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Tadalafil

Tadalafil is a potent and selective phosphodiesterase type 5 (PDE5) inhibitor used to treat erectile dysfunction and pulmonary arterial hypertension.
It works by relaxing the blood vessels, allowing for increased blood flow to the penis or lungs.
Tadalafil is notable for its long duration of action, with effects lasting up to 36 hours.
Careful dosing and monitoring is required, as tadalfil may interact with other medications and have side effects such as headache, flushing, and indigestion.
Researchers can leverage PubCompare.ai's advanced protocol optimization tools to streamline Tadalafil studies, identifying the most reproducible and accurate research methods from published literature, preprints, and patents.

Most cited protocols related to «Tadalafil»

1
Pulmonary Hemodynamics Assessment
Cited 4 times
Echocardiographic analyses were performed using a Vevo770 (VisualSonics). Pulse-wave Doppler of pulmonary outflow was recorded in the parasternal short-axis view at the level of the aortic valve. Baseline measurements were obtained one day prior to placing animals in chambers. PAP was measured with a Millar catheter placed in the main pulmonary artery via the RV; correct placement of the catheter was confirmed by observing a significant rise in diastolic pressure as the catheter moved out of the ventricle. Systemic blood pressure was monitored with another pressure catheter inserted in the femoral artery. Cardiac performance was assessed using a pressure-volume system (Scisense). For analyses, animals were anesthetized using 2% isoflurane and their body temperature was maintained at 37°C. Hemodynamic analyses were performed ~20 – 24 hrs following the final dose of compound (MGCD0103 and MS-275) or 2 hrs post-dosing (tadalafil). Total pulmonary vascular resistance index (PVRI) was calculated as mPAP/cardiac index (CI), where CI = cardiac output/body weight, as described previously 15 (link). For data from all in vivo studies, GraphPad Prism software was used to generate graphs and analyze data. ANOVA with Bonferroni’s post-test (p<0.05) was used to determine statistical differences between groups. Rats presented no health concerns associated with compound treatment. Animals were monitored daily and showed no evidence of paleness in eyes, nose or skin, which are the most common signs of hematological toxicities. Rats were alert and conducted normal activities such as eating, drinking and grooming.
Cavasin M.A., Demos-Davies K., Horn T.R., Walker L.A., Lemon D.D., Birdsey N., Weiser-Evans M.C., Harral J., Irwin D.C., Anwar A., Yeager M.E., Li M., Watson P.A., Nemenoff R.A., Buttrick P.M., Stenmark K.R, & McKinsey T.A. (2012). Selective Class I HDAC Inhibition Suppresses Hypoxia-Induced Cardiopulmonary Remodeling Through an Anti-Proliferative Mechanism. Circulation research, 110(5), 739-748.
Publication 2012
Animals Body Temperature Body Weight Cardiac Output Catheters Echocardiography Epistropheus Eye Femoral Artery Heart Heart Ventricle Hemodynamics Isoflurane Lung MGCD 0103 MS 27-275 neuro-oncological ventral antigen 2, human Nose Pressure Pressure, Diastolic prisma Pulmonary Artery Pulse Rate Rattus norvegicus Skin Tadalafil Valves, Aortic
2
Cavernous Nerve Stimulation and Tadalafil Nanoparticles
Cited 4 times
Rats were first anesthetized via intraperitoneal injection of sodium pentobarbital (35 mg/kg; Abbott Laboratory, Chicago, IL, USA). A cannula was inserted into the carotid artery for systemic pressure (BP). Next, an incision was made in the perineum, the ischiocavernosus muscle removed to expose the corpus cavernosum crus, and a 23-gauge needle was inserted to measure ICP. The changes in ICP and systemic BP were monitored continuously throughout the experiments.
Nanoparticles were applied as a gel to the glans and shaft of the penis and left in place for the duration of the experiment. The nanoparticles were administered as a 50- to 200-μL suspension in 1.5% carboxymethylcellulose (used as a bulking agent). These suspensions represented approximately 10 nMoles NO (steady-state delivery), 50 ng sialorphin, and 1 mg tadalafil.
With the tadalafil nanoparticles, we determined the ICP/BP response following cavernous nerve stimulation before and after administration of the nanoparticles. In order to do this, the cavernous nerves were identified ventrolateral to the prostate gland and carefully isolated. Direct electrostimulation of the cavernous nerve was performed using a delicate stainless steel bipolar hook electrode attached to a multijointed clamp. Each probe was 0.2 mm in diameter with a 1 mm separation between the two poles. Monophasic rectangular pulses were delivered by a signal generator (custom made and with built-in constant current amplifier). Stimulation was performed at 0.75 mA and 4 mA. Following the untreated ICP/BP recording, animals were administered with a 200-μL suspension of the tadalafil nanoparticles. Animals were then stimulated at 0.75 mA and 4 mA at 30-minute intervals after application and the ICP/BP determined.
Han G., Tar M., Kuppam D.S., Friedman A., Melman A., Friedman J, & Davies K.P. (2009). Nanoparticles as a Novel Delivery Vehicle for Therapeutics Targeting Erectile Dysfunction. The journal of sexual medicine, 7(1 Pt 1), 224-233.
Publication 2009
Animals Cannula Carboxymethylcellulose Common Carotid Artery Injections, Intraperitoneal Leg Muscle Tissue Needles Nervousness Obstetric Delivery Penis Pentobarbital Sodium Perineum Pressure Prostate Pulses Rattus sialorphin Stainless Steel Tadalafil
3
Negative Image-Based Modeling of Ligand-Binding Cavities
Cited 3 times
The negative
images or NIB (negative image-based) models of the target proteins’
ligand-binding cavities (Figure 2) were generated using PANTHER0.18.15.22 (link) The cavity centroids were calculated directly using the
ligands present in inputing the protein structures (Figures 1-2; Table 1). The same default
PANTHER settings were utilized for all models, if not specified otherwise.
The NIB model volumes were limited using the ligand distance limit
of 1.5 Å (2.0 Å for the NEU); i.e., the models were not
allowed to grow too far from the area occupied by the co-crystallized
ligands. The box radius option was set to 20.0–27.0 Å
depending on the target protein’s cavity volume.
The
face-centered cubic (FCC) packing method was used with RXRα,
NEU, and tadalafil-bound PDE5 structures, whereas the less dense body-centered
cubic lattice (BCC) packing was selected for COX-2, MR, and sildenafil-bound
PDE5 structures. With COX-2, the lining id angle option was decreased
to 10° to include one positively charged cavity point near the
side-chain oxygen of Gln178 in the model. With MR, the radius for
the charged atoms option was decreased to 0.2 Å, and the exclusion
distance for the charged atoms and their residues was set to 0.4 Å.
This was done to make one end of the NIB model slightly thicker. The
only positively charged cavity point near the main chain oxygen of
Asn306 in the NIB model of RXRα was removed from the negative
image manually as it was considered unconnected with the rest of the
model.
The PANTHER input files, PDB files, and NIB models are
included
in the Supporting Information.
Kurkinen S.T., Lätti S., Pentikäinen O.T, & Postila P.A. (2019). Getting Docking into Shape Using Negative Image-Based Rescoring. Journal of Chemical Information and Modeling, 59(8), 3584-3599.
Publication 2019
Binding Proteins Cuboid Bone Dental Caries Ligands Oxygen Proteins protein S, human PTGS2 protein, human Radius Sildenafil Tadalafil
4
Swine Model of Heart Failure with Aortic Banding
Cited 3 times
HF was induced with aortic banding over a period of 24 weeks as previously reported by our laboratory16, 17, 18 with modifications. These modifications included the use of younger pigs (3 months old) and a reduced afterload (50 mm Hg). Intact male Yucatan miniature swine were matched for body mass (10–15 kg) and cardiac function and divided into 4 experimental groups: nonbanded untreated control (CON; n=6), aortic‐banded untreated HF (HF; n=7), aortic‐banded tadalafil‐treated HF (HF‐TAD; n=8), and aortic‐banded saxagliptin‐treated HF (HF‐SAX; n=8). The aortic band was placed around the ascending aorta (proximal to the brachiocephalic artery) and a systolic trans‐stenotic gradient of ≈50 mm Hg was achieved (50±1, 50±3, 48±2 for HF, HF‐TAD, and HF‐SAX, respectively, P=NS). The aortic band was set under equivalent hemodynamic conditions for all pigs and characterized by a peripheral vascular mean arterial pressure of ≈90 mm Hg (90±1, 92±1, 90±1 for HF, HF‐TAD and HF‐SAX, respectively, P=NS) under anesthesia using phenylephrine (IV 1–3 μg kg−1 min−1) at a heart rate of ≈100 beats/min (96±6, 112±6, and 102±6 for HF, HF‐TAD, and HF‐SAX, respectively, P=NS). One week after aortic banding, treatment with tadalafil (2 mg·kg−1 twice daily, oral; Eli Lily, Indianapolis, IN) or saxagliptin (10 mg·kg−1·day−1, oral; AstraZeneca Diabetes Alliance, Wilmington, DE) began and continued for 23 weeks. Animals were fed a standard diet averaging 15–20 g/kg once daily and water was provided ad libitum. All animal protocols were in accordance with the “Principles for the Utilization and Care of Vertebrate Animals Used in Testing Research and Training” and approved by the University of Missouri Animal Care and Use Committee.
Hiemstra J.A., Lee D.I., Chakir K., Gutiérrez‐Aguilar M., Marshall K.D., Zgoda P.J., Cruz Rivera N., Dozier D.G., Ferguson B.S., Heublein D.M., Burnett J.C., Scherf C., Ivey J.R., Minervini G., McDonald K.S., Baines C.P., Krenz M., Domeier T.L, & Emter C.A. (2016). Saxagliptin and Tadalafil Differentially Alter Cyclic Guanosine Monophosphate (cGMP) Signaling and Left Ventricular Function in Aortic‐Banded Mini‐Swine. Journal of the American Heart Association: Cardiovascular and Cerebrovascular Disease, 5(4), e003277.
Publication 2016
Anesthesia Animals Aorta Arteries Ascending Aorta Diabetes Mellitus Diet Heart Hemodynamics Human Body Lilium Males Phenylephrine Pigs Rate, Heart saxagliptin Stenosis Swine, Miniature Systole Tadalafil Trunks, Brachiocephalic Vertebrates
5
Thermal Analysis of Tadalafil-Repaglinide Coamorphous Mixtures
Cited 2 times
Thermal analyses of the samples were conducted using a differential scanning calorimeter (DSC 204F1, Netzsch, Germany). Calibration of the DSC instrument was carried out using indium as a standard. Sample powders (3–5 mg) were analyzed in open aluminum pans and equilibrated at 25 °C, followed by heating from 25 °C to 330 °C at a heating rate of 10 °C min−1. The value of Tg was calculated using NETZSCH-Proteus software (version 4.2).
The theoretical value of Tg were calculated using the Gordon–Taylor equation (eqn (5)):9,42 (link) where Tg12 is the glass transition temperature of the coamorphous mixture, while Tg1 and Tg2 are the glass transition temperatures of amorphous tadalafil and amorphous repaglinide, respectively. W1 and W2 are the weight fractions of each component in the mixture. K is a correlation coefficient, which can be obtained from the Simha–Boyer rule (eqn (6)): where ρ1 and ρ2 are the respective true densities of the single amorphous components. Densities of 1.24 g cm−3 and 1.14 g cm−3 for tadalafil and repaglinide, respectively, which were determined in triplicate using a helium pycnometer.
Su M., Xia Y., Shen Y., Heng W., Wei Y., Zhang L., Gao Y., Zhang J, & Qian S. (2020). A novel drug–drug coamorphous system without molecular interactions: improve the physicochemical properties of tadalafil and repaglinide. RSC Advances, 10(1), 565-583.
Publication 2019
Aluminum Helium Indium Powder Proteus, salamanders repaglinide Tadalafil Vitrification

Most recents protocols related to «Tadalafil»

1
Treatment of Dermatological Condition with Topical Compounds
Not available on PMC !

Example 12

30 mg of 3-[[(aminocarbonyl)oxy]methyl]-7-methoxy-8-oxo-7-[(2-thienylacetyl)amino]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid 2-diethylaminoethyl ester hydrochloride, 30 mg of diethylaminoethyl acetylsalicylate hydrochloride, 3 mg of diethylaminoethyl [R-(E)]-1-[[[1-[3-[2-(7-chloro-2-quinolinyl)ethenyl]phenyl]-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]thio]methyl]cyclopropaneacetate hydrochloride (an example of a HPP of montelukast), 5 mg of tadalafil HCl (an example of a compound having structure PDE5-I-3, wherein HA is HCl), and 5 mg of isopropyl (E)-3-{6-[(E)-1-(4-methylphenyl)-3-pyrrolidine-1-yl-prop-1-enyl]pyridin-2-yl}prop-2-enoate in 0.5 ml of 25% ethanol was applied to the skin on the thorax of a subject every morning and evening (twice per day) for until the condition was alleviated. Then 30 mg of diethylaminoethyl acetylsalicylate hydrochloride in 0.5 ml of water was applied to the skin on the thorax of a subject every morning and evening (twice per day) to prevent the recurrence of the condition.

US11857545B2. High penetration prodrug compositions and pharmaceutical composition thereof for treatment of pulmonary conditions (2024-01-02). TECHFIELDS PHARMA CO., LTD. [CN]. Inventors: Chongxi Yu [US], Lina Xu [CN].
Full text: Click here
Patent 2024
Acids Asthma Carboxylic Acids Chest Edan Esters Ethanol Lung Diseases montelukast POU2F2 protein, human pyrrolidine Recurrence Skin Tadalafil
2
Systematic Review of Tamsulosin and Tadalafil for LUTS/BPH
This meta-analysis was carried out using the Preferred Reporting Items for
Systematic Reviews and Meta-Analyses (PRISMA) checklist (Moher et al., 2009 ). First, six online
academic databases were searched for papers published in English, with no
publication restrictions, including Medline, Embase, PubMed, Scopus, Web of
Science, and Cochrane Controlled Trials Register until January 2022. The search
keywords were a combination of free text and controlled vocabulary (i.e., MeSH
terms) for each database, including “tamsulosin, tadalafil, LUTS, BPH and
randomized controlled trial (RCT).”
Then, using Endnote X9 software (Clarivate, PA, USA), we deleted duplicates from
the list of literatures retrieved in the first step. The following studies were
excluded: reviews, editorials, book or book chapters, commentaries, conference
papers, brief communications, articles with no complete text, studies that used
qualitative methods only or interventional research. If multiple papers analyzed
the same data set, the article with the most data was selected.
Third, articles were separately reviewed by two researchers who examined the
title and abstract, followed by the full text if the paper matched the inclusion
criteria. A third researcher would include or exclude papers in the event of a
disagreement between the two researchers.
Zhou R., Che X., Zhou Z, & Ma Y. (2023). A Systematic Review and Meta-Analysis of the Efficacy and Safety of Tamsulosin Plus Tadalafil Compared With Tamsulosin Alone in Treating Males With Lower Urinary Tract Symptoms Secondary to Benign Prostrate Hyperplasia. American Journal of Men's Health, 17(1), 15579883231155096.
Publication 2023
Lutein prisma Tadalafil Tamsulosin
3
Mpox Surveillance in Urban Clinics
The following data were extracted for each participant: MVA-BN vaccination, mpox diagnosis, RT–PCR laboratory results, age, geographical district of primary healthcare clinic, population sector, the score for socioeconomic status, history of HIV/AIDS; STIs detected in rectal, pharyngeal or urine PCR tests; blood test for syphilis screening (TPHA) and dispense of HIV-PrEP therapy and PDE5 inhibitors (sildenafil, tadalafil or vardenafil).
The CHS data repositories and the definition of the sociodemographic variables were previously described in published coronavirus disease 2019 studies22 (link). Data were extracted on 29 December 2022.
Wolff Sagy Y., Zucker R., Hammerman A., Markovits H., Arieh N.G., Abu Ahmad W., Battat E., Ramot N., Carmeli G., Mark-Amir A., Wagner-Kolasko G., Duskin-Bitan H., Yaron S., Peretz A., Arbel R., Lavie G, & Netzer D. (2023). Real-world effectiveness of a single dose of mpox vaccine in males. Nature Medicine, 29(3), 748-752.
Publication 2023
3-(2-methoxyphenyl)-5-methoxy-1,3,4-oxadiazol-2(3H)-one Acquired Immunodeficiency Syndrome BLOOD COVID 19 Diagnosis Hematologic Tests MVA vaccine Pharynx Phosphodiesterase 5 Inhibitor Primary Health Care Rectum Reverse Transcriptase Polymerase Chain Reaction Sexually Transmitted Diseases Sildenafil Syphilis Syphilis Serodiagnosis Tadalafil Therapeutics Urinalysis Vardenafil
4
Modeling Phosphodiesterase-5 Enzyme Structure
A model of PDE5 constructed from the crystal structure of tadalafil bound to the catalytic domain of PDE5 was obtained from the protein databank (PDB ID: 1UDT). Schrödinger Suite 2008 was used for molecular modeling studies using the induced fit protocol and parameters described in [31 (link),34 (link)]. The docking protocol and parameters were first validated by docking tadalafil to the PDE5 catalytic domain; they were then used to model SSA docking in the catalytic domain of PDE5.
Tinsley H.N., Mathew B., Chen X., Maxuitenko Y.Y., Li N., Lowe W.M., Whitt J.D., Zhang W., Gary B.D., Keeton A.B., Grizzle W.E., Grubbs C.J., Reynolds R.C, & Piazza G.A. (2023). Novel Non-Cyclooxygenase Inhibitory Derivative of Sulindac Inhibits Breast Cancer Cell Growth In Vitro and Reduces Mammary Tumorigenesis in Rats. Cancers, 15(3), 646.
Full text: Click here
Publication 2023
Catalytic Domain Tadalafil
5
Extracting Data from Pulmonary Hypertension Trials
The data were independently extracted by two investigators directly or indirectly using Engauge Digitizer software (Markmitch), version 4.1, to obtain required data from tables and images. The extracted content mainly included the basic characteristics of the included studies, including first author, publication year, study design type, sample size, sex, age, classification of PAH, WHO-FC, baseline status, tadalafil or sildenafil dose, riociguat dose, washout period, drug adjustment period, etc. (Table 1).
Liu Y.Y., Qu Y.Y., Wang S., Luo C.J., Qiu H.L., Li H.T., Yuan P., Wang L., Li J.L., Jiang R, & Zhang R. (2023). Efficacy and safety of riociguat replacing PDE-5is for patients with pulmonary arterial hypertension: A systematic review and meta-analysis. Frontiers in Pharmacology, 14, 1052546.
Full text: Click here
Publication 2023
Pharmaceutical Preparations riociguat Sildenafil Tadalafil

Top products related to «Tadalafil»

1
Tadalafil by Merck Group
Sourced in United States, Germany
Tadalafil is a pharmaceutical compound used as a key ingredient in various prescription medications. It functions as a selective inhibitor of phosphodiesterase type 5 (PDE5), an enzyme involved in the regulation of certain physiological processes. The core function of Tadalafil is to modulate the activity of PDE5 within the body.
2
Tadalafil by Eli Lilly
Sourced in United States
Tadalafil is a chemical compound used in the production of various pharmaceutical products. It functions as a phosphodiesterase type 5 (PDE5) inhibitor, which affects the regulation of certain physiological processes. The core function of Tadalafil is to provide a key component in the formulation of medicines, without further interpretation of its intended use.
3
Sildenafil citrate by Merck Group
Sourced in United States, Germany
Sildenafil citrate is a chemical compound that functions as a phosphodiesterase type 5 (PDE5) inhibitor. It is used as a laboratory reagent for research purposes.
4
Dimethyl sulfoxide (dmso) by Merck Group
Sourced in United States, Germany, United Kingdom, China, Italy, Sao Tome and Principe, France, Macao, India, Canada, Switzerland, Japan, Australia, Spain, Poland, Belgium, Brazil, Czechia, Portugal, Austria, Denmark, Israel, Sweden, Ireland, Hungary, Mexico, Netherlands, Singapore, Indonesia, Slovakia, Cameroon, Norway, Thailand, Chile, Finland, Malaysia, Latvia, New Zealand, Hong Kong, Pakistan, Uruguay, Bangladesh
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.
5
Formic acid by Merck Group
Sourced in Germany, United States, Italy, United Kingdom, France, Spain, China, Poland, India, Switzerland, Sao Tome and Principe, Belgium, Australia, Canada, Ireland, Macao, Hungary, Czechia, Netherlands, Portugal, Brazil, Singapore, Austria, Mexico, Chile, Sweden, Bulgaria, Denmark, Malaysia, Norway, New Zealand, Japan, Romania, Finland, Indonesia
Formic acid is a colorless, pungent-smelling liquid chemical compound. It is the simplest carboxylic acid, with the chemical formula HCOOH. Formic acid is widely used in various industrial and laboratory applications.
6
Tadalafil by Santa Cruz Biotechnology
Sourced in Spain, China, United States, United Kingdom
Tadalafil is a lab equipment product manufactured by Santa Cruz Biotechnology. It functions as a phosphodiesterase type 5 (PDE5) inhibitor.
7
Acetonitrile by Merck Group
Sourced in Germany, United States, Italy, India, China, United Kingdom, France, Poland, Spain, Switzerland, Australia, Canada, Brazil, Sao Tome and Principe, Ireland, Belgium, Macao, Japan, Singapore, Mexico, Austria, Czechia, Bulgaria, Hungary, Egypt, Denmark, Chile, Malaysia, Israel, Croatia, Portugal, New Zealand, Romania, Norway, Sweden, Indonesia
Acetonitrile is a colorless, volatile, flammable liquid. It is a commonly used solvent in various analytical and chemical applications, including liquid chromatography, gas chromatography, and other laboratory procedures. Acetonitrile is known for its high polarity and ability to dissolve a wide range of organic compounds.
8
Tadalafil by Selleck Chemicals
Sourced in United States
Tadalafil is a white to off-white crystalline solid that is practically insoluble in water. It is a phosphodiesterase type 5 (PDE5) inhibitor. Tadalafil is used as a reference standard in analytical procedures.
9
Sildenafil citrate by Pfizer
Sourced in United States
Sildenafil citrate is a chemical compound used in the manufacturing of pharmaceutical products. It is a key ingredient in the production of various lab equipment and medical devices. The core function of sildenafil citrate is to serve as a fundamental component in the development of these specialized products.
10
Fenofibrate by Merck Group
Sourced in United States, Germany, United Kingdom, Sao Tome and Principe, Macao, Japan, China, France
Fenofibrate is a laboratory equipment product manufactured by Merck Group. It is a type of lipid-regulating agent used in pharmaceutical research and development. The core function of Fenofibrate is to help regulate and manage lipid levels in biological samples.

More about "Tadalafil"

Tadalafil, a powerful and selective phosphodiesterase type 5 (PDE5) inhibitor, is a widely used medication for treating erectile dysfunction and pulmonary arterial hypertension.
This long-acting compound works by relaxing blood vessels, enabling increased blood flow to the penis or lungs, leading to improved function.
Sildenafil citrate, another PDE5 inhibitor, is a commonly prescribed alternative to tadalafil for treating erectile issues.
DMSO (dimethyl sulfoxide) and formic acid are solvents that may be used in tadalafil formulations, while acetonitrile is a common reagent employed in tadalafil analysis.
Fenofibrate, a lipid-lowering drug, can also interact with tadalafil, requiring careful dosing and monitoring.
Researchers can leverage the advanced protocol optimization tools offered by PubCompare.ai to streamline their tadalafil studies.
These AI-driven tools enable the identification of the most reproducible and accurate research methods from published literature, preprints, and patents, ultimately enhancing the quality and efficiency of tadalafil-related investigations.
Whether you're exploring the pharmacological properties of tadalafil, studying its interactions with other compounds, or developing new therapeutic applications, PubCompare.ai's cutting-edge technology can provide invaluable insights and support to optimize your research protocls and improve your findings.
Discover how this innovative platform can elevate your tadalafil-focused studies today.