abstract：:Derivatization of phenothiazine (PTZ, 1) has been a commonly used method to develop drugs with various pharmacological properties. In the present study, a series of PTZ derivatives 1-11 were investigated on the inhibition of the cloned α7 subunit of the human nicotinic acetylcholine receptor (α7-nAChR) expressed in Xe...

journal_title：Pharmacological research

authors： Sadek B,Ashoor A,Al Mansouri A,Lorke DE,Nurulain SM,Petroianu G,Wainwright M,Oz M

更新日期：2012-09-01 00:00:00

abstract：:Endocannabinoids exhibit vasodilatory properties and reduce blood pressure in vivo. However, the influence and mechanism of action of the prominent endocannabinoid, anandamide (AEA), in pulmonary arteries are not known. The present study determined the vascular response to AEA in isolated rat pulmonary arteries. AEA r...

journal_title：Pharmacological research

authors： Baranowska-Kuczko M,MacLean MR,Kozłowska H,Malinowska B

更新日期：2012-09-01 00:00:00

abstract：:The understanding of signaling cascades involved in the induction, promotion, and progression of cancer, although advanced in recent years, is still incomplete. Tracing the imbalance of the impaired, physiologically-essential cellular signaling that drives the neoplastic process is a complex issue. This review discuss...

journal_title：Pharmacological research

authors： Al-Wadei HA,Ullah MF,Al-Wadei MH

更新日期：2012-07-01 00:00:00

abstract：:Moderate wine consumption has been shown to reduce cardiovascular (CV) risk, due to alcohol and polyphenolic compounds, such as resveratrol. We investigated the associations between total urinary resveratrol metabolites (TRMs) as biomarkers of wine and resveratrol consumption and CV risk factors in a large cross-secti...

journal_title：Pharmacological research

authors： Zamora-Ros R,Urpi-Sarda M,Lamuela-Raventós RM,Martínez-González MÁ,Salas-Salvadó J,Arós F,Fitó M,Lapetra J,Estruch R,Andres-Lacueva C,PREDIMED Study Investigators.

更新日期：2012-06-01 00:00:00

abstract：:Fatty-acid amide hydrolase (FAAH) catalyzes the intracellular hydrolysis of the endocannabinoid anandamide and other bioactive lipid amides. In the present study, we conducted a comparative characterization of the effects of the newly identified brain-impermeant FAAH inhibitor, URB937 ([3-(3-carbamoylphenyl)-4-hydroxy...

journal_title：Pharmacological research

authors： Sasso O,Bertorelli R,Bandiera T,Scarpelli R,Colombano G,Armirotti A,Moreno-Sanz G,Reggiani A,Piomelli D

更新日期：2012-05-01 00:00:00

abstract：:This review summarizes the metabolism, secretion, regulation and sites of action of melatonin. An updated description of the melatonin receptors, including their signal transduction mechanisms, distribution and characterization of receptor genes, is given. Special emphasis is focused on the clinical aspects and potent...

journal_title：Pharmacological research

authors： Carpentieri A,Díaz de Barboza G,Areco V,Peralta López M,Tolosa de Talamoni N

更新日期：2012-04-01 00:00:00

abstract：:Advanced glycation end products (AGEs) and their receptor (RAGE) axis contributes to diabetic nephropathy. An oral hypoglycemic agent, metformin may have a potential effect on the inhibition of glycation reactions. Further, since a pathophysiological crosstalk between renin-angiotensin system (RAS) and AGEs-RAGE axis ...

journal_title：Pharmacological research

authors： Ishibashi Y,Matsui T,Takeuchi M,Yamagishi S

更新日期：2012-03-01 00:00:00

abstract：:The effects of trans-resveratrol (RSV) combined with ethanol (EtOH) were evaluated by (31)P NMR on total ATP and sn-glycerol-3-phosphate (sn-G3P) contents measured in real time in isolated and perfused whole liver of the rat. Mitochondrial ATP turnover was assessed by using specific inhibitors of glycolytic and mitoch...

journal_title：Pharmacological research

authors： Gallis JL,Serhan N,Gin H,Couzigou P,Beauvieux MC

更新日期：2012-03-01 00:00:00

abstract：:Despite our insufficient understanding of the exact molecular mechanisms of general anesthetics and sedatives, every year millions of children are treated with these drugs in a seemingly safe manner. However, increasing evidence particularly from animal studies has suggested the possibility for deleterious effects in ...

journal_title：Pharmacological research

authors： Ward CG,Loepke AW

更新日期：2012-03-01 00:00:00

abstract：:The potential drug-to-drug interaction between darunavir and raltegravir in the setting of HIV infection is a highly debated issue still unresolved. In the present study we have evaluated the pharmacokinetics of darunavir and ritonavir in 53 HIV-1 infected patients with or without concomitant raltegravir administratio...

journal_title：Pharmacological research

authors： Cattaneo D,Gervasoni C,Cozzi V,Baldelli S,Fucile S,Meraviglia P,Landonio S,Boreggio G,Rizzardini G,Clementi E

更新日期：2012-02-01 00:00:00

abstract：:Treatment of pediatric diabetes can be challenging. Strict glucose control can be accompanied by hypoglycemia and weight gain. Recently, there have been many developments in insulin preparations and delivery methods which make insulin levels more close to a physiologic pattern. Newly developed rapid/long acting analog...

journal_title：Pharmacological research

authors： Kim J,Kim SM,Nguyen HC,Redondo MJ

更新日期：2012-01-01 00:00:00

abstract：:Recent studies have shown that a higher consumption of green tea leads to a lower prevalence of depressive symptoms in elderly individuals. However, no studies have explored the antidepressant-like effect of green tea in preclinical models of depression. The aim of this study was to investigate the antidepressant-like...

journal_title：Pharmacological research

authors： Zhu WL,Shi HS,Wei YM,Wang SJ,Sun CY,Ding ZB,Lu L

更新日期：2012-01-01 00:00:00

abstract：:The role of autophagy, a process in which the cell self-digests its own components, was investigated in glioma cell death induced by the hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase-inhibiting drug simvastatin. Induction of autophagy and activation of autophagy-regulating signalling pathways were analyzed by i...

journal_title：Pharmacological research

authors： Misirkic M,Janjetovic K,Vucicevic L,Tovilovic G,Ristic B,Vilimanovich U,Harhaji-Trajkovic L,Sumarac-Dumanovic M,Micic D,Bumbasirevic V,Trajkovic V

更新日期：2012-01-01 00:00:00

abstract：:In 1996, Dr. Costa was invited by Prof. Boris Astrachan, Chairman of the Department of Psychiatry at the University of Illinois at Chicago, to direct the research of the "Psychiatric Institute, Department of Psychiatry, School of Medicine, at the University of Illinois at Chicago." He was asked to develop a seminal re...

journal_title：Pharmacological research

authors： Guidotti A,Grayson DR

更新日期：2011-10-01 00:00:00

abstract：:The lack of availability of appropriate medicines for children is an extensive and well known problem. As a consequence off label or unlicensed administration of medicinal products in every day paediatric practice is frequent. A variety of obstacles hinder the development of paediatric indications for drugs primarily ...

journal_title：Pharmacological research

authors： Rocchi F,Tomasi P

更新日期：2011-09-01 00:00:00

abstract：BACKGROUND AND OBJECTIVES:Thymidylate synthase (TS) expression levels appear to be related to response to 5-fluorouracil-(5-FU)-based chemotherapy in colorectal cancer (CRC) patients. Three polymorphisms have been proposed as modulators of TS expression: a tandemly repeated sequence (2R/3R) in the 5' UTR, a SNP (G>C) w...

journal_title：Pharmacological research

authors： Vignoli M,Nobili S,Napoli C,Putignano AL,Morganti M,Papi L,Valanzano R,Cianchi F,Tonelli F,Mazzei T,Mini E,Genuardi M

更新日期：2011-09-01 00:00:00

abstract：:Green tea (Camellia sinensis, Theaceace) is the second most popular beverage in the world and has been extensively studied for its putative disease preventive effects. Green tea is characterized by the presence of a high concentrations of polyphenolic compounds known as catechins, with (-)-epigallocatechin-3-gallate (...

journal_title：Pharmacological research

authors： Sae-tan S,Grove KA,Lambert JD

更新日期：2011-08-01 00:00:00

abstract：:Green tea and its major polyphenols constituents, tea catechins, have been shown to have many health benefits including cancer prevention. Tea catechins and tea catechin metabolites/catabolites are bioavailable in the systemic circulation after oral intake of green tea or green tea catechins. The metabolites/catabolit...

journal_title：Pharmacological research

authors： Chow HH,Hakim IA

更新日期：2011-08-01 00:00:00

abstract：:Availability of highly active antiretroviral therapy has dramatically increased survival rates and substantially modified the course of HIV infection, which has now become a chronic disease both in adults and in children. Treatment strategies in paediatric patients have to face with specific challenges associated with...

journal_title：Pharmacological research

authors： Viganò A,Manfredini V,Penagini F,Giacomet V,Zuccotti GV

更新日期：2011-07-01 00:00:00

abstract：:Metastatic and primary bone cancers are usually accompanied by severe pain that is difficult to manage. In light of the adverse side effects of opioids, manipulation of the endocannabinoid system may provide an effective alternative for the treatment of cancer pain. The present study determined that a local, periphera...

journal_title：Pharmacological research

authors： Khasabova IA,Chandiramani A,Harding-Rose C,Simone DA,Seybold VS

更新日期：2011-07-01 00:00:00

abstract：:This article summarizes the discovery and the development of endothelial biology with a special focus on the role of endothelium-dependent vasoconstriction. The physician-scientist Paul Michel Vanhoutte contributed many of the initial observations that helped to understand and form the main concepts of modern vascular...

journal_title：Pharmacological research

authors： Barton M

更新日期：2011-06-01 00:00:00

abstract：:Despite the exploration of a large number of disparate drugs in animal models and clinical trials, no pharmacological intervention, with the exception of aggressive lipid lowering therapy has reduced late vein graft failure in man. The importance of devising more effective strategies is exemplified by the enormous eco...

journal_title：Pharmacological research

authors： Jeremy JY,Shukla N,Angelini GD,Wan S

更新日期：2011-06-01 00:00:00

abstract：:The review emphasizes the role of NGF, the most representative member of the neurotrophins family, in cardiac physiopathology with a particular focus on healing and sprouting processes occurring after tissue damage. Cardiac and circulating NGF levels dramatically increase following myocardial injury (MI). A very early...

journal_title：Pharmacological research

authors： Govoni S,Pascale A,Amadio M,Calvillo L,D'Elia E,Cereda C,Fantucci P,Ceroni M,Vanoli E

更新日期：2011-04-01 00:00:00

abstract：:Metastatic cancers account for more than 90% of cancer mortality. The metastasis of all cancers is critically mediated by enzymes that degrade extracellular matrix. Aggressive tumors are characterized by an imbalance between enzymes that degrade ECM and endogenous inhibitors of the enzymes. Matrix metalloproteinases (...

journal_title：Pharmacological research

authors： Lokeshwar BL

更新日期：2011-02-01 00:00:00

abstract：:Folic acid-conjugated albumin nanospheres (FA-AN) have been developed to provide an actively targetable drug delivery system for improved drug targeting of cancer cells with reduced side effects. The nanospheres were prepared by conjugating folic acid onto the surface of albumin nanospheres using 1-ethyl-3-(3-dimethyl...

journal_title：Pharmacological research

authors： Shen Z,Li Y,Kohama K,Oneill B,Bi J

更新日期：2011-01-01 00:00:00

abstract：:Novel therapeutic strategies are needed to address and to solve the emerging problem of hypoxia-induced resistance to anticancer drugs. N-(4-Hydroxyphenyl)retinamide (4-HPR) exhibits potent anticancer and chemopreventive activities, but its inefficiency under hypoxia, through undetermined mechanisms, may contribute to...

journal_title：Pharmacological research

authors： Liu XW,Su Y,Zhu H,Cao J,Ding WJ,Zhao YC,He QJ,Yang B

更新日期：2010-11-01 00:00:00

abstract：:A novel alkynylthiophene series of cannabinoid CB1 receptor antagonists has been described to exhibit distinct intrinsic activities with minimal substructure modifications. The three representatives, BPR0432, BPR0568 and BPR0569, functioning as a neutral antagonist, an inverse agonist and a partial agonist, respective...

journal_title：Pharmacological research

authors： Lin Y,Shia KS,Hsiao WC,Hsieh WP,Yeh TK,Tseng SL,Hsu CY,Chao YS,Hung MS

更新日期：2010-10-01 00:00:00

abstract：:It is well known that type 2 diabetes mellitus is frequently associated with vascular dysfunction and an elevated systemic blood pressure, yet the underlying mechanisms are not completely understood. We previously reported that in mesenteric arteries from established type 2 diabetic Otsuka Long-Evans Tokushima fatty (...

journal_title：Pharmacological research

authors： Matsumoto T,Ishida K,Nakayama N,Taguchi K,Kobayashi T,Kamata K

更新日期：2010-09-01 00:00:00

abstract：:Aminoglycoside antibiotics are employed clinically because of their potent bactericidal activities, less bacterial resistance, post-antibiotic effects and low cost. However, drugs belong to this class are well-known to cause nephrotoxicity, which limits their frequent clinical exploitation. Gentamicin, a commonly used...

journal_title：Pharmacological research

authors： Balakumar P,Rohilla A,Thangathirupathi A

更新日期：2010-09-01 00:00:00

abstract：:Mast cells take part of armamentarium immunologic for host defense against parasitic and bacterial infections. They are derived from bone marrow progenitors and can be activated by immunological and chemical stimuli in order to get its degranulation. The activation of mast cells generates a signalling cascade leaded t...

journal_title：Pharmacological research

authors： Maldonado MD,Mora-Santos M,Naji L,Carrascosa-Salmoral MP,Naranjo MC,Calvo JR

更新日期：2010-09-01 00:00:00

abstract：:Nanotechnology applications in medicine, termed as nanomedicine, have introduced a number of nanoparticles of variable chemistry and architecture for cancer imaging and treatment. Nanotechnology involves engineering multifunctional devices with dimensions at the nanoscale, similar dimensions as those of large biologic...

journal_title：Pharmacological research

authors： Wang M,Thanou M

更新日期：2010-08-01 00:00:00

abstract：:It is a consensus view that a strategy to increase heart resistance to ischaemia-reperfusion is a warranted. Here, based on our previous study, we have hypothesized that a nicotinamide-rich diet could increase myocardial resistance to ischaemia-reperfusion. Therefore, the purpose of this study was to determine whether...

journal_title：Pharmacological research

authors： Sukhodub A,Du Q,Jovanović S,Jovanović A

更新日期：2010-06-01 00:00:00

abstract：:Reactive oxygen species are important mediators that exert a toxic effect during ischemia-reperfusion (I/R) injury of various organs. Sulforaphane is known to be an indirect antioxidant that acts by inducing Nrf2-dependent phase 2 enzymes. In this study, we investigated whether sulforaphane protects heart against I/R ...

journal_title：Pharmacological research

authors： Piao CS,Gao S,Lee GH,Kim DS,Park BH,Chae SW,Chae HJ,Kim SH

更新日期：2010-04-01 00:00:00

abstract：:The human gut is populated by an array of bacterial species, which develop important metabolic and immune functions, with a marked effect on the nutritional and health status of the host. Dietary component also play beneficial roles beyond basic nutrition, leading to the development of the functional food concept and ...

journal_title：Pharmacological research

authors： Laparra JM,Sanz Y

更新日期：2010-03-01 00:00:00

abstract：:DB-67 and its lactone homolog DB-91 are derivatives of topoisomerase I inhibitor camptothecin (CPT) with silyl moiety, which may exhibit a slower inactivation process by changed kinetics of protein binding and/or hydrolysis of its lactone ring and result in increased antitumor activity and decreased toxicity. Pharmaco...

journal_title：Pharmacological research

authors： Yeh TK,Li CM,Chen CP,Chuu JJ,Huang CL,Wang HS,Shen CC,Lee TY,Chang CY,Chang CM,Chao YS,Lin CT,Chang JY,Chen CT

更新日期：2010-02-01 00:00:00

abstract：:Kidney disease is a frequent complication in diabetes, and significant differences have been reported between male and female patients. Our working hypothesis was that diabetes might modify the vascular actions of testosterone in isolated rabbit renal arteries and the mechanisms involved in these actions. Testosterone...

journal_title：Pharmacological research

authors： Marrachelli VG,Miranda FJ,Centeno JM,Burguete MC,Castelló-Ruiz M,Jover-Mengual T,Pérez AM,Salom JB,Torregrosa G,Alborch E

更新日期：2010-02-01 00:00:00

abstract：:Asymmetric (N(G),N(G)) dimethylarginine (ADMA) is present in plasma and cells. It can inhibit nitric oxide synthase (NOS) that generates nitric oxide (NO) and cationic amino acid transporters (CATs) that supply intracellular NOS with its substrate, l-arginine, from the plasma. Therefore, ADMA and its transport mechani...

journal_title：Pharmacological research

authors： Teerlink T,Luo Z,Palm F,Wilcox CS

更新日期：2009-12-01 00:00:00

abstract：PURPOSE OF THE RESEARCH:Overexpression of the human dimethylarginine dimethylaminohydrolase type 1 (hDDAH1) gene was reported to have beneficial cardiovascular effects in mice. To date, it is unclear whether these effects are related to enhanced metabolic clearance of asymmetric dimethylarginine (ADMA) and l-N(G)-mono-...

journal_title：Pharmacological research

authors： Schwedhelm E,von Leitner EC,Atzler D,Schmitz C,Jacobi J,Meinertz T,Münzel T,Baldus S,Cooke JP,Böger RH,Maas R,Sydow K

更新日期：2009-12-01 00:00:00

abstract：:In recent clinical observation, the growth of endothelial tumors, such as hemangiomas of infancy, was repressed by the non-selective beta-adrenergic antagonist propranolol possibly through targeting of the vascular endothelial compartment. As human brain microvascular endothelial cells (HBMEC) play an essential role a...

journal_title：Pharmacological research

authors： Annabi B,Lachambre MP,Plouffe K,Moumdjian R,Béliveau R

更新日期：2009-11-01 00:00:00

abstract：:The pharmacological profile of PF-00885706, a selective 5-HT(4) receptor partial agonist, was investigated. PF-00885706 displayed a high binding affinity for the human 5-HT(4d) receptor with a K(i) of 3.7 nM that translates to functional agonist activity in vitro with EC(50) values of 4.0 nM and 6.6 nM in cell-based a...

journal_title：Pharmacological research

authors： Komada T,Matsuura T,Mikami T,Suzuki K,Sugimoto H,Kimura N,Ohmi T,Toga T,Nakai Y,Eda H,Sakakibara M

更新日期：2009-10-01 00:00:00