsequent studies 300 mg of proxyphylline (Group 1) and 1 amp Baralgin (Group 2) were administered intravenously to 20 patients in order to study the relaxing effect of proxyphylline and Baralgin on the contracted gallbladder in connection with routine oral cholecystography. After the standard contraction meal (200 ml cream) the intravenously administered proxyphylline had no relaxing effect on the human gallbladder, whereas Baralgin caused a significant dilation. The dilation effect lasted throughout the whole study period (60 min). Proxyphylline concentrations in the serum, determined by gas-liquid chromatography, proved to be on the therapeutic level which is said to be effective in the treatment of obstructive pulmonary disease. Because with proxyphylline no dilation effect on the gallbladder was found, the clinical spasmolytic response to proxyphylline during an acute attack of pain in a patient suffering from gallstones seems to be questionable. Baralgin caused a significant dilation effect on the gallbladder, and it seems to be a useful agent in an acute gallstone attack.

Adult↗
PubMed1981

[The reproducibility of the bronchospasmolytic effects of isoprenaline tests repeated after long intervals under ambulatory conditions].

The functional results of 3 bronchospasmolytic tests using 4 puffs of an isoprenaline-spray repeated in large intervals were compared on 104 patients suffering from obstructive lung diseases. The correlation coefficients and the coefficients of determination of the differences of the forced expiration volume in one second before and after the tests showed no good correspondence of the spasmolytic effects. It is to be stated that the dimensions of an improvement of the functional results can not be prognosticated, not even on condition that the functional situation before the test, the inhalant and the dose would be the same on the repeated test. Therefore an actual test using a known effective drug for the control has to be demanded for the investigation of on bronchospasmolytic inhalant.

Forced Expiratory Volume↗
PubMed1980

[Effect of various phytotherapeutic expectorants on mucociliary transport].

The normal transport velocity of the isolated ciliated epithelium of the frog oesophagus was proved to be 228 +/- 15 micron . s-1. Bromhexin increased this transport rate 1.34 fold and KNEIPP-Hustentee 1.38 fold. The components of the cough tea had different effects on the mucociliar activity. The following ingredients increased the transport rate with falling rank order: Folia farfarae (coltsfoot), fructus foeniculi (fennel), and fructus anisi (anise). Herba plantaginis (plantain), flores verbasci (torch weed), and radix liquiritiae (liquorice) were ineffective whereas semen foenigraeci (foenugrec), radix althaeae (marsh mallow), and herba thymi (mother of thyme) had an inhibiting effect in raising rank order. The latter two groups of ingredients are constituents of the tea because of their attributed additional effects, e.g. protective effects due to mucous layers in the hypopharynx and spasmolytic, secretolytic and bactericide effects.

Animals↗