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PubMedDate not supplied

Studies on the male antifertility agent gossypol acetic acid. VI. Effect of gossypol acetic acid on the fertility of bonnet monkey. Macaca radiata.

Gossypol acetic acid (4 mg/day/5 days a week) suspended in Tonoferon tonic was given to male bonnet monkeys, Macaca radiata, by oral route for 3 months. Marked reduction in the sperm count/ejaculate and sperm motility were observed after gossypol treatment; both motility and sperm count/ejaculate returned to the normal level 8-10 weeks after termination of gossypol treatment. The citric acid and fructose levels in the semen of gossypol treated monkeys were not different from those of the controls.

Animals↗

PubMed1987

Zuclopenthixol acetate in Viscoleo--a new drug formulation. An open Nordic multicentre study of zuclopenthixol acetate in Viscoleo in patients with acute psychoses including mania and exacerbation of chronic psychoses.

Eighty-three acutely disturbed, psychotic patients were included in an open multicentre study. The aim of the study was to evaluate the clinical effect of zuclopenthixol acetate in Viscoleo (CPT-A). Each patient received from one to four intramuscular injections of CPT-A during the 6-day study period. The duration of action after one injection was between 2 and 3 days and doses from 50 mg to 150 mg were sufficient for most patients. Treatment with CPT-A caused a pronounced and rapid reduction of the psychotic symptoms. At the end of the 6-day test period the mean total score on BPRS in acute non-manic and exacerbated chronic patients was reduced by more than 50 per cent. In acute manic patients the mean total score on BRMS was reduced by 57 per cent already 1 day after injection. Rapidly after the injection of CPT-A a useful short-acting sedation can be expected, but the risk for oversedation even after a second injection is low. The frequency of unwanted effects, including extrapyramidal reactions, was low and the severity of symptoms was most often mild. With a rapid onset of action, a duration of effect of 2 to 3 days, and few and mild side effects, CPT-A offers advantages over the neuroleptic preparations conventionally used in the initial treatment of acutely disturbed, psychotic patients.

Acute Disease↗

PubMed1987

[Excretion of 5-hydroxyindole-3-acetic and 5-methoxyindole-3-acetic acids in cancer patients].

Daily urinary excretion of 5-hydroxy-3-indoleacetic acid (5-HIAA) and 5-methoxyindole-3-acetic acid (5-MIAA) was studied by chromatography-mass-spectrometry in patients with cancer and healthy subjects. A considerable increase in urinary 5-MIAA-excretion was shown in patients with cancer of the stomach, rectum and lung. In some cases, a correlation was found between high urine levels of carcinogenic 5-MIAA and similarly high levels of 5-HIAA excretion with urine.

Humans↗

PubMed1979

Studies on the derivatives of thiazole acetic acid. II. Syntheses and pharmacological analysis of 2-N-aralkylidene and 2-N-aralkyl derivatives of 2-amino-4-p-chlorophenylthiazole-5-acetic acid.

A number of 2-N-aralkylidene, 2-N-aralkyl and 2-N-aralkyl-alpha-sulphoderivatives of 2-amino-4-p-chlorophenylthiazole-5-acetic acid (I, R = H) and its methyl ester (I, R = CH3) were synthesized. As a result of condensation of methyl ester I with various aromatic aldehydes in boiling benzene solution, the Schiff-bases (anils) II--VIII were obtained. After reduction with NaBH4 compounds II--VIII were transformed into adequate amino esters IX--XV. Esters IX--XV heated with diluted aqueous solution of sodium hydroxide underwent selective hydrolysis giving the respective amino acids XVI--XXII. Some of Schiff bases (II, III, V, VII, VIII) reacted with aqueous alcoholic solution of sodium bisulphite after its several (XXIII--XXVII). alpha-sulphoderivatives had been obtained. Several tests were performed in order to detect the anti-inflammatory and immunosuppressive activity of the compounds. The pharmacological analysis allowed us to draw conclusions concerning the relationship between chemical structure and biological activity in this group of compounds. The most efficacious immunosuppressive and anti-inflammatory activity exhibited 2-aralkyl-alpha-sulphoderivatives.

Adjuvants, Immunologic↗

PubMed1985

Stereoisomers of alpha-tocopheryl acetate. III. Simultaneous determination of resorption-gestation and myopathy in rats as a means of evaluating biopotency ratios of all-rac- and RRR-alpha-tocopheryl acetate.

The resorption-gestation test furnishes information on a more complex vitamin activity than is the case with other vitamin E tests, so that correspondingly more importance attaches to the results. A drawback is their questionable validity for species other than the small rodents in which fetal resorption has so far been observed. In the four experiments carried out, RRR-alpha-tocopheryl acetate (alpha-TA) was compared with all-rac-alpha-TA (USP standard) and a mean relative activity of 1.32 was determined. The additional measurement of pyruvate kinase (PK) activity serves to emphasize the correlation with nutrition-linked myopathy. This biochemical lesion is seen in various animal species and man. In two experiments, the parameters fetal resorption and plasma PK activity were measured together. For all-rac-alpha-TA and RRR-alpha-TA, the following activity ratios were calculated: Resorption-gestation 1:1.35; Myopathy 1:1.47. It could be shown that the two parameters are measurable quantitatively in a single experimental set-up and that the results are in good agreement. The accepted activity of 1 mg RRR-alpha-TA = 1.36 USP Units was fully confirmed.

Animals↗

PubMed1981

Studies on derivatives of 2-amino-4-p-chlorophenylthiazole-5-acetic acid. IV. Addition reactions of thioglycolic acid to 2-N-aralkylidene derivatives of 2-amino-4-p-chlorophenylthiazole-5-acetic acid.

In the course of studies on compounds with expected antiinflammatory and immunosuppressive activity a series of new derivatives of 2-amino-4-p-chlorophenylthiazole-5-acetic acid have been synthesized. Several new and unexpected details of the chemical properties of these compounds were revealed. The chemical structure of the new compounds was confirmed by degradation and identification of the decomposition products and by spectral analysis.

Amino Acids↗

PubMed1981

Studies on derivatives of 2-amino-4-p-chlorophenylthiazole-5-acetic acid. V. Syntheses of 2-N-aralkylidene and 2-N-aralkyl derivatives of 2-amino-4-p-chlorophenylthiazole-5-acetic acid.

A number of new N-aralkylidene and N-aralkyl derivatives of amides and hydrazides of 2-amino-4-p-chlorophenylthiazole-5-acetic acid (III-XXIX) have been synthesized. These compounds were obtained in two various ways depending on the character of substituents in the carboxyl group. The chemical structure of the newly obtained compounds was determined on the basis of the data of elementary and spectral analyses.

Amino Acids↗

PubMed1981

Studies on derivatives of 2-amino-4-p-chlorophenylthiazole-5-acetic acid. VI. Syntheses and properties of 2-N-aralkyl-alpha-sulphoderivatives of tert-amides of 2-amino-4-p-chlorophenylthiazole-5-acetic acid.

In the course of the studies on compounds with expected antiinflammatory and immunosuppressive activity several new tert-amides derivatives of 2-N-aralkylamino-alpha-sulpho-2-amino-4-p-chlorophenylthiazole-5-acetic acid were synthesized. Some of the previously described Schiff bases reacted with aqueous alcoholic solution of sodium bisulphite and as a result several (III-VIII) alpha-sulphoderivatives were obtained. The course of the reactions was studied and the structure of the new compounds was confirmed.

Amides↗

PubMed1993

Reduction of sunburn damage to skin by topical application of vitamin E acetate following exposure to ultraviolet B radiation: effect of delaying application or of reducing concentration of vitamin E acetate applied.

The skin of the skh-1 mouse after ultraviolet B (280-320 nm, UVB) irradiation shows the pathological changes typical of sunburn damage: spongiosis (edematous spaces) around some cells, necrosis of keratinocytes, giving rise to sunburn cells, inflammatory infiltration of polymorphonuclear leucocytes, etc. In our previous study, these were accompanied by erythema, increased skin sensitivity, and edematous swelling. The topical application of tocopherol acetate (TA) immediately after the UVB exposure decreased these changes. In this paper, multiple measurements of the skin thickness were made at different locations along the magnetic resonance imaging (MRI) cross-sectional image of the skin. This permits effects to be quantified with (if desired) the contralateral half of the back serving as an internal control, either exposed (positive control) or unexposed (negative control). Topical application of TA resulted in an increase in the concentration of free tocopherol in the skin. No qualitative differences in ultrastructural appearance of the UVB-irradiated, TA-treated skin could be discerned by careful examination. In vivo high resolution video microscopy of blood flow in venules of the irradiated mouse ear revealed a large (tenfold) but not statistically significant decrease in stationary lymphocytes adhering to the venule walls. The delaying of the application of TA up to 8 hours after the termination of UVB irradiation still offered statistically significant protection as did immediate application of 5% TA in diluent Myritol 318 (Delios S, Henkel).

Administration, Topical↗

PubMed1977