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Journal de pharmacologie最新文献

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[Flavonoids extracted from Ribes nigrum L. and Alchemilla vulgaris L.: 1. In vitro inhibitory activities on elastase, trypsin and chymotrypsin. 2. Angioprotective activities compared in vivo]. 黄酮类化合物的提取[j];对弹性酶、胰蛋白酶和凝乳胰蛋白酶的体外抑制活性。2. 体内血管保护活性比较[j]。
Journal de pharmacologie Pub Date : 1986-01-01
M Jonadet, M T Meunier, F Villie, J P Bastide, J L Lamaison
{"title":"[Flavonoids extracted from Ribes nigrum L. and Alchemilla vulgaris L.: 1. In vitro inhibitory activities on elastase, trypsin and chymotrypsin. 2. Angioprotective activities compared in vivo].","authors":"M Jonadet,&nbsp;M T Meunier,&nbsp;F Villie,&nbsp;J P Bastide,&nbsp;J L Lamaison","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>In vitro experiments were conducted on the inhibitory properties of extracts from Ribes nigrum L. and Alchemilla vulgaris L. (fractions A1 + A2, A1, A2) on activity of the proteolytic enzymes elastase, trypsin and alpha-chymotrypsin. Extracts from Ribes Nigrum L. and Alchemilla Vulgaris L. (Fraction A1) inhibited 50% of the activity of porcine pancreas elastase at concentrations of 0.56 mg/ml and 0.16 mg/ml, respectively, against a synthetic substrate. Inhibition was less effective on activity of trypsin and alpha-chymotrypsin. Marked in vivo angioprotective properties were shown by the compounds studied, except Fraction A2 of Alchemilla vulgaris L. which had no significant activity. The results suggest a possible role by these inhibitors in the protection of conjunctive and elastic tissues adversely affected by proteolytic enzymes. An additional advantage is their lack of toxicity.</p>","PeriodicalId":14817,"journal":{"name":"Journal de pharmacologie","volume":"17 1","pages":"21-7"},"PeriodicalIF":0.0,"publicationDate":"1986-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14755536","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
Specific binding of 3H-nicergoline in rat brain: comparison with the selective alpha 1-antagonist 3H-prazosin. 3h -尼克麦角啉在大鼠脑中的特异性结合:与选择性α - 1拮抗剂3h -吡唑嗪的比较。
Journal de pharmacologie Pub Date : 1986-01-01
L Diop, J P Dausse
{"title":"Specific binding of 3H-nicergoline in rat brain: comparison with the selective alpha 1-antagonist 3H-prazosin.","authors":"L Diop,&nbsp;J P Dausse","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>In rat cerebral cortex, the 3H-Nicergoline (an ergot alkaloid derivative) binding was rapid, reversible, saturable and of high affinity. In various structures of the central nervous system except midbrain and cerebellum, the maximum binding capacity (B max) for 3H-Nicergoline is greater that for 3H-Prazosin. The specificity studies of 3H-Nicergoline binding show interactions with alpha 1-adrenergic and serotoninergic receptors. These results are confirmed after irreversible blockade with phenoxybenzamine. In conclusion, as nicergoline is known to cross the blood-brain barrier, this study shows that it exerts its central action on alpha 1-adrenoceptors as well as serotoninergic receptors.</p>","PeriodicalId":14817,"journal":{"name":"Journal de pharmacologie","volume":"17 1","pages":"65-74"},"PeriodicalIF":0.0,"publicationDate":"1986-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14831885","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
[A unique psychopharmacologic profile of adrafinil in mice]. [阿非尼在小鼠体内独特的精神药理学特征]。
Journal de pharmacologie Pub Date : 1986-01-01
F A Rambert, J Pessonnier, J E de Sereville, A M Pointeau, J Duteil
{"title":"[A unique psychopharmacologic profile of adrafinil in mice].","authors":"F A Rambert,&nbsp;J Pessonnier,&nbsp;J E de Sereville,&nbsp;A M Pointeau,&nbsp;J Duteil","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The following psychopharmacological effects of adrafinil have been observed in mice: increase in locomotor activity (64-256 mg.kg-1), antagonism (16-128 mg.kg-1) of the hypnotic effects of barbitone but not of pentobarbitone, reduction of immobility duration in the forced swimming test (16-256 mg.kg-1); slight antagonism (256 mg.kg-1) of electroshock-induced convulsions; no modification of rectal temperature; no stereotyped or climbing behaviour; no increase in lethality in aggregated mice (LD50 isolated = 1022 mg.kg-1, LD50 aggregated = 859 mg.kg-1); lack of effects on the provisional tests for antidepressants: no interaction with reserpine-, oxotremorine-, or apomorphine-induced hypothermia but potentiation of yohimbine-induced toxicity; lack of peripheral sympathetic effects (no mydriasis, no salivation, no contraction of the pilomotor muscles, no antagonism of reserpine-induced ptosis); lack of peripheral anticholinergic effects (no mydriasis, no antagonism of oxotremorine-induced salivation or lacrimation). As compared to no analeptic, anticholinergic or antidepressant drugs, adrafinil shows a unique behavioural profile in mice defined on the one hand by a specific stimulant activity associated with antidepressant-like effects that do no seem related to a beta-adrenergic mechanism and on the other hand by a lack of dopaminergic effects. Most adrafinil-induced effects (increase in locomotor activity, reduction of immobility duration in the forced swimming test) may correspond to a central alpha 1-adrenergic stimulation, but the unexpected lack of peripheral sympathetic effects remains unexplained.</p>","PeriodicalId":14817,"journal":{"name":"Journal de pharmacologie","volume":"17 1","pages":"37-52"},"PeriodicalIF":0.0,"publicationDate":"1986-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14831882","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
[Determination of optimal posology for hypnotic and anxiolytic agents]. [确定催眠和抗焦虑药物的最佳效价]。
Journal de pharmacologie Pub Date : 1986-01-01
J F Dreyfus, J Puech, P Simon, J P Boulenger, J P Couzinier, M Garreau, J D Guelfi, J Y Guichoux, S Hecquet, G Lefur
{"title":"[Determination of optimal posology for hypnotic and anxiolytic agents].","authors":"J F Dreyfus,&nbsp;J Puech,&nbsp;P Simon,&nbsp;J P Boulenger,&nbsp;J P Couzinier,&nbsp;M Garreau,&nbsp;J D Guelfi,&nbsp;J Y Guichoux,&nbsp;S Hecquet,&nbsp;G Lefur","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":14817,"journal":{"name":"Journal de pharmacologie","volume":"17 Suppl 1 ","pages":"19-24"},"PeriodicalIF":0.0,"publicationDate":"1986-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14011804","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 effects of nicergoline on the heart rate in the normotensive or spontaneously hypertensive rat. Possible participation of central alpha-1 receptors]. 尼麦角林对正常血压或自发性高血压大鼠心率的影响。中枢α -1受体的可能参与]。
Journal de pharmacologie Pub Date : 1986-01-01
A M Huchet, H Schmitt
{"title":"[The effects of nicergoline on the heart rate in the normotensive or spontaneously hypertensive rat. Possible participation of central alpha-1 receptors].","authors":"A M Huchet,&nbsp;H Schmitt","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The cardiovascular effects of nicergoline, a preferential alpha 1-adrenoceptor blocking drug, were studied in anaesthetized normotensive or spontaneously hypertensive (SH) rats. Nicergoline (300 micrograms/kg, i.v.) significantly reduced blood pressure and heart rate in control, bivagotomized or beta-blocked normotensive or SH rats. In bilaterally vagotomized and beta-blocked rats, nicergoline reduced mean blood pressure but did no longer modify heart rate. Thus, it is postulated that nicergoline could reduce the sympathetic tone and increase the vagal nerve activity, possibly by inhibiting central alpha 1-adrenoceptors. The nicergoline--induced bradycardia was greater in bivagotomized SHR than in normotensive ones. Intracerebroventricular injections of nicergoline (30 micrograms/kg) did not modify heart rate in normotensive control, bivagotomized or beta-blocked rats. On the contrary, nicergoline (30 micrograms/kg) injected into the cisterna magna induced a significant bradycardia in the three groups of normotensive rats. Blood pressure was reduced in the same way in all groups centrally treated by nicergoline. In conclusion, it seems that nicergoline reduces blood pressure by peripheral alpha-adrenoceptor blockade and modulates the autonomic nervous activity by inhibiting alpha 1-adrenoceptors mainly localized in the brainstem.</p>","PeriodicalId":14817,"journal":{"name":"Journal de pharmacologie","volume":"17 1","pages":"53-9"},"PeriodicalIF":0.0,"publicationDate":"1986-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14145565","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
Trophic role of the sympathetic innervation. 交感神经支配的营养作用。
Journal de pharmacologie Pub Date : 1986-01-01
I Azevedo, W Osswald
{"title":"Trophic role of the sympathetic innervation.","authors":"I Azevedo,&nbsp;W Osswald","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":14817,"journal":{"name":"Journal de pharmacologie","volume":"17 Suppl 2 ","pages":"30-43"},"PeriodicalIF":0.0,"publicationDate":"1986-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14938901","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
Simultaneous modeling of pharmacodynamics and pharmacokinetics. 同时建立药效学和药代动力学模型。
Journal de pharmacologie Pub Date : 1986-01-01
R L Galeazzi
{"title":"Simultaneous modeling of pharmacodynamics and pharmacokinetics.","authors":"R L Galeazzi","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":14817,"journal":{"name":"Journal de pharmacologie","volume":"17 Suppl 1 ","pages":"63-70"},"PeriodicalIF":0.0,"publicationDate":"1986-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14866178","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
Pharmacokinetics of daunorubicinol in the rabbit: comparison with daunorubicin. 柔红霉素与柔红霉素在家兔体内的药动学比较。
Journal de pharmacologie Pub Date : 1986-01-01
D M Maniez-Devos, R Baurain, A Trouet, M Lesne
{"title":"Pharmacokinetics of daunorubicinol in the rabbit: comparison with daunorubicin.","authors":"D M Maniez-Devos,&nbsp;R Baurain,&nbsp;A Trouet,&nbsp;M Lesne","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The pharmacokinetics of daunorubicinol (DOL), the main metabolite of daunorubicin (DNR), was studied in rabbits and compared to that of daunorubicin after an 8 mg/kg dose. High-performance liquid chromatography was used to separate parent drug and metabolites. The plasma disappearance of DNR and DOL was triexponential. DOL was the major species detected in plasma and urine. Both drugs had large volumes of distribution. About 70% of DNR or DOL were bound to plasma proteins and mainly to albumin. Pharmacokinetic parameters of DOL obtained after injection of DOL were different from those calculated for DNR and those calculated for DOL after injection of DNR. The total urinary excretions of DNR or DOL were similar and amounted to 25% of the dose. No conjugates were identified in urine after enzymatic treatment. No fluorescent drug was identified in the feces. Anthracyclines were degraded in vitro in rabbit feces. The rabbit seems to be a good model for the study of anthracycline pharmacokinetics as our results in rabbits after DNR injection were similar to those in human studies.</p>","PeriodicalId":14817,"journal":{"name":"Journal de pharmacologie","volume":"17 1","pages":"14-20"},"PeriodicalIF":0.0,"publicationDate":"1986-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14831880","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
[Information systems for phase III and IV clinical trials]. [III期和IV期临床试验的信息系统]。
Journal de pharmacologie Pub Date : 1986-01-01
Y Alamercery, Begaud, Chastang, Derzko, Y Dupuis, R Gomeni, L Go, Lemarie, Mery, Wartelle
{"title":"[Information systems for phase III and IV clinical trials].","authors":"Y Alamercery,&nbsp;Begaud,&nbsp;Chastang,&nbsp;Derzko,&nbsp;Y Dupuis,&nbsp;R Gomeni,&nbsp;L Go,&nbsp;Lemarie,&nbsp;Mery,&nbsp;Wartelle","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":14817,"journal":{"name":"Journal de pharmacologie","volume":"17 Suppl 1 ","pages":"12-8"},"PeriodicalIF":0.0,"publicationDate":"1986-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14866171","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
[Monoclonal antibodies in diagnosis and therapy]. 【单克隆抗体在诊断和治疗中的应用】。
Journal de pharmacologie Pub Date : 1986-01-01
M Delaage
{"title":"[Monoclonal antibodies in diagnosis and therapy].","authors":"M Delaage","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The discovery of monoclonal antibodies has brought about a revolution in diagnostic and therapeutic. New antigens have been discovered on cell surfaces allowing the fine classification of cell lineages. Leukemia cells and tumors can now be characterized accurately. Regarding in vitro diagnostics monoclonal antibodies have allowed uniform standardization and a rational approach to hormone polymorphism. Monoclonal antibodies are now tested as pharmacological drugs. They have proved their use in the prevention and cure of rejection in bone marrow and kidney transplantation.</p>","PeriodicalId":14817,"journal":{"name":"Journal de pharmacologie","volume":"17 Suppl 2 ","pages":"59-64"},"PeriodicalIF":0.0,"publicationDate":"1986-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14938902","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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