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Adamantane

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101. Supramolecular Probes for Assessing Glutamine Uptake Enable Semi-Quantitative Metabolic Models in Single Cells (PubMed)

Supramolecular Probes for Assessing Glutamine Uptake Enable Semi-Quantitative Metabolic Models in Single Cells We describe a supramolecular surface competition assay for quantifying glutamine uptake from single cells. Cy3-labeled cyclodextrins were immobilized on a glass surface as a supramolecular host/FRET donor, and adamantane-BHQ2 conjugates were employed as the guest/quencher. An adamantane-labeled glutamine analog was selected through screening a library of compounds and validated by cell

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2016 Journal of the American Chemical Society

102. Inhibition of Spinal Ca2+-Permeable AMPA Receptors with Dicationic Compounds Alleviates Persistent Inflammatory Pain without Adverse Effects (PubMed)

effects because of the crucial role of CP-AMPARs in synaptic plasticity. Here we have tested whether the inhibition of spinal CP-AMPARs with dicationic compounds, the open-channel antagonists acting in an activity-dependent manner, can relieve inflammatory pain without adverse effects being developed. Dicationic compounds, N1-(1-phenylcyclohexyl)pentane-1,5-diaminium bromide (IEM-1925) and 1-trimethylammonio-5-1-adamantane-methyl-ammoniopentane dibromide (IEM-1460) were applied intrathecally (i.t

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2016 Frontiers in cellular neuroscience

103. Clinical, epidemiological and virological characteristics of the first detected human case of avian influenza A(H5N6) virus (PubMed)

(H5N1) and A/chicken/Jiangxi/12782/2014(H10N6) viruses, respectively. The six internal genes were homologous to avian influenza A (H5N2) viruses isolated in duck from Jiangxi in China. This H5N6 virus has not gained genetic mutations necessary for human infection and was suggested to be sensitive to neuraminidase inhibitors, but resistant to adamantanes. Epidemiological investigation of the exposure history of the patient found that a live poultry market could be the source place of infection

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2016 Infection, genetics and evolution : journal of molecular epidemiology and evolutionary genetics in infectious diseases

104. Proteasomal degradation of sphingosine kinase 1 and inhibition of dihydroceramide desaturase by the sphingosine kinase inhibitors, SKi or ABC294640, induces growth arrest in androgen-independent LNCaP-AI prostate cancer cells (PubMed)

Proteasomal degradation of sphingosine kinase 1 and inhibition of dihydroceramide desaturase by the sphingosine kinase inhibitors, SKi or ABC294640, induces growth arrest in androgen-independent LNCaP-AI prostate cancer cells Sphingosine kinases (two isoforms termed SK1 and SK2) catalyse the formation of the bioactive lipid sphingosine 1-phosphate. We demonstrate here that the SK2 inhibitor, ABC294640 (3-(4-chlorophenyl)-adamantane-1-carboxylic acid (pyridin-4-ylmethyl)amide) or the SK1/SK2

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2016 Oncotarget

105. Inhibition of Leishmania mexicana Growth by the Tuberculosis Drug SQ109. (PubMed)

Inhibition of Leishmania mexicana Growth by the Tuberculosis Drug SQ109. We report that the tuberculosis drug SQ109 [N-adamantan-2-yl-N'-((E)-3,7-dimethyl-octa-2,6-dienyl)-ethane-1,2-diamine] has potent activity against the intracellular amastigote form of Leishmania mexicana (50% inhibitory concentration [IC50], ∼11 nM), with a good selectivity index (>500). It is also active against promastigotes (IC50, ∼500 nM) and acts as a protonophore uncoupler, in addition to disrupting Ca(2

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2016 Antimicrobial Agents and Chemotherapy

106. Case series: Antidepressant effects of low-affinity and low-trapping NMDA receptor antagonists did not predict response to ketamine in seven subjects (PubMed)

, Non-U.S. Gov't 2016 11 22 England J Psychiatr Res 0376331 0022-3956 0 AZD6925 0 Antidepressive Agents 0 Excitatory Amino Acid Antagonists 0 Receptors, N-Methyl-D-Aspartate 25X51I8RD4 Niacinamide 690G0D6V8H Ketamine PJY633525U Adamantane W8O17SJF3T Memantine IM Adamantane analogs & derivatives therapeutic use Adult Antidepressive Agents therapeutic use Depression drug therapy Excitatory Amino Acid Antagonists therapeutic use Female Humans Ketamine therapeutic use Male Memantine therapeutic use

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2016 Journal of psychiatric research

107. A self-assembled cyclodextrin nanocarrier for photoreactive squaraine (PubMed)

A self-assembled cyclodextrin nanocarrier for photoreactive squaraine Photoreactive squaraines produce cytotoxic oxygen species under irradiation and have significant potential for photodynamic therapy. Herein we report that squaraines can be immobilized on a self-assembled nanocarrier composed of amphiphilic cyclodextrins to enhance their photochemical activity. To this end, a squaraine was equipped with two adamantane moieties that act as anchors for the cyclodextrin vesicle surface

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2016 Beilstein journal of organic chemistry

108. Epoxygenated Fatty Acids Inhibit Retinal Vascular Inflammation (PubMed)

(EDPs), were significantly decreased. Exogenous addition of 11,12-EET or 19,20-EDP when combined with 12-(3-adamantane-1-yl-ureido)-dodecanoic acid (AUDA), an inhibitor of epoxide hydrolysis, inhibited VCAM-1 and ICAM-1 expression and protein levels; conversely the diol product of 19,20-EDP hydrolysis, 19,20-DHDP, induced VCAM1 and ICAM1 expression. 11,12-EET and 19,20-EDP also inhibited leukocyte adherence to human retinal microvascular endothelial cell monolayers and leukostasis in an acute mouse

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2016 Scientific reports

109. Novel Adamantanyl-Based Thiadiazolyl Pyrazoles Targeting EGFR in Triple-Negative Breast Cancer (PubMed)

Novel Adamantanyl-Based Thiadiazolyl Pyrazoles Targeting EGFR in Triple-Negative Breast Cancer The epidermal growth factor receptor (EGFR) is a validated therapeutic target for triple-negative breast cancer (TNBC). In the present study, we synthesize novel adamantanyl-based thiadiazolyl pyrazoles by introducing the adamantane ring to thiazolopyrazoline. On the basis of loss of cell viability in TNBC cells, 4-(adamantan-1-yl)-2-(3-(2,4-dichlorophenyl)-5-phenyl-4,5-dihydro-1H-pyrazol-1-yl

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2016 ACS Omega

110. Acute myocardial infarction, associated with the use of a synthetic adamantyl-cannabinoid: a case report (PubMed)

Acute myocardial infarction, associated with the use of a synthetic adamantyl-cannabinoid: a case report "Legal highs" are novel psychoactive substances that have evaded statutory control. Synthetic cannabinoid compounds with adamantane moieties have recently been identified, which have high potency at target receptors and are undetectable on conventional toxicology testing. However, little is known about any harmful effects, and their potential to cause serious ill health. We describe a case

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2016 BMC pharmacology & toxicology

111. A targeted nanoglobular contrast agent from host-guest self-assembly for MR cancer molecular imaging (PubMed)

and effective cancer molecular MRI. Multiple β-cyclodextrins attached POSS (polyhedral oligomeric silsesquioxane) nanoglobule was used as host molecule. Adamantane-modified macrocyclic Gd(III) contrast agent, cRGD (cyclic RGDfK peptide) targeting ligand and fluorescent probe was used as guest molecules. The targeted host-guest nanoglobular contrast agent cRGD-POSS-βCD-(DOTA-Gd) specifically bond to αvβ3 integrin in malignant 4T1 breast tumor and provided greater contrast enhancement than the corresponding

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2016 Biomaterials

112. Inhibition of Soluble Epoxide Hydrolase Limits Mitochondrial Damage and Preserves Function Following Ischemic Injury (PubMed)

injury caused by myocardial infarction.sEH null and WT littermate mice were subjected to surgical occlusion of the left anterior descending (LAD) artery or sham operation. A parallel group of WT mice received an sEH inhibitor, trans-4-[4-(3-adamantan-1-y1-ureido)-cyclohexyloxy]-benzoic acid (tAUCB; 10 mg/L) or vehicle in the drinking water 4 days prior and 7 days post-MI. Cardiac function was assessed by echocardiography prior- and 7-days post-surgery. Heart tissues were dissected into infarct, peri

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2016 Frontiers in pharmacology

113. Polysaccharide Nanoparticles for Efficient siRNA Targeting in Cancer Cells by Supramolecular pKa Shift (PubMed)

assembly constructed by the dual host‒guest interactions of an adamantane-bis(diamine) conjugate (ADA) with cucurbit[6]uril (CB[6]) and a polysaccharide. The potential application of such biocompatible nanostructure was further implemented by the selective transportation of small interfering RNA (siRNA) in a controlled manner. It is demonstrated that the strong encapsulation of the ADA's diammonium tail by CB[6] not only reduced the cytotoxicity of the nano-scaled vehicle but also dramatically enhanced

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2016 Scientific reports

114. Evolution of hierarchical porous structures in supramolecular guest-host hydrogels (PubMed)

pair adamantane (Ad-HA, guest) and β-cyclodextrin (CD-HA, host), as well as with methacrylate groups to both tether fluorescent agents and to covalently stabilize the material structure. We observed microporous materials in the hydrated state, which temporally arose from initially homogenous hydrogels composed of the two polymers. Independent fluorescent labeling of Ad-HA and CD-HA demonstrated spatiotemporal co-localization, indicative of guest-host polymer condensation on the microscale

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2016 Soft matter

115. KCNE1 induces fenestration in the Kv7.1/KCNE1 channel complex that allows for highly specific pharmacological targeting (PubMed)

for the binding site for adamantane derivatives and their putative access pathway in Kv7.1/KCNE1 channels. The adamantane compounds, exemplified by JNJ303, are highly potent gating modifiers that bind to fenestrations that become available when KCNE1 accessory subunits are bound to Kv7.1 channels. This mode of regulation by auxiliary subunits may facilitate the future development of potent and highly subtype-specific Kv channel inhibitors.

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2016 Nature communications

116. [New attempt in a benefit evaluation]. (PubMed)

0 Glucosides 0 Glycated Hemoglobin A 0 Sulfonylurea Compounds 0 hemoglobin A1c protein, human 6KY687524K glimepiride 9100L32L2N Metformin 9GB927LAJW saxagliptin PJY633525U Adamantane IM Adamantane analogs & derivatives therapeutic use Benzhydryl Compounds therapeutic use Diabetes Mellitus, Type 2 blood drug therapy Dipeptides therapeutic use Drug Therapy, Combination Glucosides therapeutic use Glycated Hemoglobin A analysis Humans Metformin therapeutic use Sulfonylurea Compounds therapeutic use

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2016 MMW Fortschritte der Medizin Controlled trial quality: uncertain

117. The effects and safety of vildagliptin on cardiac function after acute myocardial infarction. (PubMed)

I6B4B2U96P Vildagliptin PJY633525U Adamantane IM Adamantane administration & dosage analogs & derivatives Aged Diabetes Mellitus, Type 2 complications diagnosis drug therapy Echocardiography, Doppler Electrocardiography methods Female Follow-Up Studies Glomerular Filtration Rate drug effects Glycated Hemoglobin A metabolism Heart Function Tests drug effects Humans Incretins administration & dosage Male Middle Aged Myocardial Infarction complications diagnosis drug therapy Natriuretic Peptide, Brain blood

2016 International journal of cardiology Controlled trial quality: uncertain

118. Response to: 'Baseline differences in SAVOR trial'-- prespecified vs. post hoc analysis--a potential source of bias. (PubMed)

Hebrew University Medical Center, Jerusalem, Israel. Scirica B M BM Heart and Vascular Center, Brigham and Women's Hospital, Harvard Medical School, Boston, MA, USA. Bhatt D L DL Heart and Vascular Center, Brigham and Women's Hospital, Harvard Medical School, Boston, MA, USA. eng Letter Comment England Diabetes Obes Metab 100883645 1462-8902 0 Dipeptides 0 Dipeptidyl-Peptidase IV Inhibitors PJY633525U Adamantane IM Diabetes Obes Metab. 2015 Dec;17(12):1202 26094750 Adamantane analogs & derivatives

2016 Diabetes, obesity & metabolism Controlled trial quality: uncertain

119. ACP Journal Club. In at-risk patients with type 2 diabetes, saxagliptin and placebo did not differ for CV events. (PubMed)

Dipeptides 0 Dipeptidyl-Peptidase IV Inhibitors 0 Hypoglycemic Agents PJY633525U Adamantane AIM IM N Engl J Med. 2013 Oct 3;369(14):1317-26 23992601 Adamantane analogs & derivatives Cardiovascular Diseases epidemiology Diabetes Mellitus, Type 2 drug therapy Dipeptides therapeutic use Dipeptidyl-Peptidase IV Inhibitors therapeutic use Female Humans Hypoglycemic Agents therapeutic use Male 2014 1 22 6 0 2014 1 22 6 0 2014 4 1 6 0 ppublish 24445719 1814450 10.7326/0003-4819-160-2-201401210-02009

2014 Annals of Internal Medicine Controlled trial quality: uncertain

120. Primary Care Corner with Geoffrey Modest MD: Immunization Updates

….. But at least it looks good so far. By the way, the breakdown for the first 1698 cases of influenza so far in the US is 54% influenza A (of which 5% were pH1N1, 93% H3N2), 46% influenza B. There have been a handful of variant viruses but of the H3N2 and H1N1 strains. All of the tested viruses were susceptible to neuraminidase inhibitors, but adamantanes (e.g. amanadine) does not work/lots of resistance.​ (Visited 21 times, 1 visits today) Post navigation 27 March 2019 Original EBM Research 23 March 2019

2015 Evidence-Based Medicine blog

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