Abstract：
:In incubated blood mononuclear cells from normal subjects bezafibrate inhibited the incorporation of 14C-acetate into squalene, methylsterols and cholesterol. Similarly, the drug produced a sharp decrease of the incorporation of labelled 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) into non-saponifiable lipids, while the incorporation of 14C-mevalonate was unaffected by the presence of bezafibrate in the incubation mixture. This strongly suggests that bezafibrate inhibits HMG-CoA reductase activity. In cultured cells from patients with heterozygous familial hypercholesterolaemia the presence of bezafibrate in the incubation medium resulted in an inhibition of the incorporation of labelled acetate into non-saponifiable lipids. Bezafibrate then inhibits cholesterol biosynthesis in cells from normal and hypercholesterolaemic patients and this effect is likely, to contribute to the hypocholesterolaemic activity of the drug.
journal_name
Pharmacol Resjournal_title
Pharmacological researchauthors
Blasi F,Sommariva D,Cosentini R,Cavaiani B,Fasoli Adoi
10.1016/s1043-6618(89)80002-7subject
Has Abstractpub_date
1989-05-01 00:00:00pages
247-54issue
3eissn
1043-6618issn
1096-1186pii
S1043-6618(89)80002-7journal_volume
21pub_type
杂志文章abstract：:The effects of betel leaf extract (0.10, 0.40, 0.80 and 2.0 g kg-1 day-1 for 15 days) on the alterations in thyroid hormone concentrations. lipid peroxidation (LPO) and on the activities of superoxide dismutase (SOD) and catalase (CAT) were investigated in male Swiss mice. Administration of betel leaf extract exhibite...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.1998.0398
更新日期：1998-12-01 00:00:00
abstract：:The insulinotropic action of several new esters of succinic acid was assessed in isolated rat islets incubated in the presence of 7 mM D-glucose. An efficient secretory response was observed with the monobenzyl, monoisopropyl, monoallyl, monopropyl, monoethyl, monobutyl, dibutyl, dipropyl and diallyl esters of succini...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.1996.0038
更新日期：1996-04-01 00:00:00
abstract：:Although calcimimetics were developed to block parathyroid hormone synthesis, some reports suggest that they may also reduce blood pressure by unknown mechanisms. Calcimimetic-induced changes in the synthesis of endothelial vasoactive factors could be involved. Wistar rats were treated with the calcimimetic R-568, and...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2013.07.006
更新日期：2013-10-01 00:00:00
abstract：:Sphingosine 1-phosphate (S1P) is an extracellular lipid signaling molecule that acts as a selective, high-affinity ligand for a family of five G protein-coupled receptors. This signaling system was first identified twenty years ago, and has since been shown to regulate a diverse range of physiological processes and di...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2016.09.025
更新日期：2016-11-01 00:00:00
abstract：:Breast cancer (BC) is the most common cancer in women, and the second most frequent cause of cancer-related deaths in women worldwide. It is a heterogeneous disease composed of multiple subtypes with distinct morphologies and clinical implications. Quantitative systems pharmacology (QSP) is an emerging discipline brid...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2017.07.015
更新日期：2017-10-01 00:00:00
abstract：:Oxidative stress is related to the progression of renal diseases and modulation of oxidative stress can lead to a reduction in vascular events in patients with chronic renal insufficiency (CRI). Indoxyl sulfate (IS) and xanthine oxidase (XO) are related to impaired neovasculogenesis in CRI. Hydralazine is suggested fo...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2019.104509
更新日期：2020-01-01 00:00:00
abstract：:The clear importance of mutated KRAS as a therapeutic target has driven the investigation of multiple approaches to inhibit oncogenic KRAS signaling at different molecular levels. However, no KRAS-targeted therapy has reached the clinic to date, which underlies the intrinsic difficulty in developing effective, direct ...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2017.01.006
更新日期：2017-03-01 00:00:00
abstract：:Because many Ca2+ channel blocking agents are known to cause adverse systemic effects, in this study we tested the haemodynamic side effects of nimodipine with and without a mild hypoxic-ischaemic (HI) insult in a newborn piglet model. Fifteen min after completing a brief period of asphyxia we gave i.v. nimodipine as ...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.1996.0002
更新日期：1996-01-01 00:00:00
abstract：:The insulinotropic action of the meglitinide analogues KAD-1229, A-4166 and repaglinide was examined in rat pancreatic islets deprived of exogenous nutrient or incubated in the presence of nutrient secretagogues such as D-glucose and the methyl esters of pyruvic acid, succinic acid and glutamic acid. The meglitinide a...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.1996.0026
更新日期：1996-03-01 00:00:00
abstract：OBJECTIVES:There is still a need to develop new effective medications for the treatment of ulcerative colitis, particularly for patients who are intolerant or resistant to first line therapies. This article compared the efficacy and safety of etrolizumab and infliximab in moderate to severe ulcerative colitis. METHODS...
journal_title：Pharmacological research
pub_type： 杂志文章,meta分析
doi：10.1016/j.phrs.2018.11.003
更新日期：2019-01-01 00:00:00
abstract：:Most solid tumor cells adapt to their heterogeneous microenvironment by depending largely on aerobic glycolysis for energy production, a phenomenon called the Warburg effect, which is a hallmark of cancer. The altered energy metabolism not only provides cancer cell with ATP for cellular energy, but also generate essen...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2019.104511
更新日期：2019-12-01 00:00:00
abstract：:A study was carried out relating to the anticholinergic action of clonidine on the cardiovascular responses to i.c.v. injection of neostigmine, a quaternary anticholinesterase, in conscious sham-operated animals and rats with sinoaortic denervation, 7 days after the corresponding operation. Neostigmine (0.1-1 microgra...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.1997.0295
更新日期：1998-04-01 00:00:00
abstract：:Protein kinase C (PKC) is a family of kinases that are critical in many cellular events. These enzymes are activated by lipid-derived second messengers, are dependent on binding to negatively charged phospholipids and some members also require calcium to attain full activation. The interaction with lipids and calcium ...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2007.04.014
更新日期：2007-06-01 00:00:00
abstract：:Secretion of matrix metalloproteinases (MMPs) by macrophages and smooth muscle cells (SMC) may impair atherosclerotic cap integrity leading to atherosclerosis complications. Selective estrogen receptor modulators (SERMs) have favourable impact on plasma lipid levels, but their role in the prevention of atherosclerosis...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2007.05.004
更新日期：2007-08-01 00:00:00
abstract：:An interaction of drug with food, herbs, and dietary supplements is usually the consequence of a physical, chemical or physiologic relationship between a drug and a product consumed as food, nutritional supplement or over-the-counter medicinal plant. The current educational review aims at reminding to the prescribing ...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2016.09.038
更新日期：2017-04-01 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
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2011.05.007
更新日期：2011-08-01 00:00:00
abstract：:Antidepressants, especially tricyclic agents (TCAs), are increasingly used in geriatric patients since depression is a common mood disorder in the elderly and the size of elderly population is increasing. Notwithstanding the importance of kinetics to better use of drugs, its study in the elderly (regarding TCAs) is no...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/1043-6618(90)90739-z
更新日期：1990-01-01 00:00:00
abstract：:Our goal was to establish the requirement of β3 adrenoceptor (β3Adr) for green tea (GT) effects on the energy metabolism of obese mice. This study was carried out in wild-type (WT) and β3Adr knockout (KO) male mice fed with a standard diet or a high-fat diet (HFD/16 weeks) treated or not with GT (0.5 g/kg of body weig...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2020.104956
更新日期：2020-09-01 00:00:00
abstract：:Paradoxical sleep deprivation in rats is considered as an experimental animal model of mania endowed with face, construct, and pharmacological validity. We induced paradoxical sleep deprivation by placing rats onto a small platform surrounded by water. This procedure caused the animal to fall in the water at the onset...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2016.11.029
更新日期：2017-03-01 00:00:00
abstract：:The smoothened (SMO) receptor, an essential signal transducer in the Hedgehog pathway, was targeted with antagonists to suppress the tumor. It is interesting that SMO D473H mutation confers resistance on inhibitor LDE-225 rather than LEQ-506. In this paper, the binding modes of them against the wild type and mutant SM...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2017.11.025
更新日期：2018-03-01 00:00:00
abstract：:Biotechnologicals are an invaluable resource in the treatment of patients with inflammatory rheumatic diseases (IRD) non-responsive or intolerant to conventional therapies. However, they are the main driver for increase in direct costs and represent a significant economic burden to healthcare systems worldwide. Since ...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2019.104467
更新日期：2019-11-01 00:00:00
abstract：:Rheumatoid arthritis (RA) is a systemic and chronic autoimmune inflammatory disorder affecting multiple joints. Various cytokines, chemokines and growth factors synergistically modulate the joint physiology leading to bone erosion and cartilage degradation. Other than these conventional mediators that are well establi...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2018.05.016
更新日期：2018-08-01 00:00:00
abstract：:Baroreflex plays a crucial role in regulation of arterial blood pressure (BP). Recently, Piezo1 and Piezo2, the mechanically-activated (MA) ion channels, have been identified as baroreceptors. However, the underlying molecular mechanism for regulating these baroreceptors in hypertension remains unknown. In this study,...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2020.105391
更新日期：2020-12-19 00:00:00
abstract：:Cardiovascular baroreflex mechanisms and sympathetic tone could be involved in the arterial hypertension by coarctation of abdominal aorta artery (CoA). The present work analyzes the effect on the arterial pressure and heart rate (HR) of the clonidine, an alpha(2)-adrenergic central acting antihypertensive agent, afte...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：
更新日期：2003-07-01 00:00:00
abstract：:Corticosteroids are shown to have deleterious effects on wound healing for various tissues. Arginine metabolism and nitric oxide (NO) synthesis play an important role in many aspects of inflammation and wound healing. The study was designed to evaluate the relationship of dexamethasone impaired healing of tracheal ana...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/s1043-6618(02)00130-5
更新日期：2002-09-01 00:00:00
abstract：:Flt3 is expressed by early myeloid and lymphoid progenitor cells and it regulates the proliferation and differentiation of hematopoietic cells. Flt3 is activated by the Flt3 ligand, the monomeric form of which is a polypeptide of about 200 amino acid residues. Both membrane-associated and soluble Flt3 ligands, which a...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2020.104725
更新日期：2020-05-01 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
pub_type： 杂志文章
doi：10.1016/j.phrs.2012.05.004
更新日期：2012-09-01 00:00:00
abstract：:Neuroinflammation plays an important role in the progression of various neurodegenerative diseases. In this study, we investigated the anti-inflammatory effects of lonchocarpine, a natural compound isolated from Abrus precatorius, under in vitro and in vivo neuroinflammatory conditions induced by challenge with lipopo...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2017.02.027
更新日期：2017-05-01 00:00:00
abstract：:Tachykinins are important in the development of pulmonary inflammation in mice but the tachykinin receptor subtype mediating this response has not been defined. To elucidate the role of tachykinin NK3-receptors on allergen-induced pulmonary inflammation, studies were performed on ovalbumin (OVA) sensitized and challen...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2004.07.002
更新日期：2004-12-01 00:00:00
abstract：BACKGROUND AND PURPOSE:Chronic obstructive pulmonary disease (COPD) is characterized by progressive alveolar damage and generally irreversible airflow limitation. Nuclear factor-κB (NF-κB) plays a critical role in COPD pathogenesis. Receptor-interacting protein 2 (Rip2), a 60 kDa adaptor protein, is a positive regulato...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2018.10.016
更新日期：2019-01-01 00:00:00
