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Acta pharmaceutica Nordica最新文献

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Fluoxetine and its two enantiomers as selective serotonin uptake inhibitors. 氟西汀及其两个对映体作为选择性血清素摄取抑制剂。
Acta pharmaceutica Nordica Pub Date : 1990-01-01
D T Wong, R W Fuller, D W Robertson
{"title":"Fluoxetine and its two enantiomers as selective serotonin uptake inhibitors.","authors":"D T Wong,&nbsp;R W Fuller,&nbsp;D W Robertson","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The biochemical and pharmacological profiles of R,S-fluoxetine and its R and S enantiomers have been compared and reviewed. Both enantiomers exhibit profiles analogous to R,S-fluoxetine as inhibitors of serotonin uptake in vitro and in vivo with about equal potencies or a eudismic ratio near unity.</p>","PeriodicalId":7082,"journal":{"name":"Acta pharmaceutica Nordica","volume":"2 3","pages":"171-80"},"PeriodicalIF":0.0,"publicationDate":"1990-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"13352602","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}
引用次数: 0
The covariation of chemical contamination, particulate matter and turbidity in soft polyvinyl chloride infusion fluid bags. 软质聚氯乙烯输液袋中化学污染、颗粒物和浊度的共变。
Acta pharmaceutica Nordica Pub Date : 1990-01-01
P O Roksvaag, G Smistad, T Waaler
{"title":"The covariation of chemical contamination, particulate matter and turbidity in soft polyvinyl chloride infusion fluid bags.","authors":"P O Roksvaag,&nbsp;G Smistad,&nbsp;T Waaler","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>About 200 samples of normal saline, isotonic glucose and Ringer acetate infusions in soft polyvinyl chloride (PVC) bags obtained from three manufacturers have been analyzed by conductometric particle counting, turbidimetry and gas liquid chromatography (GLC). The particle counts were fitted to an exponentially modified log-normal model and integrated for total particle-volume. Di(2-ethylhexyl) phthalate (DEHP) and epoxidized vegetable oils (EVO), which are the main water insoluble contaminants in PVC fluid bags, were determined by GLC. There was a strong linear correlation between turbidity and GLC results. The correlation between particle-volume concentration and the DEHP and EVO concentrations was fairly good. The results seem to verify that an emulsion of plastic additives is formed when soft PVC infusion fluid bags are shaken.</p>","PeriodicalId":7082,"journal":{"name":"Acta pharmaceutica Nordica","volume":"2 5","pages":"327-32"},"PeriodicalIF":0.0,"publicationDate":"1990-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"13238493","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}
引用次数: 0
Potential antitumor agents XVII (1). Cytotoxic agents from indole derivatives and their intermediates. 潜在的抗肿瘤药物XVII(1).吲哚衍生物及其中间体的细胞毒性药物。
Acta pharmaceutica Nordica Pub Date : 1990-01-01
A Andreani, M Rambaldi, A Locatelli, F Andreani, P Aresca, R Bossa, I Galatulas
{"title":"Potential antitumor agents XVII (1). Cytotoxic agents from indole derivatives and their intermediates.","authors":"A Andreani,&nbsp;M Rambaldi,&nbsp;A Locatelli,&nbsp;F Andreani,&nbsp;P Aresca,&nbsp;R Bossa,&nbsp;I Galatulas","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>New indole derivatives and their intermediates were tested as cytotoxic agents on a culture of P388 leukemia cells. The aldehyde 2a was more active than the thiosemicarbazones 3a, b and the nitrosourea 14. The chloroacetyl derivatives 10, 11 were the most potent cytotoxic agents.</p>","PeriodicalId":7082,"journal":{"name":"Acta pharmaceutica Nordica","volume":"2 6","pages":"407-14"},"PeriodicalIF":0.0,"publicationDate":"1990-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"13250853","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}
引用次数: 0
Stereoselective synthesis and the polyene macrolide antibiotics. 立体选择性合成及多烯大环内酯类抗生素。
Acta pharmaceutica Nordica Pub Date : 1990-01-01
S D Rychnovsky
{"title":"Stereoselective synthesis and the polyene macrolide antibiotics.","authors":"S D Rychnovsky","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The stereochemical complexity of roflamycoin and other polyene macrolide antibiotics presents a formidable challenge to the synthetic chemist, and the lack of obvious disconnections makes the retrosynthetic analysis very complex. The alternating (1, 3, 5, ...) polyol chain in roflamycoin is difficult to synthesize in part because there is no simple method to assemble these chains from smaller subunits. We have addressed this problem and developed a simple, convergent method for assembling alternating polyol chains. It is designed around a new class of 1,3-diol synthons: 6-alkyl-4-thiophenyl-1,3-dioxanes. These 1,3-diol synthons are readily available from either homoallylic alcohols or beta-hydroxyesters, which are themselves readily prepared in optically pure form. Reduction of these synthons under the appropriate conditions gives configurationally stable alkyllithiums with either syn or anti stereochemistry. Reaction with electrophiles produces protected syn or anti-1,3-diols.</p>","PeriodicalId":7082,"journal":{"name":"Acta pharmaceutica Nordica","volume":"2 3","pages":"155-60"},"PeriodicalIF":0.0,"publicationDate":"1990-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"13352600","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}
引用次数: 0
Pyrrolizidine alkaloids in Senecio vulgaris L. growing in Iceland. 产自冰岛的绿皮草中吡咯利西啶类生物碱。
Acta pharmaceutica Nordica Pub Date : 1990-01-01
K Ingolfsdóttir, P J Hylands
{"title":"Pyrrolizidine alkaloids in Senecio vulgaris L. growing in Iceland.","authors":"K Ingolfsdóttir,&nbsp;P J Hylands","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The distribution of toxic pyrrolizidine alkaloids in the Icelandic flora has been studied for the first time. In addition to the isolation of senecionine, seneciphylline, and retrorsine from Senecio vulgaris L., the presence of riddelline was confirmed by high resolution NMR spectroscopy. The presence of this alkaloid in S. vulgaris has previously been controversial. Furthermore, senecionine oxide and seneciphylline oxide were isolated by preparative centrifugal chromatography.</p>","PeriodicalId":7082,"journal":{"name":"Acta pharmaceutica Nordica","volume":"2 5","pages":"343-8"},"PeriodicalIF":0.0,"publicationDate":"1990-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"13238404","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}
引用次数: 0
Synergistic action of clotrimazole and certain anionic surfactants may be due to ion pair formation. 氯霉唑与某些阴离子表面活性剂的协同作用可能是由于离子对的形成。
Acta pharmaceutica Nordica Pub Date : 1990-01-01
M Pedersen
{"title":"Synergistic action of clotrimazole and certain anionic surfactants may be due to ion pair formation.","authors":"M Pedersen","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>A synergistic effect of clotrimazole and certain anionic surfactants against a strain of Candida albicans was confirmed. Measurement of apparent partition coefficients indicated that lipophilic ion pairs between clotrimazole and anionic surfactants were formed. It is suggested that the synergistic effect of the drugs may be due to ion pair formation.</p>","PeriodicalId":7082,"journal":{"name":"Acta pharmaceutica Nordica","volume":"2 6","pages":"367-70"},"PeriodicalIF":0.0,"publicationDate":"1990-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"13250969","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}
引用次数: 0
The influence of salicylic acid on the in vitro release of anthralin from an o/w cream. 水杨酸对0 /w乳膏中炭疽素体外释放的影响。
Acta pharmaceutica Nordica Pub Date : 1990-01-01
M Kneczke, C Rahm, L Landersjö
{"title":"The influence of salicylic acid on the in vitro release of anthralin from an o/w cream.","authors":"M Kneczke,&nbsp;C Rahm,&nbsp;L Landersjö","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>A diffusion cell with an artificial membrane (dialysis membrane) was used to study the in vitro release of antralin from an o/w cream (Locobase) in the presence of salicylic acid. The concentration range of antralin was 0.04-3.0%. The influence of salicylic acid on the in vitro release was studied by adding 0.5-3.0% salicylic acid to the creams. Addition of salicylic acid improves the solubility of anthralin in water and probably also in the aqueous phase of the cream. It may also have an effect on the microviscosity of the cream as the structure of the cream changes. Both these factors promoted the in vitro release of antralin. There was also an improvement in clinical efficacy when salicylic acid was added. In this case, the results also can be explained by an isolated effect on the permeability of the stratum corneum.</p>","PeriodicalId":7082,"journal":{"name":"Acta pharmaceutica Nordica","volume":"2 5","pages":"313-8"},"PeriodicalIF":0.0,"publicationDate":"1990-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"13238490","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}
引用次数: 0
The anti-inflammatory activity of 5H-dibenz[c,e]azepine-5,7(6H)dione, 6,7-dihydro-5H-dibenz[c,e]azepine, N-benzoylbenzamide and 1H-benz[d,e]isoquinoline-1,3(2H)dione derivatives in rodents. 5h -二苯并[c,e]氮平-5,7(6H)二酮、6,7-二氢- 5h -二苯并[c,e]氮平、n -苯甲酰苯酰胺和1h -苯并[d,e]异喹啉-1,3(2H)二酮衍生物对啮齿动物的抗炎活性。
Acta pharmaceutica Nordica Pub Date : 1990-01-01
I H Hall, R Simlot, C B Oswald, A R Murthy, H elSourady, J M Chapman
{"title":"The anti-inflammatory activity of 5H-dibenz[c,e]azepine-5,7(6H)dione, 6,7-dihydro-5H-dibenz[c,e]azepine, N-benzoylbenzamide and 1H-benz[d,e]isoquinoline-1,3(2H)dione derivatives in rodents.","authors":"I H Hall,&nbsp;R Simlot,&nbsp;C B Oswald,&nbsp;A R Murthy,&nbsp;H elSourady,&nbsp;J M Chapman","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>A series of N-substituted 5H-dibenz[c,e]azepin-5,7(6H)dione, 6-substituted 6,7-dihydro-5H-dibenz[c,e]azepine, 1H-benz[d,e]isoquinoline-1,3(2H)dione and N-benzoyl derivatives was shown to have anti-inflammatory and local analgesic activity in rodents. 6-(4-Chlorophenyl)-5H-dibenz[c,e]azepin-5,7(6H)dione demonstrated greater than 50% inhibition of induced edema and the writhing reflex at 25 mg/kg, I.P. in mice. 6-Methyl-6,7-dihydro-5H-dibenz[c,e]azepine and the N-butyl and N-pentyl derivatives of the dibenz-[c,e]azepine and N-benzoylbenzamide series demonstrated potent activity in both screens. The 1H-benz[d,e]isoquinoline-1,3(2H)diones were generally less active than the other three chemical classes of agents tested. However, the 2-(methylthio)ethyl derivative of this series demonstrates good activity in both screens. These agents appeared to be as potent as the standards, indomethacin and phenylbutazone, as anti-inflammatory agents in these animal models. Selected agents, e.g. 6-(4-methylphenyl)-5H-dibenz[c,e]azepin-5,7(6H)dione demonstrated anti-arthritic and anti-gout activities in rodents. The N-methyl and N-butyl derivatives of 6,7-dihydro-5H-dibenz[c,e]azepine afforded good anti-pleurisy activity in rats at 25 mg/kg x 2. The agents which demonstrated potent anti-inflammatory action were found to inhibit acid lysosomal hydrolytic enzyme activities in mouse liver and macrophages at 10(-5) M concentrations. Trypsin, elastase and collagenase activities were also inhibited by the derivatives. Prostaglandin synthetase activity of bovine seminal vesicles and mouse macrophages was inhibited by the compounds at 10(-5) M concentrations.</p>","PeriodicalId":7082,"journal":{"name":"Acta pharmaceutica Nordica","volume":"2 6","pages":"387-400"},"PeriodicalIF":0.0,"publicationDate":"1990-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"13250973","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}
引用次数: 0
Electrostatic requirements for high benzodiazepine receptor affinity among betacarboline-3-carboxylic acid derivatives. β -3-羧酸衍生物中苯二氮卓类受体高亲和力的静电要求。
Acta pharmaceutica Nordica Pub Date : 1990-01-01
J Gynther, H Konschin, H Tylli, J Rouvinen
{"title":"Electrostatic requirements for high benzodiazepine receptor affinity among betacarboline-3-carboxylic acid derivatives.","authors":"J Gynther,&nbsp;H Konschin,&nbsp;H Tylli,&nbsp;J Rouvinen","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Electrostatic requirements for high benzodiazepine receptor affinity among C3-substituted betacarbolines have been discussed on the basis of theoretical calculations employing ab initio quantum chemical methods. The molecular electrostatic potentials (MEPs) were evaluated in the plane of the tricyclic ring and at the distance of 160 pm perpendicular to the plane. In the ring plane three distinct minima were found, one in the A-ring and the other two at the nitrogens, for all BCs studied. One or two strong negative areas are also associated with the C3-substituent (COOH, COOR or CN). At the distance of 160 pm a large MEP minimum was found near N2 and the substituent at C3. Lack of either or both of these regions yields a dramatic decrease in their BZ-receptor binding affinity. The electrostatic potential characteristics of the title compounds has led us to suggest an MEP pharmacophore for BCs.</p>","PeriodicalId":7082,"journal":{"name":"Acta pharmaceutica Nordica","volume":"2 1","pages":"45-52"},"PeriodicalIF":0.0,"publicationDate":"1990-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"13314273","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}
引用次数: 0
Racemates and enantiomers in drug research and development--introductory remarks. 药物研究与开发中的外消旋体和对映体——导言。
Acta pharmaceutica Nordica Pub Date : 1990-01-01
L Dalgaard
{"title":"Racemates and enantiomers in drug research and development--introductory remarks.","authors":"L Dalgaard","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":7082,"journal":{"name":"Acta pharmaceutica Nordica","volume":"2 3","pages":"131-6"},"PeriodicalIF":0.0,"publicationDate":"1990-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"13352599","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}
引用次数: 0
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