Pharmacy and Pharmacology Communications最新文献_第6页

In-vivo Modulation of Gastrointestinal Motility by Cannabinoid Drugs 大麻素类药物对胃肠运动的体内调节

Pharmacy and Pharmacology Communications Pub Date : 2000-06-01 DOI: 10.1211/146080800128736033

A. Izzo, Domenico Addeo, M. Amato, F. Borrelli, R. Capasso, G. Carlo, Emilia Nocerino, N. Mascolo, L. Pinto, F. Capasso

引用次数: 2

Rat Cognitive Functions During and After Treatment with the Cannabinoid Agonist, HU 210 大麻素激动剂治疗前后大鼠的认知功能，HU 210

Pharmacy and Pharmacology Communications Pub Date : 2000-06-01 DOI: 10.1211/146080800128736015

A. Ottani, D. Giuliani, F. Ferrari

引用次数: 1

Medical Uses and Toxicological Profile of Cannabis 大麻的医疗用途和毒理学概况

Pharmacy and Pharmacology Communications Pub Date : 2000-06-01 DOI: 10.1211/146080800128735999

N. Mascolo

引用次数: 0

Endocannabinoids and Peripheral Pain 内源性大麻素与外周性疼痛

Pharmacy and Pharmacology Communications Pub Date : 2000-06-01 DOI: 10.1211/146080800128736042

G. L. Rana, Roberta Maria Lobello, D. Piomelli, A. Calignano

引用次数: 0

Nitric Oxide Accounts for Endothelium‐dependent Relaxation of Pig Coronary Artery in Response to Noradrenaline 去甲肾上腺素对猪冠状动脉内皮依赖性松弛的影响

Pharmacy and Pharmacology Communications Pub Date : 2000-05-01 DOI: 10.1211/146080800128735881

F. Yamaki, Hikaru Tanaka, K. Shigenobu, Yoshio Tanaka

{"title":"Nitric Oxide Accounts for Endothelium‐dependent Relaxation of Pig Coronary Artery in Response to Noradrenaline","authors":"F. Yamaki, Hikaru Tanaka, K. Shigenobu, Yoshio Tanaka","doi":"10.1211/146080800128735881","DOIUrl":"https://doi.org/10.1211/146080800128735881","url":null,"abstract":"Vasorelaxant substances responsible for endothelium-dependent relaxation of pig coronary artery in response to noradrenaline have been investigated pharmacologically. Noradrenaline relaxed pig coronary artery in an endothelium- and concentration-dependent way in the presence of prazosin (10−6 M) and propranolol (3 times 10−6 M), to block α1- and β-adrenoceptors in smooth muscle cells. Prazosin- and propranolol-resistant endothelium-dependent relaxation of the coronary artery to noradrenaline was greatly attenuated by the NO synthase inhibitor, NG-nitro-L-arginine methyl ester (L-NAME) (10−4 M) and the soluble guanylate cyclase inhibitor (1H-[1,2,4]-oxadiazolo-[4,3-a]-quinoxalin-1-one, ODQ; 10−5 M). Noradrenaline-induced endothelium-dependent coronary relaxation in the presence of prazosin and propranolol was almost abolished by rauwolscine (3 times 10−6 M), a selective α2-adrenoceptor antagonist. These findings suggest that noradrenaline-induced endothelium-dependent relaxation of pig coronary artery is largely mediated by release of endothelium-derived NO as a consequence of the stimulation of endothelial α2-adrenoceptors.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":"122 1","pages":"195-199"},"PeriodicalIF":0.0,"publicationDate":"2000-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77712450","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: 1

Reduced Effects of Isoprenaline on the Membrane Potential of Aortic Smooth Muscle from Rats Pre‐ and During Hypertension 异丙肾上腺素对高血压前期和高血压期间大鼠主动脉平滑肌膜电位的影响

Pharmacy and Pharmacology Communications Pub Date : 2000-05-01 DOI: 10.1211/146080800128735908

Ying-Yu Chen, S. Doggrell

引用次数: 0

Oral Delivery of Proteins: Effect of Chicken and Duck Ovomucoid on the Stability of Insulin in the Presence of α‐Chymotrypsin and Trypsin 蛋白质口服:在α‐凝乳胰蛋白酶和胰蛋白酶存在下，鸡和鸭卵泡样液对胰岛素稳定性的影响

Pharmacy and Pharmacology Communications Pub Date : 2000-05-01 DOI: 10.1211/146080800128735935

V. Agarwal, I. Reddy, M. Khan

{"title":"Oral Delivery of Proteins: Effect of Chicken and Duck Ovomucoid on the Stability of Insulin in the Presence of α‐Chymotrypsin and Trypsin","authors":"V. Agarwal, I. Reddy, M. Khan","doi":"10.1211/146080800128735935","DOIUrl":"https://doi.org/10.1211/146080800128735935","url":null,"abstract":"The in-vitro stability of insulin in the presence of α-chymotrypsin and trypsin has been evaluated in the presence of different concentrations of chicken and duck ovomucoid (CkOVM and DkOVM), a new class of enzyme inhibitor derived from the egg white of avian species. The inhibitory effect was compared with that of aprotinin. The effectiveness of DkOVM was also determined in the presence of agents that accelerate α-chymotrypsin-mediated degradation of insulin in solution by deaggregation. \u0000 \u0000 \u0000 \u0000Insulin solutions (18μM) were incubated at 37°C with 0.1 μM chymotrypsin and 0.5 μM trypsin in lOOmM Tris buffer containing 1 mM calcium chloride and different concentrations of CkOVM and DkOVM. Samples were treated with cold Tris containing 1% (v/v) trifluoroacetic acid to stop the enzyme action and analysed by reversed-phase high-performance liquid chromatography. Similar studies were performed with aprotinin, EDTA (0.05 mM) and sodium glycocholate (30mM) in the presence of α-chymotrypsin and DkOVM. DkOVM was effective against α-chymotrypsin-mediated degradation of insulin at enzyme-to-inhibitor ratios of 1:0–5, 1:1 and 1:2. CkOVM was ineffective against α-chymotrypsin even at an enzyme-to-inhibitor ratio of 1:4. In contrast, both DkOVM and CkOVM were completely effective against trypsin-mediated degradation of insulin at an enzyme-to-inhibitor ratio of 1:1. This effect was comparable with that of aprotinin at an enzyme-to-inhibitor ratio of 1:1. Inhibition of the enzyme was reduced in the presence of sodium glycocholate and EDTA. \u0000 \u0000 \u0000 \u0000DkOVM effectively stabilized insulin against degradation for a study period of 1 h in the presence of α-chymotrypsin and trypsin. Because insulin is extensively degraded by α-chymotrypsin, DkOVM might be used to enhance the oral delivery of insulin.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":"32 1","pages":"223-227"},"PeriodicalIF":0.0,"publicationDate":"2000-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79228694","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: 30

Resveratrol Activates Membrane‐bound Guanylate Cyclase in PC12 Cells 白藜芦醇激活PC12细胞膜结合鸟苷酸环化酶

Pharmacy and Pharmacology Communications Pub Date : 2000-05-01 DOI: 10.1211/146080800128735917

Zi‐Jiang Chen, D. Che, Chung‐ho Chang

引用次数: 3

Synthesis and Activity of Fluorinated Derivatives of Sulindac Sulphide and Sulindac Sulphone 磺胺酸和磺胺酸氟化衍生物的合成及活性研究

Pharmacy and Pharmacology Communications Pub Date : 2000-05-01 DOI: 10.1211/146080800128735926

M. Jung, A. Wahl, W. Neupert, G. Geisslinger, P. Senter

{"title":"Synthesis and Activity of Fluorinated Derivatives of Sulindac Sulphide and Sulindac Sulphone","authors":"M. Jung, A. Wahl, W. Neupert, G. Geisslinger, P. Senter","doi":"10.1211/146080800128735926","DOIUrl":"https://doi.org/10.1211/146080800128735926","url":null,"abstract":"The synthesis of fluorinated derivatives of the sulphide and sulphone metabolites of sulindac, a non-steroidal anti-inflammatory agent with chemopreventative activity, is reported. \u0000 \u0000 \u0000 \u0000The key step in the synthesis is a Pummerer-rearrangement of the parent sulindac sulphoxide using (diethylamino)sulphur trifluoride as an activating agent and as a source of the fluoride nucleophile. The reaction leads to the formation of the 4-fluoromethylthio and 4-fluoromethylsulphonyl derivatives of sulindac (4a and 4b, respectively). Sulindac sulphide is 2.5 times more potent as a COX-1 inhibitor compared with its fluorinated counterpart 4a. The sulphones were inactive as COX-1 inhibitors, and none of the compounds inhibited COX-2 concentrations up to 0.1 mM. Cytotoxicity assays showed that 4a and 4b were as cytotoxic as sulindac sulphide and sulindac sulphone on 3719 colorectal carcinoma cell lines. Compound 4b was the most potent compound on RCA cells with an IC50 of 95 μM (sulindac sulphide 140μM, sulindac sulphone 175 μM). \u0000 \u0000 \u0000 \u0000Fluorinated sulindac derivatives warrant further investigation since we have shown that cytotoxic activity can be retained or even increased independently from COX-inhibitory properties. This could help minimize the undesired side-effects associated with chronic sulindac administration.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":"1 1","pages":"217-221"},"PeriodicalIF":0.0,"publicationDate":"2000-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83167017","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: 5

Protective Effects of Glucocorticoids on Nitric Oxide-induced Apoptosis in Leukaemia HL-60 Cells in Man 糖皮质激素对一氧化氮诱导人白血病HL-60细胞凋亡的保护作用

Pharmacy and Pharmacology Communications Pub Date : 2000-05-01 DOI: 10.1211/146080800128735872

H. Pae, Yoo-hyun Kim, Y. Shin, Jae-Heon Yang, J. Eun, Hun-taeg Chung

{"title":"Protective Effects of Glucocorticoids on Nitric Oxide-induced Apoptosis in Leukaemia HL-60 Cells in Man","authors":"H. Pae, Yoo-hyun Kim, Y. Shin, Jae-Heon Yang, J. Eun, Hun-taeg Chung","doi":"10.1211/146080800128735872","DOIUrl":"https://doi.org/10.1211/146080800128735872","url":null,"abstract":"Inappropriate release of nitric oxide (NO) has been linked to the pathogenesis of several disease states. Glucocorticoids inhibit the synthesis of NO and could be effective in the treatment of NO-mediated diseases. We show the protective effect of dexamethasone on NO-induced apoptosis in leukaemia HL-60 cells in man. Agarose electrophoresis of the DNA extracted from HL-60 cells resulted in a ladder-like pattern of fragmentation after 6-and 9-h exposure of the cells to 1 mM S-nitrosoglutathione, a physiologically relevant NO donor. Pre-incubation of the cells with 1 μM dexamethasone for 6 h blocked NO-induced DNA fragmentation. This effect was abolished by RU-486, a steroid receptor antagonist, and cycloheximide, a protein synthesis inhibitor, suggesting that the protective effect of dexamethasone might require glucocorticoid receptor binding and protein synthesis. Concerning NO signal transduction, we found that dexamethasone efficiently prevented NO-induced activation of caspase-3 proteases, suggesting an inhibitory mechanism upstream of the terminal death pathway. Collectively, these findings highlight a novel protective effect of dexamethasone on NO-mediated cellular injury.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":"11 1","pages":"191-194"},"PeriodicalIF":0.0,"publicationDate":"2000-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79393590","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