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Biomedical subjects

Z Kleinrok

Publications and source records attributed to Z Kleinrok.

At least 361 records · Page 20Linked to original sources
PubMedDate not supplied

Comparison of pharmacological properties of rubidomycine and its newly synthesized derivatives DR-22 and DR-27 in animals.

The effect of two newly synthesized 5-amino modified analogues of rubidomycine was submitted to preliminary pharmacological and histological investigations in healthy Albino Swiss mice. The results showed a similarity of the tested properties of the new compounds and commercial rubidomycine, suggesting the same spectrum undesired side-effects after acute administration. Of the two novel compounds DR-22 was found to be less toxic, while much potent in its action on the haematopoietic system in comparison to rubidomycine, in prolonged treatment. DR-22 is a candidate for further, more detailed investigations.

Analgesics↗
PubMedDate not supplied

Opiate-like peptides. Part VIII. Methylamides and dimethylamides of [D-Leu5]-enkephalin and [D-Ala2, D-Leu5]-enkephalin. Synthesis and analgesic activity.

Syntheses of [D-Ala2, D-Leu5]-enkephalin, methyl ester of [D-Ala2, D-Leu3]-enkephalin, methylamides and dimethylamides of [D-Leu5]-enkephalin and [D-Ala2, D-Leu5]-enkephalin are described together with their analgesic activity determined on the basis of four analgesic tests: the hot-plate method, the reaction to electric stimulus, the tail immersion test and the frequency of writhing syndrome test. The neurotoxicity was estimated by the rota-rod test. The most pronounced analgesic effect was induced by compound: [D-Ala2, D-Leu5]-enkephalin, [D-Ala2, D-Leu5-OMe]-enkephalin and [D-Ala2, D-Leu5-NMe2]-enkephalin. In the tail immersion test all analogs did not exhibit analgesic activity.

Analgesics↗
PubMedDate not supplied

The influence of insulin on 5-methoxytryptamine-induced wet dog shake behavior in rats.

The administration of insulin intraperitoneally (2 U/kg) and intracerebroventricularly (4 U per rat) caused an increased wet dog shake response to 5-methoxytryptamine, suggesting an increase in reactivity of central serotonergic structures. Glucose, in doses which prevented hypoglycemia virtually did not change the effect of insulin.

5-Methoxytryptamine↗
PubMedDate not supplied

Preliminary pharmacological evaluation of newly synthesized derivatives of phosphonoamino acids.

Ten newly synthesized derivatives of phosphonoamino acids were subjected to preliminary pharmacological evaluation in mice and rats. We investigated their effect on acute toxicity, body temperature, spontaneous and exploratory activity, electrogenic and pentetrazole convulsions, and motor coordination and gamma-amino-butyric acid concentration in various brain regions. The most active derivatives were alpha-amino-alpha-p-hydroxyphenyl-methylphosphonic acid 40, beta-(alpha-aminoethyl)-carbamoyl-ethylphosphonic acid 43, alpha-amino-beta-phenylethylphosphonic acid 46, and alpha-amino-beta-(p-nitrophenyl)-ethylphosphonic acid 47. Those compounds depressed the spontaneous locomotor activity and displayed protective action in electrogenic and pentetrazole convulsions.

Amino Acids↗
PubMedDate not supplied

The influence of alpha-adrenergic drugs on catalepsy induced by haloperidol or fluphenazine in rats.

Clonidine (ip) and methoxamine (ivc) inhibit the catalepsy produced by haloperidol or fluphenazine. Naphazoline and xylometazoline antagonize the catalepsy produced by haloperidol, but do not affect significantly that produced by fluphenazine. Phenylephrine did not affect the catalepsy produced by either neuroleptic. The results indicate that drugs stimulating central noradrenergic receptors antagonize the action of compounds blocking the central dopaminergic receptors.

Adrenergic alpha-Agonists↗
PubMedDate not supplied

Central action of sanumgerman in mice.

In the behavioral and biochemical investigations performed on Albino Swiss mice it was found that sanumgerman possessed inhibitory properties on the CNS. The mechanism of this action seems to be connected with depression of central catecholaminergic and a stimulation of central serotoninergic neurons.

Animals↗
PubMedDate not supplied

Effects of atropine and toxogonine on metabolism of the isolated rat liver changed by diisopropylofluorophosphate (DEP).

Effects of atropine and toxogonine on metabolism of the isolated rat liver changed by diisopropylofluorophosphate (DFP). Acta Physiol., 1979, 30 (2): 289--294. In the investigations on isolated rat liver it was found that DFP in a dose corresponding to 1/2 of the LD50 inhibited the activity of AChE, caused hypoglycaemia, decreased the level or pyruvate and increased that of lactate and hepatic glycogen, and increased the activity of transaminases. Atropine and toxogonine administered separately in a concentration of 0.5 mg/100 ml reduced the pyruvate level without changing the other parameters. Administered together with DFP they reactivated the activity of AChE, abolished hypoglycaemia and antagonized in part the effect of DFP on lactate level and transaminase activity.

Animals↗
PubMedDate not supplied

Effects of fluorostigmine, toxogonin and atropine on monoamine oxidase activity and the level of biogenic amines in mouse brain.

Effects of fluorostigmine, toxogonin and atropine on monoamine oxidase activity and the level of biogenic amines in mouse brain. Acta physiol. pol., 1979, 30 (4): 437--444. Fluorostigmine (DFP) given i.p. to mice in doses of 1.2 and 2.45 mg/kg reduced MAO activity in the brain. Given in doses of 0.6 and 1.2 mg/kg it reduced the level of noradrenaline and dopamine as well as 5-hydroxytryptamine in the brain. DFP in such doses had no effect on the brain level of 5-hydroxyindoloacetic acid. Toxogonin (5 mg/kg i.p.) or atropine (5 mg/kg i.p.) given together with DFP reduced or abolished completely the inhibitory effect of DFP.

Animals↗
PubMedDate not supplied

Effects of histamine and cimetidine on the levels of serotonin and 5-hydroxyindoleacetic acid in various parts of the digestive tract and in the blood and brain of rats.

In the investigations on male Wistar rats it was demonstrated that histamine (0.05 and 0.5 mg/kg) decreased the serotonin level, without affecting the level of 5-HIAA in the stomach and duodenum. Contrary to this, cimetidine (15, 75 and 150 mg/kg) raised slightly the level of serotonin and decreased the 5-HIAA level in the stomach and duodenum. In the jejunum histamine in the lower dose raised the levels of serotonin and 5-HIAA, and in the higher dose it decreased only the concentration of serotonin. Cimetidine, on the other hand, only in the highest dose increased the serotonin level and decreased significantly the level of 5-HIAA. In the brain a rise of the serotonin level was observed only after histamine. No effects were observed of histamine and cimetidine on the blood serotonin level. Histamine reduced the number of enterochromaffinocytes in the duodenum. These results point to an evident interaction between the histaminergic and the serotoninergic structures in the digestive tract of rats.

Animals↗
PubMedDate not supplied

Effects of pentagastrin and oxyphenonium on the levels of serotonin and 5-hydroxyindoleacetic acid in different parts of the digestive tract, blood and brain of rats.

In the experiments of Wistar rats it was found that pentagastrin in a dose of 0.6 microgram/kg decreased the level of serotonin and increased that of 5-HIAA in the stomach wall, and in a dose of 3 micrograms/kg it had no effect on these parameters, while in a dose of 6 micrograms/kg it decreased only the serotonin level. Oxyphenonium 0.5 mg/kg increased only the 5-HIAA level in the stomach, and in a dose of 5 mg/kg it decreased also the level of serotonin, In the duodenum these substances remained unchanged after pentagastrin administration, but oxyphenonium 5 mg/kg caused a significant fall of serotonin and increase of 5-HIAA, which was associated with a decrease in the number of enterochromaffin cells. In the small intestine pentagastrin 0.6 micrograms/kg increased the serotonin level and decreased that of 5-HIAA, in a dose of 3 micrograms/kg it decreased only the 5-HIAA level, and in the 6 micrograms/kg dose it had no effect on the levels of these substances. Oxyphenonium increased only the intestinal 5-HIAA level but only when administered in a dose of 5 mg/kg. In the brain both higher doses of pentagastrin decreased the serotonin level, and all three doses raised significantly the 5-HIAA level. Oxyphenonium in the higher dose raised the brain serotonin level, but was without effect on the 5-HIAA level. The blood serotonin level was not changed by pentagastrin and oxyphenonium.

Animals↗