Abstract:
:There is considerable evidence to support the role of anandamide (AEA), an endogenous ligand of cannabinoid receptors, in neuropathic pain modulation. AEA also produces effects mediated by other biological targets, of which the transient receptor potential vanilloid type 1 (TRPV1) has been the most investigated. Both, inhibition of AEA breakdown by fatty acid amide hydrolase (FAAH) and blockage of TRPV1 have been shown to produce anti-nociceptive effects. Recent research suggests the usefulness of dual-action compounds, which may afford greater anti-allodynic efficacy. Therefore, in the present study, we examined the effect of N-arachidonoyl-serotonin (AA-5-HT), a blocker of FAAH and TRPV1, in a rat model of neuropathic pain after intrathecal administration. We found that treatment with AA-5-HT increased the pain threshold to mechanical and thermal stimuli, with highest effect at the dose of 500nM, which was most strongly attenuated by AM-630, CB2 antagonist, administration. The single action blockers PF-3845 (1000nM, for FAAH) and I-RTX (1nM, for TRPV1) showed lower efficacy than AA-5-HT. Moreover AA-5-HT (500nM) elevated AEA and palmitoylethanolamide (PEA) levels. Among the possible targets of these mediators, only the mRNA levels of CB2, GPR18 and GPR55, which are believed to be novel cannabinoid receptors, were upregulated in the spinal cord and/or DRG of CCI rats. It was previously reported that AA-5-HT acts in CB1 and TRPV1-dependent manner after systemic administration, but here for the first time we show that AA-5-HT action at the spinal level involves CB2, with potential contributions from GRP18 and/or GPR55 receptors.
journal_name
Pharmacol Resjournal_title
Pharmacological researchauthors
Malek N,Kostrzewa M,Makuch W,Pajak A,Kucharczyk M,Piscitelli F,Przewlocka B,Di Marzo V,Starowicz Kdoi
10.1016/j.phrs.2016.06.012subject
Has Abstractpub_date
2016-09-01 00:00:00pages
251-263eissn
1043-6618issn
1096-1186pii
S1043-6618(16)30566-7journal_volume
111pub_type
杂志文章abstract::The aim of this study was to verify the role of Vitamins C and E on the cognitive function of young and aged mice. First and second groups of young animals (aged 3 months) received either Vitamin E (250mg/kg per day) or Vitamin C (300mg/kg per day) for 60 days. Third group was treated with the combination of Vitamin E...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2003.10.004
更新日期:2004-03-01 00:00:00
abstract::Capsaicin at a concentration of 10(-7)m induced a significant increase in heart rate and increased coronary flow in isolated Langendorff-perfused guinea-pig hearts. This effect was completely blocked by 30 microm of N(omega)-nitro-L-arginine methyl ester (L-NAME), an inhibitor of nitric oxide synthase. Additional incu...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.1999.0475
更新日期:1999-08-01 00:00:00
abstract::Sumatriptan is a 5-HT1B/D receptor agonist of documented efficacy in relieving migraine and associated symptoms such as nausea and vomiting. In the past decade, several studies reported an important delay of gastric emptying induced by sumatriptan in healthy humans. The impact of this gastric motor effect of sumatript...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1006/phrs.2000.0766
更新日期:2001-03-01 00:00:00
abstract::Macroscale delivery systems that can be locally implanted on the tumor tissue as well as avoid all the complications associated to the systemic delivery of therapeutics have captured researchers' attention, in recent years. Particularly, the microneedle-based devices can be used to efficiently deliver both small and m...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2019.104438
更新日期:2019-10-01 00:00:00
abstract::We investigated the anti-platelet effect of a newly synthesized guanidine derivative KR-32560, a sodium/hydrogen exchanger-1 (NHE-1) inhibitor, together with the elucidation of the possible mode of action. KR-32560 concentration dependently inhibited the aggregation of washed rabbit platelets induced by collagen (10 m...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2005.12.003
更新日期:2006-03-01 00:00:00
abstract::Erdosteine was introduced in the market as a mucolytic agent for chronic pulmonary diseases more than 10 years ago. The drug contains two blocked sulphydryl groups one of which, after hepatic metabolization and opening of the thiolactone ring, becomes available both for the mucolytic and free radical scavenging and an...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2006.12.006
更新日期:2007-04-01 00:00:00
abstract::The accident to the nuclear power plant of Chernobyl (in April 1986) caused a radioactive contamination in large areas of the majority of European countries. During the first transient time the fall-out phenomenon was the most important method of contamination, particularly from 131I whose relative isotopic abundance ...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/s1043-6618(95)80011-5
更新日期:1995-07-01 00:00:00
abstract::Spinal muscular atrophy (SMA) is an autosomal recessive neurodegenerative disease characterized by motor neurons degeneration and muscular atrophy. There is no effective SMA treatment. Loganin is a botanical candidate with anti-inflammatory, anti-oxidant, glucose-lowering and anti-diabetic nephropathy activities. The ...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2016.05.023
更新日期:2016-09-01 00:00:00
abstract::Anti-hypertensive agents may differently stimulate compensatory neuro-hormonal mechanisms and induce different effects on the cardiovascular remodeling and function. The combination of low doses of the two synergistic drugs may lead to a lesser activation of counter regulatory mechanisms and could provide optimal ther...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2004.10.010
更新日期:2005-04-01 00:00:00
abstract::Most cancer cells generate energy through aerobic glycolysis to enable their rapid growth and proliferation, which is a phenomenon known as Warburg effect. Inhibition of aerobic glycolysis reduces lactate and ATP generation in cancer cells, and ultimately kills tumor cells. Increasing evidence suggests that wogonin, a...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2018.07.011
更新日期:2018-09-01 00:00:00
abstract::The DNA microarrays have proven to be a state of the art technique for high throughput comprehensive analysis of thousand of genes in parallel. The application of a DNA microarray to compare normal and pathological cells, tissues or organs may allow, along with classical positional cloning techniques, to speed up the ...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2003.06.001
更新日期:2004-04-01 00:00:00
abstract::Diabetic erectile dysfunction (DED) hugely affected the patients' sexual life quality. However, there are no satisfactory therapeutic methods and intervention targets for this subtype of erectile dysfunction (ED). Inspired by the clinical practice of traditional Chinese medicine (TCM), we found that hirudin, the main ...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2020.105244
更新日期:2021-01-01 00:00:00
abstract::In previous studies we observed an enhanced anti-inflammatory activity of MPEG-SOD derivatives in acute inflammation in rat. To assess the activity in chronic inflammation we tested the compound with longer half-life (MPEG-SOD 18) in complete adjuvant arthritis in rat. According to the prophylactic schedule of treatme...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/s1043-6618(05)80106-9
更新日期:1991-01-01 00:00:00
abstract::Insulin-like growth factor-1, angiotensin-(1-7) and angiotensin-(1-9) have been proposed to be important mediators in cardioprotection. A large body of evidence indicates that insulin like growth factor-1 has pleotropic actions in the heart (i.e., contractility, metabolism, hypertrophy, autophagy, senescence and cell ...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2015.06.018
更新日期:2015-11-01 00:00:00
abstract::Cardiac arrhythmia can be a serious complication during general anaesthesia of patients suffering from cardiac arrhythmias and using antiarrhythmic drugs. The aim of the present experiments was to establish the way in which lidocaine and verapamil influence haemodynamic parameters of rabbits after midazolam anaesthesi...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.1998.0464
更新日期:1999-06-01 00:00:00
abstract::Advanced glycation end-products (AGE) and the receptor for AGE (RAGE) have been linked to numerous diabetic vascular complications. RAGE activation promotes a self-sustaining state of chronic inflammation and has been shown to induce apoptosis in various cell types. Although previous studies in vascular smooth muscle ...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2015.12.015
更新日期:2016-02-01 00:00:00
abstract::Isoxanthohumol (IXN), a prenylated flavonoid from hops, exhibits diverse biological activities, e.g. antitumor, antiinflammatory, antioxidant and antiangiogenic. In this study, the effect of IXN is evaluated on two melanoma cell lines with dissimilar molecular background, B16 and A375. The treatment of both cell lines...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2016.01.011
更新日期:2016-03-01 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::Diabetes mellitus is associated with both microvascular and macrovascular complications, which can result in visceral aneurysms as for example splenic artery aneurysms: in their management, an endovascular treatment, less invasive than surgery, is generally preferred. Endovascular treatment of splenic artery aneurysms...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2018.07.023
更新日期:2018-09-01 00:00:00
abstract::Our preliminary data suggested that 1,4-bis(1-naphthyl)-2,3-dinitro-1,3-butadiene [Viale M, Ottone M, Chiavarina B, Mariggiò MA, Prevosto C, Dell'Erba C, et al. Preliminary evaluation in vitro of the inhibition of cell proliferation, cytotoxicity and induction of apoptosis by 1,4-bis(1-naphthyl)-2,3-dinitro-1,3-butadi...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2005.03.011
更新日期:2005-09-01 00:00:00
abstract::Mammalian cells are commonly employed in screening assays to identify active compounds that could potentially affect the progression of different human diseases including retinitis pigmentosa (RP), a class of inherited diseases causing retinal degeneration with compromised vision. Using transcriptome analysis, we comp...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2016.10.031
更新日期:2017-01-01 00:00:00
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, whi...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/s1043-6618(89)80002-7
更新日期:1989-05-01 00:00:00
abstract:AIM AND SCOPE:To determine the acute effects of increased intra-abdominal pressure (IAP) on the biochemistry, morphology, and contractility of the isolated terminal ileum of rats. BACKGROUND:Laparoscopic procedures are used clinically in diagnostic and treatment modalities and experimentally as a model of ischemia-rep...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2005.09.010
更新日期:2006-02-01 00:00:00
abstract::Some macrolide antibiotics have been shown to produce significant drug-drug interactions through the inhibition of cytochrome P450 (CYP) enzymes. In renal transplant patients these interactions pose potentially serious problems for the safe administration of cyclosporine A (CSA), a substrate of CYP3A4. The effects of ...
journal_title:Pharmacological research
pub_type: 临床试验,杂志文章
doi:10.1016/s1043-6618(03)00018-5
更新日期:2003-06-01 00:00:00
abstract::CYT387 is an orally bioavailable, small molecule inhibitor of Janus family of tyrosine kinases (JAK) 1 and 2. It is currently undergoing Phase I/II clinical trials for the treatment of myelofibrosis and myeloproliferative neoplasms. We aimed to establish whether the multidrug efflux transporters P-glycoprotein (P-gp; ...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2013.06.009
更新日期:2013-10-01 00:00:00
abstract::Sixteen adult hypertensive patients of both sexes, classified as having 'medium' (total lipid profile 240-300 mg dl(-1)), and 'high' (total lipid profile >300 mg dl(-1)) baseline values, underwent serum lipids, lipoproteins and plasma fibrinolytic parameters evaluations after 3 months of cilnidipine treatment. Patient...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.1999.0558
更新日期:2000-01-01 00:00:00
abstract::Several factors such as proteinuria and renal fibrosis may be important in the progression of many forms of chronic renal diseases. The purposes of the current study were to investigate the progressive renal failure of the rats with surgical renal mass reduction (RMR) and the effect of the angiotensin-converting enzym...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/s1043-6618(02)00321-3
更新日期:2003-03-01 00:00:00
abstract::Severely obese patients undergoing bariatric surgery (BS) are at increased risk for venous thromboembolism (VTE). How standard low molecular weight heparin (LMWH) regimen should be adapted to provide both sufficient efficacy and safety in this setting is unclear. We aimed to compare the influence of four body size des...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2018.02.012
更新日期:2018-05-01 00:00:00
abstract::Boldo (Peumus boldus Mol.), a Chilean tree traditionally employed in folk medicine and recognized as a herbal remedy in a number of pharmacopoeias, mainly for the treatment of liver ailments, has recently been the subject of increasing attention. Boldine, in particular, the major and most characteristic alkaloidal con...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/1043-6618(94)80093-6
更新日期:1994-01-01 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
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2009.11.001
更新日期:2010-03-01 00:00:00