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Imidazoles (37):
- Nitroimidazoles
- Imidazolidines
- Enoximone
- Creatinine
- Fluspirilene
- Dexmedetomidine
- Tetramisole
- Levamisole
- Impromidine
- Etomidate
- Clotrimazole
- Aminoimidazole Carboxamide
- Imidazolines
- Fadrozole
- Dacarbazine
- Phentolamine
- Ondansetron
- Cimetidine
- Carbimazole
- Antazoline
- Trimethaphan
- Miconazole
- Methimazole
- Econazole
- Biotin
- Medetomidine
- Losartan
- Idazoxan
- Histamine
- Etimizol
- Urocanic Acid
- Oxymetazoline
- Niridazole
- Naphazoline
- Histidinol
- 4-(3-Butoxy-4-methoxybenzyl)-2-imidazolidinone
- Bis(4-Methyl-1-Homopiperazinylthiocarbonyl)disulfide
Recent article
Imidazoles
Abstract
We have discovered that other cellular stressors are integrated with glucocorticoid signaling through a new hormone-independent phosphorylation site, Ser134, on the human glucocorticoid receptor (GR). Ser134 phosphorylation is induced by a variety of stress-activating stimuli in a p38 mitogen-activa...
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PMID: 21930780
PDF is available here.
PDF is available here.
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New England Journal of Medicine (364)23 2011
Abstract
New England Journal of Medicine (364)23 2011
Abstract
New England Journal of Medicine (364)23 2011
Abstract
New England Journal of Medicine (364)23 2011
Abstract
Abstract
We have investigated whether or not the novel and promising hypoxia-selective cytotoxin 4-[3-(2-nitro-1-imidazolyl)-propylamino]-7-chloroquinoline hydrochloride (NLCQ-1, NSC 709257) can cause hypoxia-dependent retinal toxicity in BALB/c mice alone or in combination with cyclophosphamide (CPM), one o...
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PMID: 21205223
PDF is available here.
PDF is available here.
New England Journal of Medicine (364)10 2011
Abstract
We investigated whether treatment with an angiotensin-receptor blocker (ARB) would delay or prevent the occurrence of microalbuminuria in patients with type 2 diabetes and normoalbuminuria.
In a randomized, double-blind, multicenter, controlled trial, we assigned 4447 patients with t...
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PMID: 21388309
PDF is available here.
PDF is available here.
New England Journal of Medicine (364)10 2011
Abstract
Abstract
We performed repetitive active anterior rhinomanometry in 9 persons during 5 months to test reproducibility of nasal airway resistance (NAR) over time. We also did test-retest measurements in several participants. Xylometazoline hydrochloride was applied in each nasal cavity to minimize effects of m...
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PMID: 21468374
PDF is available here.
PDF is available here.
Abstract
We tested the role of this intramolecular H(+) shuttle on CA activity in an intact cell. The data revealed that CAIII, shown in vitro to have ∼1,000-fold reduced activity as compared with CAII, displays significant catalytic activity in the intact cell. Furthermore, we tested the hypothesis that t...
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PMID: 21282642
PDF is available here.
PDF is available here.
Abstract
Inhibitor ofadenylate cyclase (SQ 22,536) and inhibitors ofserin/threonine protein kinases A (PKA -Rp-cAMPS), G (PKG - H-Arg-Lys-Arg-Ala-Arg-Lys-Glu-OH), calcium/calmodulin-dependent kinase II (CaMKII - KN-93), p38mitogen-activated (MAPK - PD 169316), and tyrosine protein kinases (ge...
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PMID: 21961321
PDF is available here.
PDF is available here.
Metallomics (3)1 2011
Abstract
From the reaction of 1-methylimidazole (1a), 4,5-dichloro-1H-imidazole (1b(I)) and 1-methylbenzimidazole (1c) with p-cyanobenzyl bromide (2a), non-symmetrically substituted N-heterocyclic carbene (NHC) [(3a-c)] precursors, 5,6-dimethyl-1H-benzimidazole (1d) and 4,5-diphenyl-1H-imidaz...
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PMID: 21135954
PDF is available here.
PDF is available here.
Neonatology (99)2 2011
Abstract
We studied the effects of lipopolysaccharide (LPS) on expression and function of NF-κB and p38 MAPK in whole neonatal cord and adult blood.
Th1/Th2 cytokine concentrations and phosphorylation of NF-κB and p38 MAPK were determined by flow-cytometric analysis.
Tumor n...
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PMID: 20798552
PDF is available here.
PDF is available here.
Abstract
The aim of the present study was to evaluate the effects of phosphodiesterase 5 inhibitors on renal tubular apoptosis and also on expressions of endothelial and inducible nitric oxide synthases (eNOS and iNOS) in the ipsilateral kidney after partial unilateral ureteral obstruction (P...
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PMID: 21329887
PDF is available here.
PDF is available here.
Abstract
The aim of the present study was to evaluate the effects of phosphodiesterase 5 inhibitors on renal tubular apoptosis and also on expressions of endothelial and inducible nitric oxide synthases (eNOS and iNOS) in the ipsilateral kidney after partial unilateral ureteral obstruction (P...
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PMID: 21329887
PDF is available here.
PDF is available here.
Abstract
The aim of the present study was to evaluate the effects of phosphodiesterase 5 inhibitors on renal tubular apoptosis and also on expressions of endothelial and inducible nitric oxide synthases (eNOS and iNOS) in the ipsilateral kidney after partial unilateral ureteral obstruction (P...
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PMID: 21329887
PDF is available here.
PDF is available here.
Abstract
The aim of the present study was to evaluate the effects of phosphodiesterase 5 inhibitors on renal tubular apoptosis and also on expressions of endothelial and inducible nitric oxide synthases (eNOS and iNOS) in the ipsilateral kidney after partial unilateral ureteral obstruction (P...
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PMID: 21329887
PDF is available here.
PDF is available here.
Abstract
I clinical trials indicated that 2, the first clinically studied inhibitor of S1PL, produced a dose-dependent and reversible reduction of circulating lymphocytes and was well tolerated at dose levels of up to 180 mg daily. Phase II evaluation of 2 in patients with active rheumatoid arthritis is curr...
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PMID: 21090716
PDF is available here.
PDF is available here.
Abstract
To determine whether sublingual detomidine gel administration to horses would be effective in providing an appropriate degree of sedation and restraint to facilitate completion of veterinary and husbandry procedures under field conditions.
Multicenter, prospective, randomized, blinded, placebo-contr...
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PMID: 21155687
PDF is available here.
PDF is available here.
Abstract
Abstract
We found in this study that blockade of the interaction of p53 and MDM2 by the MDM2 antagonist nutlin-3 in melanoma cells did not induce apoptosis, even though it upregulated p53 and its proapoptotic targets. Nevertheless, nutlin-3 enhanced TRAIL-induced apoptosis as a result of p53-mediated upregul...
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PMID: 21159614
PDF is available here.
PDF is available here.
Clinical Breast Cancer (10)6 2010
Abstract
I collagen corrected for creatinine (uNTx; primary objective, pmol BCE/µmol creatinine). Adverse events (AEs) were monitored throughout the 4-week study and up to 14 days after last dose.
A total of 43 patients (mean age, 60 years) received odanacatib (n = 29) or ZA (n = 14); 40 pat...
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PMID: 21147688
PDF is available here.
PDF is available here.
Journal of Antibiotics (63)12 2010
Abstract
Two new alkaloids, dysideanins A (1) and B (2), along with two known diketopiperazines, cyclo-(Pro-Leu) (3) and cyclo-(Pro-Ile) (4), were isolated from the marine sponge Dysidea sp. The structures were established from NMR and MS analysis. Dysideanin B (2) exhibited antibacterial activity. The thiom...
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PMID: 21063424
PDF is available here.
PDF is available here.
Abstract
We demonstrate that an analog of doxorubicin (a representative example of an anticancer therapeutic) conjugated to human serum albumin (HSA, a representative example of a macromolecular carrier) via this NEBI crosslinker can internalize and localize into acidic lysosomes of ovarian cancer cells. Flu...
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PMID: 20820656
PDF is available here.
PDF is available here.
Abstract
The discovery of sulfoxaflor [N-[methyloxido[1-[6-(trifluoromethyl)-3-pyridinyl]ethyl]-λ(4)-sulfanylidene] cyanamide] resulted from an investigation of the sulfoximine functional group as a novel bioactive scaffold for insecticidal activity and a subsequent extensive structure-activity relationship...
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PMID: 21105655
PDF is available here.
PDF is available here.
Biomedical Chromatography (24)12 2010
Abstract
A simple, high-throughput and specific high-performance liquid chromatography tandem mass spectrometry method has been developed and validated according to the FDA guidelines for simultaneous quantification of olmesartan and pioglitazone in rat plasma. The bioanalytical method consists of liquid-liq...
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PMID: 21077253
PDF is available here.
PDF is available here.
Abstract
Charge transport in 1-hexyl-3-methylimidazolium hexafluorophosphate ionic liquid in oxidized nanoporous silicon membranes is investigated in a wide frequency and temperature range by a combination of Broadband Dielectric Spectroscopy (BDS) and Pulsed Field Gradient Nuclear Magnetic Resonance (PFG NM...
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PMID: 20824257
PDF is available here.
PDF is available here.
Chemmedchem (5)11 2010
Abstract
A new class of imidazo[2,1-b]thiazole chalcone derivatives were synthesized and evaluated for their anticancer activity. These chalcone derivatives show promising activity, with log GI(50) values ranging from -7.51 to -4.00. The detailed biological aspects of these derivatives towa...
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PMID: 20836120
PDF is available here.
PDF is available here.
Radiation Research (174)5 2010
Abstract
The radiation stability of the ionic liquid 1-butyl-3-methylimidazolium chloride ([Bmim]Cl) was investigated after (60)Co γ irradiation at doses up to 600 kGy. Thermal and spectroscopic analysis revealed the formation of a small quantity of radiolytic products and an evident change in the physicoch...
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PMID: 20726704
PDF is available here.
PDF is available here.
Free Radical Research (44)11 2010
Abstract
The aim was to evaluate the role of the combination of olmesartan, an angiotensin II (Ang II) receptor blocker (ARB), with daunorubicin (DNR) in reducing cardiac toxicity in rats. DNR was administered at a dose of 3 mg/kg/day every other day for 12 days. Olmesartan was administered orally every day...
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PMID: 20815778
PDF is available here.
PDF is available here.
Abstract
We report a case of a 16-year-old female with Gorham-Stout disease and recurrent pleural effusions who was successfully treated with concurrent zoledronic acid and peg-interferon α-2b....
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PMID: 20962674
PDF is available here.
PDF is available here.
Abstract
We measured the changes in the plasma concentration of tumor necrosis factor (TNF)-α and interferon (IFN)-α, which are induced downstream from the TLR-ligand interaction, in exhaustive-exercised mice immediately after treatment with the imidazoquinoline R-848, which can bind to and activate TLR7....
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PMID: 20602110
PDF is available here.
PDF is available here.
Abstract
The hexaazamacrocycles [28](DBF)(2)N(6) {cyclo[bis(4,6-dimethyldibenzo[b,d]furaniminoethyleneiminoethylene]} and [32](DBF)(2)N(6) {cyclo[bis(4,6-dimethyldibenzo[b,d]furaniminopropyleneiminopropylene]} form stable dinuclear copper(ii) complexes suitable to behave as receptors for several anionic subs...
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PMID: 20820604
PDF is available here.
PDF is available here.
Abstract
Resistance development and limited lepidopteran activities call for the discovery of "super-neonicotinoids" solving these problems. Compounds with the cis-configuration offer an opportunity for further optimization. Fixing the nitro group in the cis-configuration provided a new approach for neonicoti...
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PMID: 21043520
PDF is available here.
PDF is available here.
Journal of Hypertension (28)11 2010
Abstract
To compare the efficacy and safety of the angiotensin II antagonist olmesartan medoxomil (O) and the ACE inhibitor ramipril (R) in elderly patients with essential arterial hypertension.
After a 2-week placebo wash-out 1102 treated or untreated elderly hypertensive patients aged 65-89 years (office s...
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PMID: 20829713
PDF is available here.
PDF is available here.
Abstract
We previously showed that neurotoxin-induced dopaminergic (DA) cell loss is decreased by inhibition of angiotensin receptors, but the location and functional effects of prorenin receptor (PRR) in the brain, including the DA system, are unknown. In the substantia nigra of Macaca fascicularis and in r...
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PMID: 20940627
PDF is available here.
PDF is available here.
Archives of Dermatology (146)11 2010
Abstract
Arthritis & Rheumatism (62)11 2010
Abstract
The activity of p38 MAPK regulates lipopolysaccharide (LPS)-stimulated production of key proinflammatory cytokines such as tumor necrosis factor α (TNFα). Consequently, p38 MAPK inhibitors have attracted considerable interest as potential treatments of rheumatoid arthritis (RA), and studies in mur...
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PMID: 20589681
PDF is available here.
PDF is available here.
Biochemical Journal (432)1 2010
Abstract
We investigated the role of the ERK (extracellular-signal-regulated kinase) and p38 MAPK (mitogen-activated protein kinase) signalling pathways in MEL (mouse erythroleukaemia) cell differentiation. We found that treatment of HMBA (hexamethylene bisacetamide)-induced MEL cells with the ERK pathway in...
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PMID: 20738258
PDF is available here.
PDF is available here.
Journal of Biological Chemistry (285)43 2010
Abstract
Plasmodium falciparum, the causative agent of the most deadly form of human malaria, is unable to salvage pyrimidines and must rely on de novo biosynthesis for survival. Dihydroorotate dehydrogenase (DHODH) catalyzes the rate-limiting step in the pyrimidine biosynthetic pathway and r...
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PMID: 20702404
PDF is available here.
PDF is available here.
Abstract
A series of N-aryl-2-arylthioacetamide derivatives (2-4) designed as non-nucleoside reverse transcriptase inhibitors was synthesized and evaluated for their inhibitory activity against HIV-1 (IIIB) replication in MT-4 cell cultures. The compounds 2-4 were performed by the reaction of thiols and 2-ch...
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PMID: 20731670
PDF is available here.
PDF is available here.
YAKUGAKU ZASSHI (130)10 2010
Abstract
We paid an attention to inhibitors against three enzymes, ubiquitin-activating enzyme (E1), ubiquitin-conjugating enzyme (E2), and ubiquitin-protein ligase (E3), which are required for polyubiquitination of proteins and prerequisite to proteasome-mediated protein degradation. We succeeded in isolati...
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PMID: 20930478
PDF is available here.
PDF is available here.
Abstract
Abstract
Sixteen captive female red deer were successfully anesthetized to surgically implant a telemetry system. The deer were immobilized with (mean±SD) 1.79±0.29 mg/kg xylazine and 1.79±0.29 mg/kg tiletamine/zolazepam given intramuscularly with a dart gun. Anesthesia was maintained for 69±2 min using...
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PMID: 20966270
PDF is available here.
PDF is available here.
Abstract
Purine analogs modified in the five-membered ring have been synthesized and examined for antibacterial activity against Mycobacterium tuberculosis H(37)Rv in vitro employing the microplate alamar blue assay (MABA). The 9-deaza analogs were only found to be weak inhibitors, but the 8-aza-, 7-deaza- a...
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PMID: 20833056
PDF is available here.
PDF is available here.
Abstract
We examined the mechanisms by which Ang II affected the cell proliferation in AT1R-positive MCF-7 human breast cancer cells. Ang II stimulated the growth of breast cancer cells in a dose- and time-dependent manner. The maximal proliferation effect on MCF-7 cells was obtained with 10(-4) M Ang II at...
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PMID: 20458733
PDF is available here.
PDF is available here.
Anesthesiology (113)4 2010
Abstract
Baseline adenosine levels before stimulating lymphocytes with 4CmC were 0.025 ± 0.004 and 0.041 ± 0.006 μm (mean ± SEM) in lymphocytes from normal and MHS swine, respectively (P = 0.125). Maximum responses were achieved at 1 mm 4CmC for both cell-line groups. Adenosine levels after stimulation w...
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PMID: 20823761
PDF is available here.
PDF is available here.
Abstract
The physicochemical properties of candidate compounds play important roles in the design of new pesticides. Pesticides must be absorbed by pests, be transported to the target site, and then interact with proteins. Hydrophobicity is very important for these processes. Log P, where P is the partition c...
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PMID: 20879794
PDF is available here.
PDF is available here.
Biochemical Journal (431)2 2010
Abstract
We describe a novel cell-permeable inhibitor of S6K1, PF-4708671, which specifically inhibits the S6K1 isoform with a Ki of 20 nM and IC50 of 160 nM. PF-4708671 prevents the S6K1-mediated phosphorylation of S6 protein in response to IGF-1 (insulin-like growth factor 1), while having no effect upon t...
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PMID: 20704563
PDF is available here.
PDF is available here.
Toxicology (276)1 2010
Abstract
The essence of the Druckrey-Küpfmüller equation dtn = constant (where d = daily dose and t = exposure time-to-effect, with n > 1) for chemical carcinogens is that the total dose required to produce the same effect decreases with decreasing exposure levels, even though the exposure times required t...
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PMID: 20803795
PDF is available here.
PDF is available here.
Abstract
Many patients with hypertension require more than one drug to control their blood pressure.1 Tribenzor (Daiichi Sankyo), recently approved by the FDA for treatment of hypertension, combines the calcium channel blocker amlodipine (Norvasc, and others), the angiotensin receptor blocker (ARB) olmesarta...
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PMID: 20814402
PDF is available here.
PDF is available here.
Abstract
We found no evidence for a difference in outcomes; therefore, pamidronate is an effective choice where clinic capacity permits....
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PMID: 20682850
PDF is available here.
PDF is available here.
Abstract
Our results report a novel mechanism through which P188 exerts its protective effects on cartilage in the model of acute injury. In addition to its effect on cellular membrane, P188 affects stress-related p38 signaling, apoptosis-related GSK3, and inflammation-related IL-6 signaling. Taken together,...
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PMID: 20736797
PDF is available here.
PDF is available here.
Abstract
The pathology of pulmonary arterial hypertension (PAH) is characterized by vascular vasoconstriction, smooth muscle cell proliferation, and thrombosis. Experimental studies have shown the beneficial effect of phosphodiesterase type 5 (PDE-5) inhibitors on pulmonary vascular remodeling and vasodilata...
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PMID: 20819751
PDF is available here.
PDF is available here.
Chemical Communications (46)32 2010
Abstract
The synthesis of a bicyclic enediyne capable of photosensitive triggering and conjugated to a pyrrole-imidazole polyamide is described. Using UV irradiation, this hybrid molecule is shown to exhibit 100-fold stronger potency for DNA cleavage, in an in vitro assay, as compared to the enediyne without...
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PMID: 20601986
PDF is available here.
PDF is available here.
Journal of Hypertension (28)9 2010
Abstract
We suggest that the inhibition of central sympathetic outflow may improve cardiovascular prognosis in ESRD....
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PMID: 20634720
PDF is available here.
PDF is available here.
Journal of Hypertension (28)9 2010
Abstract
We examined the effect of FAD286 (FAD), an aldosterone synthase inhibitor, on the development of atherosclerosis in spontaneous atherosclerotic apolipoprotein E-deficient mice. Mice were divided into three treatment groups: normal diet, low-salt diet (LSD) and LSD treated with FAD at 30 mg/kg per da...
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PMID: 20699715
PDF is available here.
PDF is available here.
Anticancer Research (30)9 2010
Abstract
Repeated treatment with ZOL induced drug resistance with down-regulation of apoptosis in the resistant cell line. Although ABC expression was down-regulated, up-regulation of HSP27 in the resistant cell line was confirmed. The resistance was overcome by HSP27 silencing. CONCLUSION: Resistance to ZOL...
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PMID: 20944138
PDF is available here.
PDF is available here.
Abstract
We demonstrate that both gardiquimod and imiquimod promote the proliferation of murine splenocytes, stimulate the activation of splenic T, NK and natural killer T (NKT) cells, increase the cytolytic activity of splenocytes against B16 and MCA-38 tumor cell lines, and enhance the expression of costim...
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PMID: 20543857
PDF is available here.
PDF is available here.
Anesthesia & Analgesia (111)3 2010
Abstract
These findings indicate that lidocaine can directly act on microglia. Lidocaine, by inhibiting the increase of intracellular calcium, also inhibited p38 MAPK activation and attenuated the production of proinflammatory cytokines (including TNF-alpha, IL-1beta, and IL-6), which were triggered by extra...
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PMID: 20686009
PDF is available here.
PDF is available here.