Pharmacy and Pharmacology Communications最新文献_第9页

Effects of 3-alkylamino-7-chloro-4H-pyrido[2,3-e]-1,2,4-thiadiazine 1,1-dioxides on smooth muscle contractile activity 3-烷基胺-7-氯- 4h -吡啶[2,3-e]-1,2,4-噻二嗪1,1-二氧化物对平滑肌收缩活性的影响

Pharmacy and Pharmacology Communications Pub Date : 2000-02-01 DOI: 10.1211/146080800128735700

R. Ouedraogo, J. Fontaine, M. Antoine, B. Pirotte, P. Lebrun

引用次数: 3

1,2,3,4,5,6‐Hexahydrobenzo[h][1,6]naphthyridin‐5‐ones: 5‐HT7 Receptor Affinity

Pharmacy and Pharmacology Communications Pub Date : 2000-02-01 DOI: 10.1211/146080800128735656

A. Hinschberger, Alain-Claude Gillard, F. Dauphin, S. Rault

引用次数: 4

Synthesis and biological effects of new 3-alkylamino-4H-1,2,4-benzothiadiazine 1,1-dioxides on insulin-secreting cells 新型3-烷基氨基- 4h -1,2,4-苯并噻嗪1,1-二氧化物的合成及其对胰岛素分泌细胞的生物学效应

Pharmacy and Pharmacology Communications Pub Date : 2000-02-01 DOI: 10.1211/096089296765556980

F. Somers, P. Tullio, S. Boverie, J. Dogné, X. Leval, M. Antoine, P. Lebrun, B. Pirotte

引用次数: 2

Relationship Between the 5‐HT3 Receptor Pharmacophore and the Conformations of 5‐Hydroxytryptamine 5‐HT3受体药效团与5‐羟色胺构象的关系

Pharmacy and Pharmacology Communications Pub Date : 2000-02-01 DOI: 10.1211/146080800128735665

C. Daveu, R. Bureau, S. Rault

引用次数: 0

Pharmacomodulation Studies of Torasemide Leading to Original Non‐carboxylic Thromboxane A2 Receptor Antagonists 托拉塞米导致原始非羧基血栓素A2受体拮抗剂的药物调节研究

Pharmacy and Pharmacology Communications Pub Date : 2000-02-01 DOI: 10.1211/146080800128735674

J. Dogné, X. Leval, P. Neven, S. Rolin, J. Wouters, J. Delarge, B. Masereel

{"title":"Pharmacomodulation Studies of Torasemide Leading to Original Non‐carboxylic Thromboxane A2 Receptor Antagonists","authors":"J. Dogné, X. Leval, P. Neven, S. Rolin, J. Wouters, J. Delarge, B. Masereel","doi":"10.1211/146080800128735674","DOIUrl":"https://doi.org/10.1211/146080800128735674","url":null,"abstract":"Because torasemide, a loop diuretic, dose-dependently relaxes canine coronary artery precontracted with thromboxane A2 (TxA2), a series of pyridine derivatives have been investigated with the aim of developing original TxA2 receptor antagonists. \u0000 \u0000 \u0000 \u0000A binding test showed the affinity (IC50; the dose reducing binding by 50%) of one sulphonylurea derivative (BM 27) and two sulphonylcyanoguanidine derivatives (BM 114 and BM 115) for the TxA2 receptor of washed platelets from man were 161, 1. 75 and 0.54 μM, respectively. The IC50 of torasemide was only 2.69 μM. Their antagonism was confirmed by the capacity of the compounds to prevent the aggregation of platelets, from man, induced by arachidonic acid, the biological precursor of TxA2 (IC50: BM 114, 29.3 μM; BM 115, 12.0 μM; BM 27, 234 μM; torasemide, 350 μM; sulotroban, 12.3 μM). Similar results were obtained with the best compound BM 115 (IC50 11.5 μM) when U-46619, a stable TxA2 agonist, was used as the aggregating agent. \u0000 \u0000 \u0000 \u0000This molecule can be regarded as a template for the design of novel non-carboxylic TxA2 receptor antagonists.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":"10 1","pages":"77-82"},"PeriodicalIF":0.0,"publicationDate":"2000-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78283401","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 optimum length and width for a spacer device 间隔装置的最佳长度和宽度

Pharmacy and Pharmacology Communications Pub Date : 2000-01-01 DOI: 10.1211/146080800128735395

P. Barry, C. O’Callaghan

{"title":"The optimum length and width for a spacer device","authors":"P. Barry, C. O’Callaghan","doi":"10.1211/146080800128735395","DOIUrl":"https://doi.org/10.1211/146080800128735395","url":null,"abstract":"The aim of this study was to determine the delivery of two different drugs from spacer devices of different lengths and diameter. Spacer devices were prepared from lengths of plastic tubing of length 5, 10, 20, 50 and 100 cm, and diameter 30, 50 and 100 mm. Metered dose inhalers of sodium cromoglycate and budesonide were actuated into the spacers and drug output and particle size were measured using a glass multistage liquid impinger. To determine the effect of delay on the recovery of drug from the spacers, budesonide was actuated into spacers and output measured after a delay of 5, 10 or 20 s. For both drugs, increasing spacer length up to 20 cm increased drug recovery. There was no further increase or reduction with longer spacers. Increasing spacer diameter also increased drug recovery, although the increase was greater for sodium cromoglycate than budesonide. Budesonide delivery was greatest for spacers with a volume of 300 mL or greater, whereas maximum sodium cromoglycate delivery was from spacers with a volume of 1000 mL or greater. Drug half-life was also longer in larger spacers, being 6 s in a 10 cm length spacer (196 mL volume) and 15 s in a 20 cm length spacer (392 mL volume). The optimum spacer size was different for the two drugs. Sodium cromoglycate is best delivered from a larger spacer than budesonide. Conclusions from studies with one drug and spacer combination cannot be applied to another.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":"1 1","pages":"1-5"},"PeriodicalIF":0.0,"publicationDate":"2000-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73723775","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: 6

SYNTHESIS AND ANTICONVULSANT ACTIVITY OF 5-ARYL-1,3,4-THIADIAZOLE DERIVATIVES 5-芳基-1,3,4-噻二唑衍生物的合成及其抗惊厥活性

Pharmacy and Pharmacology Communications Pub Date : 2000-01-01 DOI: 10.1211/146080800128735430

A. Foroumadi, S. Tabatabai, G. Gitinezhad, M. Zarrindast, A. Shafiee

引用次数: 13

Crystallinity of Omeprazole in Various Film Polymers 奥美拉唑在各种薄膜聚合物中的结晶度

Pharmacy and Pharmacology Communications Pub Date : 2000-01-01 DOI: 10.1211/146080800128735403

N. Sarisuta, M. Kumpugdee

引用次数: 2

First Synthesis of N-(4-Fluorophenyl)-5-(4-fluorophenyl)-2-(4-hydroxybenzyl)pentanamide, a New Potential Cholesterol Absorption Inhibitor 新型潜在胆固醇吸收抑制剂N-(4-氟苯基)-5-(4-氟苯基)-2-(4-羟基苯基)五胺的首次合成

Pharmacy and Pharmacology Communications Pub Date : 2000-01-01 DOI: 10.1111/J.2042-7158.2000.TB00212.X

J. Guillon, S. Stiebing, M. Robba

引用次数: 1

Leptin Improves Insulin Sensitivity of Skeletal Muscle in Obese‐diabetic ob/ob Mice 瘦素改善肥胖糖尿病小鼠骨骼肌胰岛素敏感性

Pharmacy and Pharmacology Communications Pub Date : 2000-01-01 DOI: 10.1211/146080800128735449

C. Bailey, S. Bates, S. L. Turner, M. Rossi, I. Morgan, S. Bloom

引用次数: 2