PubMed Health⌕ Search

Biomedical subjects

K Kolasa

Publications and source records attributed to K Kolasa.

64 records · Page 4Linked to original sources
PubMedDate not supplied

Synthesis and pharmacological properties of diphenylimidazolidine acetic and propionic acids derivatives.

Several derivatives of diphenylimidazolidine-2,4-dione and diphenylimidazolidin-4-one acetic and propionic acids have been synthesized. Some of them were screened for their effect on the CNS in mice and rats. All the investigated compounds showed an analgesic activity. The most active one was 1-benzyl-5,5-diphenyl-3-imidazolidine-2,4-dione acetic acid. That compound exerted an inhibitory activity against the CNS, anxiety-relieving, anticonvulsant and antidepressive effects.

Acetates↗
PubMedDate not supplied

Preliminary pharmacological investigation on 38 aminophosphonic acids and their derivatives.

Central pharmacological properties of 38 aminophosphonic acids and their derivatives, mostly newly synthesized, were investigated on mice and rats. Acute toxicity, neurotoxic activity, influence on spontaneous locomotor activity, body temperature, electrogenic and pentetrazol convulsions, on cerebral GABA level were tested. The most active compounds were (in a decreasing order of activity): 2-amino-7-phosphonoheptanoic, 2-amino-5-phosphonovaleric, 2-amino-8-phosphonooctanoic, 2-amino-2-methyl-3-methylphosphonopropionic, and 3-amino-3-hydroxy-5-phosphonovaleric acid.

Amino Acids↗
PubMedDate not supplied

Opiate-like peptides. Part XI. 2-[2-phenyl-1,3-indandionyl]--amides of enkephalin analogs. Synthesis and analgesic activity.

Four enkephalin analogs containing C-terminal 2-amino-2-phenyl-1,3-indandione residue were prepared: [Met-NHPID5]--enkephalin (E3), [D-Ala2,Met-NHPID5]--enkephalin (E4), [Leu-NHPID5]--enkephalin (E5), [D-Ala2,Leu-NHPID5]--enkephalin (E6). Their analgesic activities were assayed by three in vivo tests: the "hot plate" method, the reaction to electric painful stimulus and the writhing syndrome test. Neurotoxicity effects were determined by the rota-rod test. The most pronounced analgesic effect was induced by compounds with D-Ala in position 2, particularly in the "hot plate" test.

Animals↗
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

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

Effects of histamine and H1 and H2-receptor antagonists on the wet-dog-shaking episodes in rats induced with lithium chloride.

In the experiments carried out on Wistar rats it was demonstrated that histamine administered intraventricularly had no effect on the number of wet-dog-shaking episodes induced with lithium chloride. Thenalidine and antazoline, antagonists of the H1 receptor, and cimetidine and ranitidine, antagonists of the H2 receptor reduced the number of shaking episodes proportionally to the dose. These results may suggest that the reduction of the number of shaking episodes induced with lithium chloride was connected with blockade of histamine receptors, although an indirect effect of H1 and H2-receptor antagonists on the serotoninergic and cholinergic systems cannot be ruled out.

Animals↗
PubMedDate not supplied

Preliminary studies on the central action of new 1,5-benzodiazepine derivatives.

Preliminary studies were carried out on pharmacological central action of 13 newly synthesized 1,5-benzodiazepine derivatives (compounds W1--W13), in comparison with allobarbital and diazepam. The results of the tests indicated that two of the compounds seem to be particularly interesting owing to their ataractic properties, low toxicity and none or weak hypnotic action and negligible ability to disturb the motor coordination.

Animals↗
PubMedDate not supplied

Effect of histamine and H1 and H2 receptors antagonists on carbachol-induced wet-dog shakes in rats.

Intracerebroventricular administration of carbachol chloride induced a characteristic wet-dog shake response in rats. Histamine did not change the number of wet-dog shakes during a 60 min observation but intensified the number of episodes in the first 30 min of the experiment. Antagonists of H1 (thenalidine and antazoline) and H2 (cimetidine and ranitidine) receptors, attenuated carbachol-induced wet-dog shakes. It may be suggested that inhibition of the central histaminergic structures decreased central cholinergic activity.

Animals↗
PubMedDate not supplied

Effects of histamine and H1 and H2-receptor antagonists on wet-dog-shake episodes in rats induced with tranylcypromine and 5-methoxytryptamine.

Intraperitoneally administered tranylcypromine and 5-methoxytryptamine induced in rats the so called wet-dogs-shake behaviour. Histamine injected intraventricularly had no effect on the number or episodes of this behaviour during the first 40 minutes of observation. On the other hand, dimaprit in doses of 5 micrograms/rat injected also intraventricularly increased the number of these episodes. Thenalidine and antazoline--antagonists of the H1-receptor, and cimetidine and ranitidine--antagonists of the H2-receptor, decreased the number of these episodes proportionally to the injected dose. Similar effects were obtained after cimetidine injection into the lateral ventricle. In the light of these observations it may be supposed that these antihistaminic agents exert an inhibitory effect not only on the histaminergic system but decrease indirectly also the activity of the serotoninergic system.

5-Methoxytryptamine↗