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Pentamidine

Pentamidine is a potent antiprotozoal medication primarily used in the treatment of Pneumocystis pneumonia, a life-threatening infection common in immunocompromised individuals.
This versatile drug has also demonstrated efficacy against other protozoan parasites, including those responsible for African trypanosomiasis and leishmaniasis.
Pentamidine functions by interfering with the parasite's cellular processes, ultimately leading to their demise.
Its precise mechanism of action is not fully understood, but it is believed to involve disruption of DNA synthesis and energy metabolism.
Ongoing research continues to explore the potential applications of Pentamidine in tackling various protozoan infections, with a focus on optimizing its efficacy and safety profile.
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Most cited protocols related to «Pentamidine»

Anti-Trypanosomal Activity Assay Protocol

Cited 9 times

Test compounds were dissolved in DMSO at 20 or 10 mM except for eflornithine which was dissolved in water and sterilised by filtration. The control drug (pentamidine) was dissolved in DMSO at 100 μM. HMI9-T medium (148.5 μl) was added to column 2 (B2-G2) of a sterile 96-well culture plate. HMI9-T + 1% DMSO (100 μl) was added to all remaining wells. Test compound solutions (1.5 μl) were added to column 2 (B2-G2). Pentamidine was placed on row G of all plates as a control. Threefold serial dilutions were carried out by transferring 50 μl from column 2 to the adjacent column (100 μl). The process was repeated up to column 10. HMI9-T containing 2 × 10³ trypanosomes ml⁻¹ (100 μl) was added to all wells except column 1. HMI9-T (100 μl) was added to column 1. Columns 1 and 11 served as controls without cells and without test compound, respectively. Cells were incubated for 3 days, after which 20 μl 0.5 mM resazurin was added to each well, before measuring fluorescence after 4 h incubation. Data were processed using GRAFIT (version 5.0.4; Erithacus software) and fitted to a 3-parameter equation, where the data are corrected for background fluorescence, to obtain the effective concentration inhibiting growth by 50% (EC₅₀):

y = \frac{y_{max}}{1 + {(i / E C_{50})}^{s}}

where y_max is the uninhibited fluorescence value, i is the inhibitor concentration and s is the Hill slope of the curve.
Measurements for each compound were carried out on 3 separate occasions and the mean weighted to the standard error calculated using the following formulas, where ‘a’ is the standard error of EC₅₀ determination ‘A’, etc.

weighted mean = \begin{array}{c} \underline{(A / a^{2}) + (B / b^{2}) + (C / c^{2})} \\ (1 / a^{2}) + (1 / b^{2}) + (1 / c^{2}) \end{array}

and

error = \begin{array}{c} \underline{(1 / a) + (1 / b) + (1 / c)} \\ (1 / a^{2}) + (1 / b^{2}) + (1 / c^{2}) \end{array}

Jones D.C., Hallyburton I., Stojanovski L., Read K.D., Frearson J.A, & Fairlamb A.H. (2010). Identification of a κ-opioid agonist as a potent and selective lead for drug development against human African trypanosomiasis. Biochemical Pharmacology, 80(10), 1478-1486.

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Publication 2010

Cells Diet, Formula Eflornithine Filtration Fluorescence Pentamidine resazurin Sterility, Reproductive Sulfoxide, Dimethyl Technique, Dilution Trypanosoma

Glucose Metabolism in First-Episode Psychosis

Cited 6 times

People with psychosis (the psychosis group) were recruited at the time of their first clinical contact for psychotic symptoms at a general academic hospital (the Hospital Clinic of Barcelona). As part of the Spanish national health system, the hospital offers psychiatric services for all who live in the surrounding catchment area, Esquerra Eixample, in the city of Barcelona. Esquerra Eixample is a relatively homogeneous middle/upper-middle class neighbourhood in the centre of the city. Although it is also possible to seek private care outside of the assigned catchment area, the Hospital Clinic is a regional referral center for psychosis, and in a survey of 2968 admissions to the emergency department of a large general hospital in an adjoining catchment area, there were no individuals with psychosis from Esquerra Eixample.
The psychosis group had a maximum cumulative (lifetime) antipsychotic exposure of 1 week, and no antipsychotic use in the 30 days prior to the study. Participants with psychosis were allowed to receive anti-anxiety medication (lorazepam) the night before blood was drawn, to a maximum of 3 mg, but not on the day of assessment.
The healthy control group (the control group) were recruited using advertisements. We attempted to match the control group to the psychosis group on BMI, age, gender, smoking habit (average number of cigarettes per day), and residence in the catchment area (yes/no) of the Hospital Clinic. All of the participants were White residents of Spain except for one Asian and one North African person in each of the groups. The control group had no current or prior diagnosis of any Axis I DSM-IV15 psychiatric disorder, after being assessed with the structured clinical interview for Axis I DSM-IV psychiatric disorders (SCID-I).16
Additional inclusion and exclusion criteria for all participants were: age from 18 to 64 years; no history of diabetes or other serious medical or neurological condition associated with glucose intolerance or insulin resistance (e.g. Cushing’s disease); not taking a medication associated with insulin resistance (hydrochlorothiazide, furosemide, ethacrynic acid (available in the USA), metolazone, chlortalidone, beta blockers, glucocorticoids, phenytoin, nicotinic acid, ciclosporine, pentamidine or narcotics); no history of cocaine use in the previous 30 days; and have not previously received an antipsychotic or antidepressant medication. Additional exclusion criteria for the control group were no lifetime diagnosis of schizophrenia or major depressive disorder and no current diagnosis of adjustment disorder. All participants gave informed consent for participation in the study, which was conducted under the supervision of the institutional review boards of the authors’ institutions.
Masked to glucose measures, individuals from the two groups that had been recruited were chosen in such a way to assure good matching as a group on gender, age, BMI and smoking habit, and to have an equal number of people in each group. This entailed omitting 6 people from the psychosis group, primarily because of a lower BMI, as well as 22 people in the control group, for purposes of matching.
A secondary, confirmatory analysis was also conducted in which all of the participants who had been recruited were included, and the matching variables were used as covariates.

Fernandez-Egea E., Bernardo M., Donner T., Conget I., Parellada E., Justicia A., Esmatjes E., Garcia-Rizo C, & Kirkpatrick B. (2009). Metabolic profile of antipsychotic-naive individuals with non-affective psychosis. The British Journal of Psychiatry, 194(5), 434-438.

Publication 2009

Adjustment Disorders Adrenergic beta-Antagonists Anti-Anxiety Agents Antidepressive Agents Antipsychotic Agents Asian Americans BLOOD Chlorthalidone Cocaine Cushing's Disease Cyclosporine Diabetes Mellitus Diagnosis Diagnosis, Psychiatric Epistropheus Ethacrynic Acid Ethics Committees, Research Furosemide Gender Glucocorticoids Glucose Hispanic or Latino Hydrochlorothiazide Insulin Resistance Intolerances, Glucose Lorazepam Major Depressive Disorder Mental Disorders Metolazone Narcotics Nervous System Disorder Niacin North African People Pentamidine Pharmaceutical Preparations Phenytoin Psychotic Disorders Schizophrenia SCID Mice Supervision

Nonmyeloablative Double Umbilical Cord Blood Transplantation

Cited 5 times

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Publication 2015

Acyclovir Alleles Anti-Infective Agents Antigens Bacterial Infections Cells Equus caballus Fluconazole fludarabine Fluoroquinolones Grafts Granulocyte Colony-Stimulating Factor HLA-B Antigens HLA-DRB1 Antigen Immunosuppressive Agents Lymphocyte Immune Globulin, Anti-Thymocyte Globulin Mycoses Neutrophil Patients Pentamidine Pharmacotherapy Pneumocystis carinii Infection Transplantation, Autologous Transplantation, Homologous Treatment Protocols Trimethoprim-Sulfamethoxazole Combination Virus Diseases Voriconazole

Adapted Trypanosoma brucei Strains

Cited 5 times

Bloodstream-form T. b. brucei, strain Lister 427 (s427; MiTat 1.2/BS221), and its derivatives were maintained as previously described.^{16 (link)} Several derivative lines were used: tbat1^−/−,^{14 (link)} B48,^{16 (link)} 2T1,^{31 (link)}aqp2/aqp3 null strains^{32 (link)} and P1000 cells (this paper). Procyclic-form T. b. gambiense STIB 386 wild-type and Cymelarsan-resistant (386MR) lines, and T. b. brucei STIB 247 wild-type and Cymelarsan-resistant (247MR) lines were grown as described previously.^{33 (link)} The P1000 line was generated by further subculturing of bloodstream forms of the B48 line in incrementally increasing concentrations of pentamidine, starting at 75 nM, until the trypanosomes proliferated in 1 μM pentamidine. This process took almost a year of continuous in vitro adaptation (Figure S1a, available as Supplementary data at JAC Online), which was presumably genetic in nature as the resistance phenotype has proven to be completely stable even after storage in liquid nitrogen or transformation to procyclic cells. There was no apparent in vitro growth defect associated with the P1000 adaptations (Figure S1b, available as Supplementary data at JAC Online). The STIB 900 line is T. b. rhodesiense, originally isolated from a human patient in Tanzania, and was adapted in vitro for resistance to pentamidine (STIB 900-P) or melarsoprol (STIB 900-M).^{34 (link)}

Munday J.C., Eze A.A., Baker N., Glover L., Clucas C., Aguinaga Andrés D., Natto M.J., Teka I.A., McDonald J., Lee R.S., Graf F.E., Ludin P., Burchmore R.J., Turner C.M., Tait A., MacLeod A., Mäser P., Barrett M.P., Horn D, & De Koning H.P. (2013). Trypanosoma brucei aquaglyceroporin 2 is a high-affinity transporter for pentamidine and melaminophenyl arsenic drugs and the main genetic determinant of resistance to these drugs. Journal of Antimicrobial Chemotherapy, 69(3), 651-663.

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Publication 2013

Acclimatization Blood Circulation Cells Cymelarsan derivatives Homo sapiens Melarsoprol Natural Childbirth Nitrogen Patients Pentamidine Phenotype Strains Trypanosoma

Evaluating Inhibitors of T. brucei

Cited 5 times

Flasks of T. brucei were seeded at 1 × 10⁴ cells ml⁻¹ and incubated in the presence of the known inhibitors pentamidine and eflornithine, and the LOPAC hit (+)-U50,488 for 3 days. Flasks were set up in triplicate for each inhibitor at multiples of EC₅₀ along with 3 control flasks with no inhibitor added. Pentamidine and (+)-U50,488 were added in DMSO in a volume of 0.1% of the culture. Eflornithine was dissolved directly in HMI9-T medium and sterilised by 0.22 μM filtration before diluting into the cell culture. Cell densities were determined at intervals using a haemocytometer and generation times calculated using GraFit (version 5.0.13; Erithacus software) using the following equation:

N = N_{0} 2^{t / g}

where N₀ and N are the number of cells at time zero and time t, respectively, and g is the time per generation. For low cell densities, samples were concentrated 150-fold by centrifugation and resuspension in an appropriate volume of medium.

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Publication 2010

Cell Culture Techniques Cells Centrifugation Eflornithine Filtration inhibitors Pentamidine Sulfoxide, Dimethyl

Most recents protocols related to «Pentamidine»

Assessing Gut Microbiome Changes in Mice

A total of 132 fecal samples were collected from female mice (n = 66) of the C57Bl/6 strain (Charles River, Calco, LC, Italy) and included in the experimental set reported in Figure 1. All procedures for animal housing and maintenance were performed in compliance with previous studies [46 (link),47 (link),48 (link)]. The age of the animals at the start of the study was between 8 and 12 weeks. The mice were monitored daily, and fecal samples were collected every 15 days for the S100B assay and 16S amplicon sequencing analysis. In order to test the effect of Pentamidine (PTM), a S100B inhibitor, as indicated in Figure 2, PTM was administered intraperitoneally (4 mg/kg) to 25 mice (50 fecal samples) vs. 28 untreated controls (as a part of the previous experimental set involving a total of 66 animals), following a previously established protocol [47 (link)]. Additionally, in a pilot test, 300 µL of a solution (phosphate-buffered saline—PBS) containing 200 µg of S100B (Sigma, St. Louis, MO, USA) or of vehicle (phosphate-buffered saline—PBS) was orally administered, respectively, to 3 and 2 C57Bl/6 mice. After 15 days, fecal samples (n = 10) were collected and analyzed for microbiota biodiversity.

Romano Spica V., Valeriani F., Orsini M., Clementi M.E., Seguella L., Gianfranceschi G., Di Liddo R., Di Sante G., Ubaldi F., Ria F., Esposito G, & Michetti F. (2023). S100B Affects Gut Microbiota Biodiversity. International Journal of Molecular Sciences, 24(3), 2248.

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Publication 2023

Animals Biological Assay Feces Females Mice, House Mice, Inbred C57BL Microbial Community Pentamidine Phosphates Rivers Saline Solution Sequence Analysis Strains

Cytotoxicity Assay Protocol for Drugs

EC₅₀ was determined using AlamarBlue in 96-well plates [76 (link)]. All drugs were titrated in two-fold dilutions: Suramin from 1.56 to 400 nM, Pentamidine from 0.98 to 250 nM, Trypan Blue from 0.2 to 50 nM, Ponceau S from 0.39 to 100 nM and CiB from 0.98 to 250 nM. Drug exposure was for 72 hours and AlamarBlue incubation overnight. Plates were read on an Infinite 200Pro plate-reader (Tecan) with the following parameters: Excitation 530nm; emission 585 nm; filter cut-off 570 nm. Data were analysed in GraphPad PRISM. Asymmetric confidence intervals (95% CI) were calculated where possible and statistical significance of each EC₅₀ shift assessed by confidence interval overlap.

Makarov A., Began J., Mautone I.C., Pinto E., Ferguson L., Zoltner M., Zoll S, & Field M.C. (2023). The role of invariant surface glycoprotein 75 in xenobiotic acquisition by African trypanosomes. Microbial Cell, 10(2), 18-35.

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Publication 2023

Alamar Blue Pentamidine Pharmaceutical Preparations ponceau S prisma Suramin Technique, Dilution Trypan Blue

Antileishmanial Activity Screening

Promastigote forms of L. amazonensis in the log growth phase (10^e6 parasites/mL) were added to 96-well plates and incubated in sextuplicate with the test samples (0.25–10.0 µg/mL). The microplates were incubated at 26 °C for 72 h. Cell viability was assessed by adding 5 mg/mL of MTT ([3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] (Sigma-Aldrich^® SP/Brazil) [20 ]. Results were expressed as the half-maximal inhibitory concentration (IC₅₀) calculated by a nonlinear dose–response regression curve using the statistical program GraphPad PRISM 5.0. Pentamidine (Sigma-Aldrich ^® SP/Brazil; 0.25–10 µg/mL) was used as a positive control, and pure Schneider culture medium was used as a negative control.

Lourenço E.M., Di Iório J.F., da Silva F., Fialho F.L., Monteiro M.M., Beatriz A., Perdomo R.T., Barbosa E.G., Oses J.P., de Arruda C.C., de Souza Júdice W.A., Rafique J, & de Lima D.P. (2023). Flavonoid Derivatives as New Potent Inhibitors of Cysteine Proteases: An Important Step toward the Design of New Compounds for the Treatment of Leishmaniasis. Microorganisms, 11(1), 225.

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Publication 2023

Bromides Cell Survival Culture Media L Forms Parasites Pentamidine prisma Psychological Inhibition

Trypanocidal Assay of Compounds

The extract and the purified compounds were cultured and tested against T. b. brucei, and T. congolense exactly as described previously, using a resazurin-based assay [16 (link),17 (link)]. The T. b. brucei strains were a standard drug-sensitive lab strain, Lister 427 (wild-type) [47 (link)] and the derived cell line B48 was developed from the wild-type by gene deletion of the drug transporter TbAT1 followed by in vitro adaptation to pentamidine [48 (link)], leading to the further loss of the gene encoding TbAQP2 [49 (link)], rendering it highly resistant to the diamidine and melaminophenyl arsenical classes of trypanocides. The T. congolense strains were the lab strain IL3000 and its diminazene-adapted clone 6C3 [50 (link)]. All EC₅₀ values presented are the average of at least three independent determinations.

Alenezi S.S., Alenezi N.D., Ebiloma G.U., Natto M.J., Ungogo M.A., Igoli J.O., Ferro V.A., Gray A.I., Fearnley J., de Koning H.P, & Watson D.G. (2023). The Activity of Red Nigerian Propolis and Some of Its Components against Trypanosoma brucei and Trypanosoma congolense. Molecules, 28(2), 622.

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Publication 2023

Arsenicals Biological Assay Cell Lines Clone Cells Diamidine Diminazene Gene Deletion Genes Membrane Transport Proteins Pentamidine Pharmaceutical Preparations resazurin Strains Trypanocidal Agents

Compound Screening in Cardiomyocytes

Pentamidine, dofetilide, nifedipine and doxorubicin were purchased from Sigma-Aldrich. The 10 mM stock solutions were prepared in dimethyl sulfoxide (DMSO). Drug dilutions were performed in pre-warmed (37 °C) cardiomyocytes medium. Data of control with DMSO are reported in Supplementary Fig. S2.

Iachetta G., Melle G., Colistra N., Tantussi F., De Angelis F, & Dipalo M. (2023). Long-term in vitro recording of cardiac action potentials on microelectrode arrays for chronic cardiotoxicity assessment. Archives of Toxicology, 97(2), 509-522.

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Publication 2023

dofetilide Doxorubicin Myocytes, Cardiac Nifedipine Pentamidine Pharmaceutical Preparations Sulfoxide, Dimethyl Technique, Dilution

Top products related to «Pentamidine»

Pentamidine by Merck Group

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Pentamidine is a chemical compound used as a laboratory reagent. It has a molecular formula of C19H24N2O2 and is a white crystalline powder. Pentamidine is commonly used in research applications, but a detailed description of its core function is not available while maintaining an unbiased and factual approach.

Lsr 2 flow cytometer by BD

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The BD LSR II flow cytometer is a laboratory instrument designed to analyze and sort cells or particles in a fluid sample. It utilizes laser technology to detect and measure various properties of the cells or particles, providing data on their size, granularity, and fluorescent characteristics.

Resazurin sodium salt by Merck Group

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Resazurin sodium salt is a chemical compound commonly used as an indicator in various laboratory applications. It is a redox-sensitive dye that changes color based on the oxidation-reduction state of the surrounding environment. When used in cell culture systems, resazurin can be employed as a viability and cytotoxicity assay to measure cellular metabolic activity.

Dimethyl sulfoxide (dmso) by Merck Group

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DMSO is a versatile organic solvent commonly used in laboratory settings. It has a high boiling point, low viscosity, and the ability to dissolve a wide range of polar and non-polar compounds. DMSO's core function is as a solvent, allowing for the effective dissolution and handling of various chemical substances during research and experimentation.

Facsdiva software by BD

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Miltefosine by Merck Group

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Miltefosine is a pharmaceutical compound used as an anti-parasitic agent. It functions as an alkylphosphocholine and has demonstrated activity against various protozoan parasites.

Annexin 5 fluos staining kit by Roche

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The Annexin-V-FLUOS Staining Kit is a laboratory product designed for the detection and quantification of apoptosis. It provides a sensitive and reliable method for the assessment of apoptosis in cell cultures and samples. The kit contains Annexin-V-FLUOS, a fluorescent conjugate that binds to phosphatidylserine, a marker of apoptotic cells. The kit also includes propidium iodide, a dye that stains necrotic cells. This combination of reagents allows for the identification and differentiation of early apoptotic, late apoptotic, and necrotic cells.

Amphotericin b by Merck Group

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Amphotericin B is a laboratory reagent used as an antifungal agent. It is a macrolide antibiotic produced by the bacterium Streptomyces nodosus. Amphotericin B is commonly used in research and biomedical applications to inhibit the growth of fungi.

Resazurin by Merck Group

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Resazurin is a redox-sensitive dye that can be used as a non-toxic indicator in cell viability and proliferation assays. It undergoes a color change from blue to pink upon reduction, which can be measured using spectrophotometric or fluorometric methods.

M199 medium by Merck Group

Sourced in United States, Germany, United Kingdom, Japan, Israel

M199 medium is a cell culture medium developed for the maintenance and growth of a variety of cell types. It provides a balanced formulation of essential nutrients, vitamins, and other components required for cell proliferation and survival in vitro.

What is Pentamidine and how is it used?

Pentamidine is a potent antiprotozoal medication primarily used in the treatment of Pneumocystis pneumonia, a life-threatening infection common in immunocompromised individuals. This versatile drug has also demonstrated efficacy against other protozoan parasites, including those responsible for African trypanosomiasis and leishmaniasis. Pentamidine functions by interfering with the parasite's cellular processes, ultimately leading to their demise. Its precise mechanism of action is not fully understood, but it is believed to involve disruption of DNA synthesis and energy metabolism.

What are some common usage challenges with Pentamidine?

Pentamidine can be challenging to use due to its potential side effects, which can include hypoglycemia, hypotension, and nephrotoxicity. Careful monitoring and dosage adjustment are often required to mitigate these risks, particularly in patients with underlying medical conditions. Additionally, Pentamidine has a narrow therapeutic window, meaning that the difference between an effective and a toxic dose is relatively small, necessitating close supervision by healthcare professionals.

Are there different variations or types of Pentamidine?

Yes, there are several variations of Pentamidine that have been developed. These include the pentavalent organic arsenical compound, which has a slightly different chemical structure, as well as various salt forms of Pentamidine, such as the isethionate and mesylate salts. These different formulations may have slightly different pharmacokinetic properties and may be preferred for specific applications or patient populations.

What are some of the specific applications of Pentamidine?

In addition to its primary use in treating Pneumocystis pneumonia, Pentamidine has demonstrated efficacy in the management of other protozoan infections, such as African trypanosomiasis (also known as sleeping sickness) and leishmaniasis. It has also been explored as a potential treatment for other conditions, including diabetes insipidus and certain types of cancer, although its use in these areas is less established.

How can PubCompare.ai assist with Pentamidine research?

PubCompare.ai allows you to screen protocol literature more efficiently and leverage AI to pinpoint critical insights. The platform can help researchers identify the most effective protocols related to Pentamidine for their specific research goals. PubCompare.ai's AI-driven analysis can highlight key differences in protocol effectiveness, enabling researchers to choose the best option for reproducibility and accuracy in their Pentamidine research efforts.

More about "Pentamidine"

Pentamidine is a powerful antiprotozoal medication primarily used to treat Pneumocystis pneumonia, a life-threatening infection common in immunocompromised individuals.
This versatile drug has also demonstrated efficacy against other protozoan parasites, including those responsible for African trypanosomiasis and leishmaniasis.
Pentamidine functions by interfering with the parasite's cellular processes, ultimately leading to their demise.
Its precise mechanism of action is not fully understood, but it is believed to involve disruption of DNA synthesis and energy metabolism.
Ongoing research continues to explore the potential applications of Pentamidine in tackling various protozoan infections, with a focus on optimizing its efficacy and safety profile.
Researchers often utilize flow cytometry techniques, such as the BD LSR II flow cytometer, to analyze the effects of Pentamidine on protozoan cells.
Resazurin sodium salt, a fluorescent dye, is commonly used in these studies to assess cell viability and proliferation.
Dimethyl sulfoxide (DMSO) is frequently employed as a solvent for Pentamidine and other compounds in experimental settings.
In addition to Pentamidine, other antiprotozoal drugs like Miltefosine and Amphotericin B are also being investigated for their potential to combat various protozoan infections.
The Annexin-V-FLUOS Staining Kit is a useful tool for evaluating apoptosis, or programmed cell death, in protozoan cells exposed to these medications.
Experince the futuure of scientific research with PubCompare.ai, a platform that can help researchers optimize their Pentamidine studies by locating relevant protocols from literature, pre-prints, and patents.
By leveraging AI-driven comparisons, researchers can identify the best protocols and products, enhancing the reproducibility and accuracy of their Pentamidine research efforts.