{"title":"High performance liquid chromatographic (HPLC) measures of hydrophobicity as determined by means of new HPLC columns.","authors":"R Gami-Yilinkou, R Kaliszan","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Two new commercially available reversed phase high performance liquid chromatographic (HPLC) columns were tested from the view point of their usefulness for determination of hydrophobicity by means of partition chromatography. One column comprised a specially prepared hydrocarbon-bonded silica stationary phase material. The other column was packed with a polybutadiene-coated alumina (PBCA) phase. As reference served a regular commercial octadecylsilica (ODS) column. A series of test solutes were pyrazine CH- and NH-acids--the compounds which are able to take part in specific as well as in nonspecific intermolecular interactions. Unique properties of the new hydrocarbonaceous column manifested themselves in regular linear relationships between logarithms of capacity factors and volume percent of methanol in aqueous eluent. The main advantage of the PBCA column is a possibility of performing chromatography at alkaline pH. Both new columns are superior to regular ODS columns in respect of providing reliable chromatographic measures of hydrophobicity. It was observed that hydrophobicity parameters determined in individual HPLC systems are not highly intercorrelated and hence can reflect different structural features of solutes.</p>","PeriodicalId":20276,"journal":{"name":"Polish journal of pharmacology and pharmacy","volume":"44 5","pages":"515-25"},"PeriodicalIF":0.0,"publicationDate":"1992-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12511629","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
B Filipek, J Krupińska, K Zebala, I Szymańska, T Librowski, W Piekoszewski
{"title":"Influence of ethanol on the antiarrhythmic activity of verapamil.","authors":"B Filipek, J Krupińska, K Zebala, I Szymańska, T Librowski, W Piekoszewski","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The aim of this work was to determine the influence of ethanol on the antiarrhythmic activity of verapamil in the model of calcium arrhythmia in rats non-dependent and dependent on ethanol. The results of the experiment show that a combined, single administration of ethanol and verapamil attenuates in a statistically significant manner the antiarrhythmic effect of verapamil. Ethanol administered repeatedly together with verapamil does not diminish the antiarrhythmic activity of verapamil.</p>","PeriodicalId":20276,"journal":{"name":"Polish journal of pharmacology and pharmacy","volume":"44 5","pages":"443-52"},"PeriodicalIF":0.0,"publicationDate":"1992-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12471315","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
A Drabczyńska, M Pawłowski, M Gorczyca, D Malec, J Modzelewski
{"title":"Synthesis and preliminary pharmacological assessment of novel 9-alkylamino substituted pyrimidino-[2,1-f]-purines.","authors":"A Drabczyńska, M Pawłowski, M Gorczyca, D Malec, J Modzelewski","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Two series of N9-alkylaminomethyl-, alkylpiperazino-, alkylpiperidino-substituted 1,3-dimethyl-(hexahydropyrimidino)- and (tetrahydropyrimidono)-[2,1-f]-purines were prepared and their physicochemical and pharmacological properties were described. The most active in central nervous system tests were the compounds with phenylpiperazinealkyl substituent i.e. 1,3-dimethyl-2,4-dioxo-9-[N1N4-(phenyl)-piperazinopropyl]-1, 3,6,7,8,9- hexahydropyrimidino-[2,1-f] purine 6a and its butyl and isobutyl homologs 9 and 12. The compounds depressed statistically significantly spontaneous locomotor and amphetamine activity and showed sedative, analgetic and hypothermizing properties.</p>","PeriodicalId":20276,"journal":{"name":"Polish journal of pharmacology and pharmacy","volume":"44 5","pages":"487-503"},"PeriodicalIF":0.0,"publicationDate":"1992-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12471924","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"XI Congress of the Polish Pharmacological Society with cooperation of the German Society of Pharmacology and Toxicology. Gdansk, September 16-19, 1992. Abstracts.","authors":"","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":20276,"journal":{"name":"Polish journal of pharmacology and pharmacy","volume":"44 Suppl ","pages":"1-267"},"PeriodicalIF":0.0,"publicationDate":"1992-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12533217","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Modulation of the 5-HT1C receptor-mediated behavior by 5-HT2, but not 5-HT1A, receptor activation.","authors":"E Chojnacka-Wójcik","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The effects of 5-HT1A-receptor agonists 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT) and gepirone, a 5-HT1A/5-HT2-receptor agonist 5-methoxy-N,N-dimethyltryptamine (5-MeODMT) and a 5-HT2-receptor agonist (+-)1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane ((+/)DOI) on the 5-HT1C-receptor-mediated exploratory hypoactivity in rats, induced by m-trifluoromethylphenylpiperazine (TFMPP) or m-chlorophenylpiperazine (m-CPP), were studied in the open field test. (+/-)DOI attenuated the effects of TFMPP and abolished those of m-CPP (not dose-dependently). 5-MeODMT showed a weak antagonistic action only at one, intermediate dose. The effects of TFMPP or m-CPP were not changed by 8-OH-DPAT or gepirone. At the same time, 8-OH-DPAT, gepirone, 5-MeODMT and (+/-)DOI themselves practically did not change the exploratory activity of rats. The obtained results permit an assumption that a functional interaction exists between 5-HT1C- and 5-HT2-receptors, but not between 5-HT1C- and 5-HT1A-ones.</p>","PeriodicalId":20276,"journal":{"name":"Polish journal of pharmacology and pharmacy","volume":"44 5","pages":"427-36"},"PeriodicalIF":0.0,"publicationDate":"1992-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12535956","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Pharmacokinetics of amikacin in gamma-irradiated mice.","authors":"S Lipski, A Gasiewski, J Chaś","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Concentrations of amikacin in sera, investigated 24 h after irradiation with 9 Gy gamma-rays of mice, were monitored using TDX system (Abbott), based on the fluorescence polarization immunoassay. Pharmacokinetic parameters of disposition (distribution + elimination) of the drug were calculated from the obtained data. In irradiated mice fast and slow phases of amikacin disposition were noted. In contrary, in the non irradiated mice only one-fast phase of the drug disposition was observed. The dependence of the disposition parameters of the antibiotic to the postirradiation tubular dystrophia and vascular changes was discussed.</p>","PeriodicalId":20276,"journal":{"name":"Polish journal of pharmacology and pharmacy","volume":"44 5","pages":"469-74"},"PeriodicalIF":0.0,"publicationDate":"1992-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12471922","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"New proctolin analogs modified in position 3 of peptide chain--synthesis and their biological evaluation.","authors":"D Konopińska, G Rosiński, W Sobótka","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Six proctolin analogs modified in position 3 of peptide chain such as Arg-Tyr-X-Pro-Thr where X = Gly (1), Val (2), Pro (3), Thr (4), Acp (1-aminocyclopentane-1-carboxylic acid residue) (5), and Ach (1-aminocyclohexane-1-carboxylic acid residue) (6) were synthesized by liquid-phase method. Biological effects of the pentapeptides (1-6) were examined in cardiostimulatory test in vitro in respect to two insect species: American cockroach (Periplaneta americana L.) and yellow mealworm (Tenebrio molitor L.). Results thus obtained pointed out that the presence of L-leucine in the position 3 of proctolin skeleton plays important role in its cardiotropic activity in insects.</p>","PeriodicalId":20276,"journal":{"name":"Polish journal of pharmacology and pharmacy","volume":"44 5","pages":"505-14"},"PeriodicalIF":0.0,"publicationDate":"1992-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12471925","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
S Suski, T Zawadowski, M Bogdal, B Przemyk, B Szafrański
{"title":"Synthesis and central pharmacological screening of new aminoalkoxy derivatives of coumarin and chromene.","authors":"S Suski, T Zawadowski, M Bogdal, B Przemyk, B Szafrański","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Several 8-(2- and 3-aminoalkoxy) derivatives of coumarin and 5-(2- and 3-aminoalkoxy) derivatives of chromene have been synthesized. The strongest, although short-time neurodepressive activity was exhibited by 8-[3-(4-phenyl-1-piperazinyl)propoxy]-7-methoxycoumarin hydrochloride 15.</p>","PeriodicalId":20276,"journal":{"name":"Polish journal of pharmacology and pharmacy","volume":"44 5","pages":"475-85"},"PeriodicalIF":0.0,"publicationDate":"1992-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12471923","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Structure-activity relationship studies of CNS agents. Part VII. The effect of the imidazole fragment in 2-substituted 1-[3-(4-aryl-1-piperazinyl)propyl]imidazoles on their interaction modes with 5-HT1A and 5-HT2 receptors.","authors":"J L Mokrosz, B Duszyńska","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The synthesis and the 5-HT1A and 5-HT2 receptor affinity of 2-substituted 1-[3-(4-aryl-1-piperazinyl)propyl]-imidazoles (1-8) has been described. It has been shown that both the N-3 imidazole atom and the N-1 piperazine one should be considered as possible protonation centers under physiological conditions. It has been found that the folded conformations of 1-8 exist predominantly in solution. Moreover, three different modes of interaction of the analyzed compounds with 5-HT1A and 5-HT2 receptor sites have been proposed.</p>","PeriodicalId":20276,"journal":{"name":"Polish journal of pharmacology and pharmacy","volume":"44 5","pages":"527-38"},"PeriodicalIF":0.0,"publicationDate":"1992-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12471928","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
B Filipek, J Krupińska, I Szymańska, K Zebala, T Librowski, W Piekoszewski
{"title":"Interaction between ethanol and diltiazem in the model of barium arrhythmia in the rat.","authors":"B Filipek, J Krupińska, I Szymańska, K Zebala, T Librowski, W Piekoszewski","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The antiarrhythmic action of diltiazem in the model of barium arrhythmia was studied in rats non-dependent and dependent on ethanol. The results of our studies showed that single intragastric administration of ethanol jointly with diltiazem did not significantly attenuate the antiarrhythmic effect of diltiazem. Ethanol administered repeatedly and jointly with diltiazem influenced the antiarrhythmic action of diltiazem in different ways, depending on the used dose of diltiazem. After repeated joint administration of ethanol and diltiazem in a lower dose, attenuation of the antiarrhythmic effect of diltiazem was not observed. Repeated joint administration of ethanol and diltiazem in a higher dose attenuated the antiarrhythmic effect of diltiazem. Those experiments also showed that single administration of diltiazem did not significantly influence the ethanol level in the blood; however, when administered repeatedly, diltiazem reduced the concentration of ethanol in blood.</p>","PeriodicalId":20276,"journal":{"name":"Polish journal of pharmacology and pharmacy","volume":"44 5","pages":"453-60"},"PeriodicalIF":0.0,"publicationDate":"1992-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12471316","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}