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Synthesis and Biological Evaluation of N-(benzene sulfonyl)acetamide Derivatives as Anti-inflammatory and Analgesic Agents with COX-2/5-LOX/TRPV1 Multifunctional Inhibitory Activity.

In this study, a series of structurally novel N-(benzene sulfonyl) acetamide derivatives were designed, synthesized, and biologically evaluated as COX-2/5-LOX/TRPV1 multitarget inhibitors for anti-inflammatory and analgesic therapy. Among them, 9a and 9b displayed favorable COX-2 (9a IC=0.011 μM, 9b IC=0.023 μM), 5-LOX (9a IC=0.046 μM, 9b IC=0.31 μM) and TRPV1 (9a IC=0.008 μM, 9b IC=0.14 μM) inhibitory activities. The pharmacokinetic (PK) study of 9a in SD rats at the dosage of 10 mg/kg demonstrated a high oral exposure, an acceptable clearance and a favorable bioavailability (Cmax=5807.18 ± 2657.83 ng/mL, CL=3.24 ± 1.47 mL/min/kg, F=96.8%). Further in vivo efficacy studies illustrated that 9a was capable of ameliorating formalin-induced pain and inhibiting capsaicin-induced ear edema.

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Implementation of a palliative care intervention for patients with COPD – a mixed methods process evaluation of the COMPASSION study.

Little direction exists on how to effectively implement palliative care for patients with COPD. In the COMPASSION study, we developed, executed, and evaluated a multifaceted implementation strategy to improve the uptake of region-tailored palliative care intervention components into routine COPD care. We evaluated the implementation strategy and assessed the implementation process, barriers, and facilitators.

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Oral Ketorolac as an Adjuvant Agent for Postoperative Pain Control After Arthroscopic Anterior Cruciate Ligament Reconstruction: A Prospective, Randomized Controlled Study.

Successful outpatient anterior cruciate ligament (ACL) reconstruction hinges on effective analgesia. Routinely, oral narcotic agents have been the preferred analgesic postoperatively in orthopaedic surgery. However, these agents have several known adverse effects and are associated with a potential for abuse. This study evaluates the efficacy of ketorolac, a nonsteroidal anti-inflammatory drug with analgesic properties, as an adjuvant agent for postoperative pain control after ACL reconstruction.

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Phytochemistry and Polypharmacological potential of Colebrookea oppositifolia Sm.

Colebrookea oppositifolia Sm. is a valuable traditional therapeutic plant belonging to the family Lamiaceae. It is a dense and wool-like shrub that is mostly found in subtropical regions of some countries of Asia, such as China and India. It has been widely used for the mitigation of nervous system disorders like epilepsy. The active constituents of the plant have exhibited antioxidant, anti-microbial, and antifungal properties, which are considered due to the presence of polyphenols and flavonoids as chief chemical constituents. Flavonoids like quercetin, landenein, chrysin, and 5, 6, 7-trimethoxy flavones cause protein denaturation of the microbial cell wall.

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Novel 4-chloro-N-phenyl Benzamide Derivatives as p38α Mitogen-activated Protein Kinase Inhibitors for Treating Cancer, COVID-19, and Other Diseases.

The present disclosure relates to p38α mitogen-activated protein kinase inhibitors, pharmaceutical compositions thereof, and the use of the p38α mitogen-activated protein kinase inhibitors and pharmaceutical compositions thereof for treating various diseases such as cancer, rheumatoid arthritis, amyotrophic lateral sclerosis, cystic fibrosis, cardiovascular disease, multiple sclerosis, inflammatory bowel disease, chronic obstructive pulmonary disease (COPD), asthma, COVID-19, acute respiratory distress syndrome (ARDS), and acute lung injury (ALI).

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A perspective on the use of the cervical flexion rotation test in the physical therapy management of cervicogenic headaches.

The Cervical Flexion-Rotation Test (CFRT) is widely used in the assessment of upper cervical spine mobility impairments and in the diagnosis of cervicogenic headache (CGH) by physiotherapist. Many studies investigated its different properties, and the results show that the CFRT has good construct validity in the measurement of C1-C2 rotation as well as good to excellent reliability.

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Adverse reactions after oral provocation with aluminium in children with vaccination granulomas and aluminium contact allergy.

According to their parents, some children with aluminium contact allergy and vaccination granulomas may react to aluminium-containing foods by developing dermatitis, granuloma itch and subjective symptoms.

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Changes and associations between gait biomechanics and knee inflammation after aspiration and corticosteroid injection for knee osteoarthritis.

Although knee inflammation is thought to adversely affect joint function in patients with knee osteoarthritis (OA), the effects of reducing knee inflammation on gait biomechanics and strength are unknown. Our objectives were to compare ultrasound (US) measures of knee inflammation, gait biomechanics, knee extension and flexion strength, and pain before and after knee aspiration and corticosteroid injection; and explore associations among changes.

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Personal protective equipment for COVID-19 among healthcare workers in an emergency department: an exploratory survey of workload, thermal discomfort, and symptoms of heat strain.

To examine workload, thermal discomfort, and heat-related symptoms among healthcare workers (HCWs) in an Australian emergency department during the COVID-19 pandemic.

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Examination of the pharmacokinetics and differential inhibition of cyclooxygenase isoenzymes in New Zealand white rabbits (Oryctolagus cuniculus) by the Non-Steroidal anti-inflammatory Robenacoxib.

Effective rabbit analgesia is challenging, and there are few studies available on the newer COX-2 selective NSAIDs, such as robenacoxib. This study aimed to establish the pharmacokinetics of oral and subcutaneous robenacoxib, describe its inhibitory actions on COX enzymes, and develop dosing, using six healthy New Zealand white rabbits. Pharmacokinetics were determined from plasma concentrations after oral administration of robenacoxib (0.83-0.96 mg/kg) and also after subcutaneous administration (2 mg/kg). The inhibitory actions of robenacoxib were evaluated by measuring plasma concentrations of thromboxane B (TBX ) and prostaglandin E (PGE ) as surrogate markers of cyclooxygenase enzyme isoform inhibition. The mean maximum concentration for oral and subcutaneous administration was 0.23 μg/ml and 5.82 μg/ml, respectively. Oral robenacoxib administration did not demonstrate a significant difference between any time point for PGE or TBX , though subcutaneous administration did for both. There was no significant difference in PGE or TBX concentrations at any time point when comparing subcutaneous versus oral routes. Although the results support that plasma robenacoxib exceeds the therapeutic levels compared to dogs and cats, there was little significance in the difference in the changes associated with COX-1 and COX-2 inhibition. Further studies are warranted to determine appropriate dosing, safety, and efficacy in rabbits.

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