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Carbenoxolone

Carbenoxolone is a synthetic derivative of glycyrrhetinic acid, a compound found in licorice root.
It has been studied for its potential therapeutic applications, particularly in the treatment of gastrointestinal disorders and inflammatory conditions.
Carbenoxolone is believed to exert its effects through a variety of mechanisms, including the inhibition of 11β-hydroxysteroid dehydrogenase, an enzyme involved in the metabolism of corticosteroids.
Research has also sugested that carbenoxolone may have antiviral, neuroprotective, and anti-fibrotic properties.
While the exact mechanisms of action and clinical efficacy of carbenoxolone are still being investigated, this compound continues to be a subject of interest in the field of biomedical research.

Most cited protocols related to «Carbenoxolone»

Independent groups of rats were orally administered juanislamin or carbenoxolone (the reference compound) at different doses in a volume of 0.5 mL/100 g. Juanislamin was suspended in 0.05% Tween 80 and applied at 1–30 mg/kg. Carbenoxolone was dissolved in distilled water and delivered at 1–100 mg/kg. At 30 min post-treatment, 1 mL of ethanol was orally applied to all animals, regardless of weight. The animals were sacrificed 2 h later and the stomachs were immediately dissected, filled with 2% formaldehyde, and then placed in a container with the same solution for 5 min. Subsequently, each stomach was opened along the greater curvature and the area of the lesions was blindly measured by using a stereoscopic microscope (×10) equipped with an ocular micrometer. The sum of the area of the lesions of each stomach represents the ulcer index. Gastroprotection (%) was calculated according to:
where UIC and UIT are the ulcer indexes of the control and experimental groups, respectively [21 (link)].
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Publication 2020
Animals Carbenoxolone Ethanol Eye Formaldehyde Microscopy Rattus norvegicus Stomach Tween 80 Ulcer
All experiments were designed with equal-sized groups (n = 6) that were predetermined based on our previous studies [13 (link),14 (link),21 (link),48 (link)]. All values are expressed as mean ± standard deviation (SD), and a p-value less than 0.05 was considered statistically significant. Analyses were performed in IBM SPSS for Windows, Version 25 (IBM Corp., Armonk, NY, USA) and BellCurve for Excel ver. 3.00 (Social Survey Research Information Co., Ltd., Tokyo, Japan). The concentration-dependent effects of the local administration of MK801 (1, 10, and 50 μM) and CLZ (30, 100, and 300 μM) on extracellular levels of l-glutamate and GABA were compared using a linear mixed effects model (LME) (IBM SPSS), followed by Tukey’s post hoc test (BellCurve) when the F-value of the concentration factor was significant (Figure 1, Figure 2, Figure 3 and Figure 4). The effects of MK801, CLZ, LY341495, (RS)-α-cyclopropyl-4-phosphonophenyl glycine (CPPG), (S)-4-carboxyphenylglycine (CPG), and carbenoxolone (CBX) on an extracellular l-glutamate level were compared using LME, followed by Tukey’s post hoc test when the F-value of the drug factor was significant (Figure 5 and Figure 6). Particularly, the effect of the local administration of CPPG into the mPFC on the biphasic kinetics of l-glutamate release induced by CLZ was analyzed by LME followed by Tukey’s post hoc test when the F-value is the reciprocal factor of CPPG × time (Figure 5A,D). The concentration-dependent effects of CLZ on basal and on cystine- and K+-evoked astroglial l-glutamate release from primary cultured astrocytes were analyzed using logistic regression analysis (BellCurve) (Figure 7). The data and statistical analysis comply with the recommendations on experimental design and analysis in pharmacology [54 (link)].
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Publication 2019
4-carboxyphenylglycine Astrocytes Carbenoxolone Cystine F Factor gamma Aminobutyric Acid Glutamate Glycine Glycine Effect Kinetics LY 341495 MK-801 Pharmaceutical Preparations
Fluorescence recovery after photobleaching (FRAP) measurements were made on an Olympus inverted microscope with a confocal laser scanning module (Olympus FluoView1000) as described previously.22 (link) Briefly, human citrated whole blood was incubated with calcein AM (2μg/ml) (Sigma Aldrich) for 20 minutes at 30°C, with exposure to gap junction blockers [100μg/ml 37,43Gap2723 (link); 100μM carbenoxolone or 18β-glycyrrhetinic acid (18β-GA)]; or appropriate control during the final 10 minutes. The blood was then perfused over a collagen (100μg/ml)-coated cover slip in a laminar flow chamber at a shear rate of 1000s−1 and thrombi were allowed to form for 3 minutes. The unbound dye and free blood cells were washed away by perfusing platelet poor plasma for 2 minutes. After confirming the absence of free dye, thrombi were selected via a 60X oil immersion objective lens (UPLSAPO 60XO, NA 1.35, UK) and an 8μm diameter circular region at the centre of the thrombus was exposed to high intensity 488nm laser light for 300 milliseconds to achieve 85% photobleach of fluorescence. Fluorescence images were continuously acquired 8 seconds before and 72 seconds after photobleach. Five thrombi were analysed for each of 4 donors for each of the gap junction blockers. A 40mW multiline argon laser was used for both imaging and photobleach, with outputs of 0.8% and 20% respectively of the 488nm line. Average fluorescence intensities for bleached, non-bleached, and background regions were recorded for each time point. Fluorescence signals were corrected for background and steady loss of signal due to imaging illumination and expressed as F/F0 ratios to normalise fluorescence levels (F) against starting fluorescence (F0). Fluorescence intensities were measured using FluoView software and further analysed using Slidebook5 software (Intelligent Imaging Innovations).
Publication 2012
Argon Ion Lasers BLOOD Blood Cells Blood Platelets Carbenoxolone Collagen Donors Fluorescence fluorexon Gap Junctions Glycyrrhetinic Acid Homo sapiens Innovativeness Lens, Crystalline Light Microscopy Neoplasm Metastasis Plasma Submersion Thrombus
Intrinsic membrane properties of BF GABAergic or PV+ neurons were characterized using our previously described protocols (Brown et al., 2006 (link), 2008b (link)). A series of 1-second long hyperpolarizing and depolarizing current pulses were applied in current-clamp from the resting membrane potential (RMP). The first hyperpolarizing step was adjusted so that the negative peak of the membrane potential during the step reached −100 mV. Progressively more depolarizing current steps (in increments one-fifth the size of the initial step) were applied until the firing rate did not increase further. The percentage depolarizing sag was determined from the largest hyperpolarizing step as 100- [((steady state voltage at end of the step - RMP)/(peak voltage - RMP)) * 100]. To characterize hyperpolarization-activated inward currents under voltage-clamp, neurons were held at −60 mV and voltage steps from − 120 mV to −60 mV with a 10-mV increment were applied with a 10-second interval. To confirm the involvement of HCN channels in the depolarizing sag under current-clamp or the slowly developing inward current in voltage-clamp we bath-applied either the nonspecific blocker CsCl (2 mM) or the more specific agent ZD7288 (4-(N-ethyl-N-phenylamino)-1,2-dimethyl-6-(methylamino) pyrimidinium chloride, 50 μM; Ascent Scientific, Cambridge, MA). To test whether “spikelets” were due to electrical coupling we bath-applied the gap junction blocker carbenoxolone (150 μM; Sigma). Data are presented as mean ± standard error of the mean (SEM). Electrophysiological data were analyzed using pClamp 9 software (Axon Instruments, Burlingame, CA). The depolarizing sag during hyperpolarizing current pulses was fit using the Standard exponential curve fitting function (Chebyshev method) of Clampfit, with a fitting coefficient ≥0.995 being accepted as a good fit to the data. If a single exponential function did not give a good fit to the data then a second exponential function was added. Drug effects were tested using Student's t-test. P < 0.05 was considered significant.
Publication 2013
ARID1A protein, human Axon Bath Carbenoxolone cesium chloride Chlorides Electricity Gap Junctions Membrane Potentials Neurons Pulses Tissue, Membrane ZD 7288
Bone marrow was flushed from femurs and tibias of mice at specified ages and pooled between like groups. Cells were immediately seeded into six-well plates at 1 × 107 cells per well, 12-well plates on type 1 collagen–coated glass coverslips at 4 × 106 cells per well, or 96-well plates at 5 × 105 cells per well in basal culture medium (a-MEM, 20% FBS, 1% antibiotic/ antimycotic [Invitrogen, Carlsbad, CA, USA; #15240–062], 1% nonessential amino acids), osteogenic culture medium (basal culture medium + 50 µg/mL ascorbic acid, 10 mM beta glycerol phosphate, ±10−7 M dexamethasone [Dex], as indicated), or adipogenic culture medium (basal culture medium +1 µM rosiglitazone, Sigma-Aldrich). Media were changed every 3 days after seeding, and BMSC were selected by their ability to adhere to the plate after the first 3 days in culture. BMSC were cultured for up to 21 days in osteogenic medium to promote osteoblastic differentiation. In a subset of experiments, cells were exposed to 5 µM carbenoxolone during osteogenic culture, as described.(33 (link),34 (link)) Demarrowed cortical bone diaphyses were digested with collagenase as described to isolate cortical bone osteoblasts.(35 (link)) Cells were grown for 6 days in culture medium (a-MEM, 5% FBS, 5% calf serum [Hyclone Laboratories, Logan, UT, USA], 1% penicillin/streptomycin [Gibco, Grand Island, NY, USA]) before protein extracts were made.
Publication 2015
Acids Adipogenesis Amino Acids Antibiotics beta-glycerol phosphate Bone Marrow Carbenoxolone Cells Collagenase Collagen Type I Compact Bone Culture Media Dexamethasone Diaphyses Femur Mus Osteoblasts Osteogenesis Penicillins Proteins Rosiglitazone Serum Streptomycin Tibia

Most recents protocols related to «Carbenoxolone»

Tyrode solution contained (in mM) 140 NaCl, 5 KCl, 2.5 CaCl2, 2 MgCl2, and 10 HEPES. The standard extracellular solution for voltage-clamp experiments contained (in mM) 140 TEA-methane-sulfonate, 2.5 CaCl2, 2 MgCl2, 1 4-aminopyridine, 10 HEPES, and 0.002 tetrodotoxin. For the experiments described in Figs. 1 and 2, the extracellular solution also contained 0.33% DMSO. The standard pipette solution contained (in mM) 120 K-glutamate, 5 Na2-ATP, 5 Na2-phosphocreatine, 5.5 MgCl2, 5 glucose, and 5 HEPES. For measurements of rhod-2 Ca2+ transients, it also contained 15 EGTA, 6 CaCl2, and 0.1 rhod-2. For measurements with fluo-4, isolated muscle fibers were incubated for 30 min in the presence of Tyrode solution containing 10 μM fluo-4 AM. All solutions were adjusted to pH 7.20. The Ringer solution used for muscle force measurements contained (in mM) 140 NaCl, 6 KCl, 3 CaCl2, 2 MgCl2, and 10 HEPES, adjusted to pH 7.40.
Probenecid was prepared as a 0.3 M aliquoted stock solution in DMSO and used in the extracellular solution at 0.5, 1, or 2 mM. Carbenoxolone was prepared as a 10 mM stock solution in the extracellular solution and used at 0.1 mM. These concentrations were chosen on the basis of their effectiveness and wide use to block Panx1 channels throughout the literature (e.g., Dahl et al., 2013 (link)). When testing the effect of either probenecid or carbenoxolone using the preincubation protocol (Figs. 1 and 2), fibers were bathed in the drug-containing extracellular solution from the beginning of the intracellular dialysis with the rhod-2-containing solution (i.e., 30 min before taking measurements). The 10panx1 peptide and the scrambled control peptide (10panx1SCr) were tested under the same conditions at 200 µM while the P2Y2 antagonist AR-C 118925XX was tested at 10 µM. All chemicals and drugs were purchased from Sigma-Aldrich, except for tetrodotoxin (Alomone Labs), rhod-2 and fluo-4 (Thermo Fisher Scientific), and AR-C 118925XX (TOCRIS—Bio-Techne).
In vitro fluorescence measurements using droplets of a solution containing (in mM) 120 K-glutamate, 10 HEPES, 15 EGTA, 6 CaCl2, and 0.1 rhod-2, with or without probenecid, showed that fluorescence intensity in the presence of 1 mM probenecid corresponded to 1.09 ± 0.12% (n = 6) the intensity in the absence of probenecid, excluding an interaction of the drug with the dye to explain the effect on resting fluorescence in muscle fibers.
Publication 2023
Aminopyridines Carbenoxolone Cardiac Arrest Dialysis Solutions Drug Interactions Egtazic Acid Figs Fluo 4 Fluorescence Glucose Glutamate HEPES Magnesium Chloride methanesulfonate Muscle Tissue P2RY2 protein, human Peptides Pharmaceutical Preparations Phosphocreatine Probenecid Protoplasm rhod-2 Ringer's Solution Sodium Chloride Sulfoxide, Dimethyl Tetrodotoxin Transients Tyrode's solution
During the experiments, muscle fibers and muscles were randomly assigned to the control and test (probenecid, carbenoxolone, or other treatment) groups. When comparing results between control muscle fibers and muscle fibers treated under a given pharmacological condition, groups of fibers from the same animal were considered as technical replicates and statistical comparison was achieved using a nested analysis, as described by Eisner (2021) (link). When determining the extent of change in a given parameter produced by the acute application of a pharmacological compound (with the initial measurement from the same muscle or muscle fiber being the control value), each experiment was considered independent, and statistics were based on the number of fibers.
The number of necessary experiments was estimated on the basis of our previous experience with each protocol. A sample size estimation (with α = 0.05 and β = 0.80) was made from our pilot data showing a 55% reduction of maximum SR Ca2+ release in the presence of 1 mM probenecid, giving a total of six per group.
Experiments on single muscle fibers and isolated muscles require a great extent of specific expertise, preparation, dexterity, and watchfulness, with the operator on duty being in charge from beginning to end. Under these conditions, further complexification by blinding was not implemented to prevent any related risk of misidentification error. Blinding would also have required two dedicated persons on duty on each experimental day, which was not routinely possible.
Data and statistical analysis complied with the recommendations on experimental design and analysis in pharmacology (Curtis et al., 2018 (link)). Electrophysiological and fluorescence data were processed with Clampfit 10.0 (Molecular Devices) and ImageJ software (National Institutes of Health), respectively, and Origin 7.0 (OriginLab Corporation). Statistical analysis was performed with GraphPad Prism 9.1 (GraphPad Software). Data values are presented as means ± SD for either n muscle fibers or n muscles. Individual datapoints for the parameters measured from each and every muscle/fiber tested are also presented in the figures. Statistical comparison was made only on measurements conducted under a given experimental condition on a minimum group of either five distinct muscles or five distinct muscle fibers. No search was made for outliers within datasets. The level of probability (p) deemed to constitute the threshold for statistical significance was defined as P < 0.05. Exact P values are indicated on the graphs in the figures.
For single muscle fiber experiments designed to test the effect of chronic exposure to a pharmacological compound (Figs. 1, 2, and 4), the normality of the distribution of each Boltzmann fit parameter was assessed using Shapiro-Wilk test, and the statistical difference between the control group and either the probenecid group or the carbenoxolone group was determined using the hierarchical (nested) analysis or linear mixed modeling described by Eisner (2021) (link), taking into account the number of fibers from each mouse.
For single muscle fiber experiments designed to test the effect of acute exposure to probenecid, statistical differences between the control group and the probenecid group in terms of the extent of change in (1) baseline rhod-2 fluorescence, (2) resting membrane conductance, and (3) peak SR Ca2+ release flux during the test period and after wash-out, was assessed using unpaired Mann–Whitney Wilcoxon test (Figs. 6 and 9).
For muscle force measurements in control conditions and in the presence of probenecid, a Mann–Whitney Wilcoxon test was used to compare the amplitude of tetanic force at a given time point of the experiment. Friedman’s nonparametric test for repeated measurements followed by Dunn’s post-hoc test was used to compare the time-dependent changes in the tetanic force amplitude in the two groups.
Publication 2023
Animals Carbenoxolone Fibrosis Figs Fluorescence Medical Devices Mice, House Muscle Tissue Myopathy prisma Probenecid rhod-2 Tetanus Tissue, Membrane
To investigate the electrical coupling between dendrites of SNs in single basiconic sensilla (Takeichi et al., 2018 (link); Uebi et al., 2022 (link)), we used the general gap junction blocker, carbenoxolone (CBX) (Miriyala et al., 2018 (link)). 3 μL of ant saline (control group) or 10 mM CBX solution (CBX group) was injected into the hemolymph of the ice-anesthetized ant. After incubation for 5–9 h at room temperature, ants were anesthetized again and attached to the acrylic plate for SSRs. In each recording, we extracted waveforms for 2.5 ms before and after the peak of a large amplitude spontaneous spike of a SN and detected all peaks of synchronized spikes within the 5-ms time window. Electrical events were acquired at a sampling rate of 20 kHz, and we defined the spike peak when the waveform potential was increased and decreased for three consecutive sampling points, respectively. In each recording, we counted the number of the large amplitude spontaneous spikes within the 3-s period of recording, and calculated the appearance ratio of the synchronized spikes.
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Publication 2023
Ants Carbenoxolone Dendrites Electricity Gap Junctions Hemolymph Saline Solution Sensilla
Whole cell membrane currents of oocytes were measured using a two-electrode voltage clamp (Gene Clamp 500B, Axon Instruments/Molecular Devices Sunnyvale, CA, USA). Glass pipettes were pulled using a P-97 Flaming/Brown type puller (Sutter, Novato, CA, USA). The recording chamber was perfused continuously with frog Ringer (OR) solution (in mM: 82.5 NaCl, 2.5 KCl, 1 CaCl2, 1 MgCl2, 1 Na2HPO4, and 5 HEPES, pH 7.5). Membrane conductance was determined using voltage pulses, and the pulse-induced current amplitudes were divided by the amplitudes of the voltage steps. For calculation of % inhibition, leak currents were subtracted. Typically, leak currents after the interventions were smaller than at the beginning of the experiment, and this smaller value was used for the subtraction to avoid overestimation of the inhibitory effect. For an independent measure of the leak current, oocytes at the end of the experiment were exposed to 100 µM carbenoxolone, which is known to close Panx1 channels 100%. Oocytes expressing Panx1 were held at −60 mV, and pulses to +60 mV were applied to transiently open the channels by means of the voltage gate. Pulses 5 s in duration were applied at 0.1 Hz for current and conductance measurements.
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Publication 2023
ARID1A protein, human Axon Carbenoxolone Genes HEPES Magnesium Chloride Medical Devices Oocytes Plasma Membrane Psychological Inhibition Pulse Rate Rana Sodium Chloride Tissue, Membrane
We used topical drug application to target local purinergic receptor signaling at the afferents’ meningeal RF level. Drug doses were based on previous studies using local administration and pilot studies in our laboratory. We used Pyridoxalphosphate-6-antagonist, and 2’,3’-O-(2,4,6-Trinitrophenyl)adenosine-5’-triphosphate tetra(triethylammonium) salt (TNP-ATP) to inhibit P2X3 and P2X2,3 receptors. N-[2-[[2-[(2-Hydroxyethyl)amino]ethyl]amino]-5-quinolinyl]-2-tricyclo[3.3.1.13,7]dec-1-ylacetamide dihydrochloride (AZ 10606120) was used to inhibit P2X7, and (3β,20β)-3-(3-Carboxy-1-oxopropoxy)-11-oxoolean-12-en-29-oic acid disodium (carbenoxolone) was employed to inhibit Panx1. All pharmacological agents were purchased from Tocris and diluted in SIF for meningeal application. We first established the level of baseline ongoing activity and mechanosensitivity for 60 min in the presence of the vehicle (SIF). We then evaluated the change in the activity and mechanosensitivity of the afferents in the presence of the drugs for 60 min to ensure a lack of direct inhibitory effect on the afferents before CSD triggering. Post-CSD data was then collected in the presence of the drug or SIF (Figure 1B).
Publication Preprint 2023
2',3'-O-(2,4,6-trinitrophenyl)adenosine 5'-triphosphate Acids Adenosine Triphosphate Administration, Topical Carbenoxolone Cardiac Arrest Meninges Pharmaceutical Preparations Psychological Inhibition Purinoceptor Pyridoxal Phosphate Sodium Chloride Tetragonopterus

Top products related to «Carbenoxolone»

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Carbenoxolone is a laboratory product manufactured by Merck Group. It is a chemical compound used in research applications, though its specific core function is not provided in order to maintain an unbiased and factual approach.
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Carbenoxolone (CBX) is a laboratory compound used for research purposes. It is a synthetic derivative of glycyrrhetinic acid, which is found in licorice root. CBX is commonly used as a tool compound in biological research studies, particularly in the investigation of cellular processes and signaling pathways.
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Probenecid is a laboratory reagent used in the analysis of biological samples. It functions as a uricosuric agent, which helps to increase the excretion of uric acid from the body. Probenecid is commonly used in various biochemical and clinical applications, such as drug interaction studies and research on uric acid metabolism.
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Carbenoxolone is a laboratory reagent used in experimental research. It is a synthetic compound that acts as a glycyrrhizic acid derivative. The primary function of Carbenoxolone is as a gap junction inhibitor, which is used to study cellular communication pathways in various biological systems.
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ATP is a laboratory instrument used to measure the presence and concentration of adenosine triphosphate (ATP) in various samples. ATP is a key molecule involved in energy transfer within living cells. The ATP product provides a reliable and accurate method for quantifying ATP levels, which is useful in applications such as microbial detection, cell viability assessment, and ATP-based assays.
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Fluo-4 AM is a fluorescent calcium indicator used for the detection and measurement of intracellular calcium levels. It functions by binding to calcium ions, which results in an increase in fluorescence intensity. This product is commonly used in various cell-based assays and research applications involving calcium signaling.
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Mefloquine is a synthetic compound used in the production of laboratory equipment. It is a key component in the manufacture of certain types of analytical instruments and devices used for research and testing purposes.
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Indomethacin is a laboratory reagent used in various research applications. It is a non-steroidal anti-inflammatory drug (NSAID) that inhibits the production of prostaglandins, which are involved in inflammation and pain. Indomethacin can be used to study the role of prostaglandins in biological processes.
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Ranitidine is a type of lab equipment used for the measurement and detection of specific chemical compounds. It functions as a tool to analyze and quantify the presence and concentration of these compounds in various samples.
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Apyrase is an enzyme that catalyzes the hydrolysis of ATP and ADP to AMP and inorganic phosphate. It is commonly used in various biochemical and cell biology applications.

More about "Carbenoxolone"

Carbenoxolone, also known as CBX, is a synthetic derivative of glycyrrhetinic acid, a compound found in licorice root.
This versatile compound has garnered significant interest in the field of biomedical research due to its potential therapeutic applications.
One of the primary focus areas for carbenoxolone is its use in the treatment of gastrointestinal disorders and inflammatory conditions.
Carbenoxolone is believed to exert its effects through various mechanisms, including the inhibition of 11β-hydroxysteroid dehydrogenase, an enzyme involved in the metabolism of corticosteroids.
This inhibitory action may contribute to its anti-inflammatory properties.
Beyond its gastrointestinal and anti-inflammatory applications, research has also suggested that carbenoxolone may possess antiviral, neuroprotective, and anti-fibrotic properties.
These additional potential benefits have expanded the scope of carbenoxolone's research and development.
To further optimize carbenoxolone research, tools like PubCompare.ai can be leveraged to enhance reproducibility and accuracy.
This platform allows researchers to easily locate relevant protocols from literature, preprints, and patents, and utilize AI-driven comparisons to identify the best protocols and products.
By leveraging these powerful tools, researchers can take their carbenoxolone optimization to the next level, improving the efficiency and quality of their studies.
Probenecid, ATP, Fluo-4 AM, Mefloquine, Indomethacin, and Ranitidine are some related terms and compounds that may be of interest to researchers working with carbenoxolone.
By incorporating these synonyms and related concepts into the research process, researchers can gain a more comprehensive understanding of the complex landscape surrounding this versatile compound.