A5089482349- Migraine and Headache Studies
- Inflammatory mediators and NSAID effects
- Pharmacogenetics and Drug Metabolism
- Eicosanoids and Hypertension Pharmacology
- Sympathectomy and Hyperhidrosis Treatments
- Heart Rate Variability and Autonomic Control
- Blood Pressure and Hypertension Studies
- Receptor Mechanisms and Signaling
- Asthma and respiratory diseases
- Diet and metabolism studies
- Nitric Oxide and Endothelin Effects
- Pharmaceutical studies and practices
- Olfactory and Sensory Function Studies
- Pharmacological Effects and Toxicity Studies
- Cardiovascular Syncope and Autonomic Disorders
- Antiplatelet Therapy and Cardiovascular Diseases
- Epilepsy research and treatment
- Pain Mechanisms and Treatments
- Cancer, Stress, Anesthesia, and Immune Response
- Neurotransmitter Receptor Influence on Behavior
- Hormonal Regulation and Hypertension
- Restless Legs Syndrome Research
- Venous Thromboembolism Diagnosis and Management
- Medical Imaging Techniques and Applications
- Cannabis and Cannabinoid Research
KU Leuven
2009-2024
Center for Clinical Research (United States)
1999-2022
University of Florida
2016
Columbus Oncology and Hematology Associates
2016
Reckitt Benckiser (United States)
2016
United States Military Academy
2007
Apotheek Haagse Ziekenhuizen
2002
Utrecht University
2002
Merck & Co., Inc., Rahway, NJ, USA (United States)
1993
MSD K.K. (Japan)
1992
Steady-state inhibitory activity of rofecoxib (Vioxx) on COX-2 versus COX-1 was compared with that commonly used nonsteroidal anti-inflammatory drugs (NSAIDs) in 76 healthy volunteers randomized to placebo, 12.5 mg qd, 25 diclofenac 50 tid, ibuprofen 800 sodium naproxen 550 bid, or meloxicam 15 qd. All these doses include the high end approved clinical dose range. Ex vivo whole-blood assays were determine effect and activity, respectively. Urinary prostanoids also measured. Mean inhibition...
In 12 healthy volunteers, paracetamol pharmacokinetics were compared following administration of 1 g propacetamol HCl given intravenously over a 15-min period and 500 mg orally. Mean +/- SD total AUC (microgram/ml.h) the iv formulation was significantly (P < 0.01) greater than oral (25.53 4.27 vs 21.04 4.49) corresponding to mean bioavailability 82.2 9.4%. Between 2 h after administration, plasma concentrations became very similar both formulations. another study, as infusion 2-min bolus...
WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT • Calcitonin gene‐related peptide (CGRP) was first described as a potent vasodilator. CGRP is also increasingly recognized key player in the pathophysiology of migraine, and receptor antagonists potentially offer new approach for treating migraine. A novel pharmacodynamic assay to measure antagonist activity non‐invasively humans has been developed, which involves measuring increase dermal blood flow induced by topical application capsaicin on...
Part I: to establish the dose and appropriate application site of capsaicin on human forearm in order produce a robust reproducible dermal blood flow (DBF) response. II: evaluate within-subject arm-to-arm period-to-period reproducibility.Both parts consisted two study visits. In part I, placebo 100, 300 1000 microg were applied at four predefined sites volar surface both forearms. Placebo doses randomized balanced by between subjects. Changes DBF assessed laser Doppler perfusion imaging up...
Taranabant is a cannabinoid-1 receptor inverse agonist for the treatment of obesity. This study evaluated safety, pharmacokinetics, and pharmacodynamics taranabant (5, 7.5, 10, or 25 mg once daily 14 days) in 60 healthy male subjects. was rapidly absorbed, with median t(max) 1.0 to 2.0 hours t(1/2) approximately 74 104 hours. Moderate accumulation observed C(max) (1.18- 1.40-fold) AUC(0-24 h) (1.5- 1.8-fold) over days 5-, 7.5-, 10-mg doses, an half-life ranging from 15 21 Steady state...
The purpose of this study was to identify the mediators involved in capsaicin-induced vasodilation human skin and evaluate a pharmacodynamic model for early clinical evaluation calcitonin gene-related peptide (CGRP) receptor antagonists. Dermal blood flow (DBF) response forearm topically applied capsaicin measured using laser Doppler perfusion imaging 22 subjects. effect intra-arterially administered CGRP<sub>8-37</sub> (1200 ng · min<sup>–1</sup> dl<sup>–1</sup> forearm), indomethacin (5 μg...
The pharmacokinetics (PK) and pharmacodynamics (PD) of omarigliptin, a novel once-weekly DPP-4 inhibitor, were assessed following single multiple doses in healthy subjects. Absorption was rapid, food did not influence single-dose PK. Accumulation minimal, steady state reached after 2 to 3 weeks. Weekly (area under the curve) AUC Cmax displayed dose proportionality within range studied at state. average renal clearance omarigliptin ∼2 L/h. inhibition ranged from ∼77% 89% 168 hours last over...
To assess the effect of calcitonin gene-related peptide (CGRP) receptor antagonist, telcagepant, on haemodynamic response to sublingual nitroglycerin (NTG).Twenty-two healthy male volunteers participated in a randomized, placebo-controlled, double-blind, two-period, crossover study. Subjects received 500 mg telcagepant or placebo followed, 1.5 h later, by 0.4 NTG. following vascular parameters were measured: blood pressure, aortic augmentation index (AIx) and brachial artery diameter (BAD)....
The histamine 3 (H3) receptor is a presynaptic autoreceptor in the central nervous system that regulates synthesis and release of modulates other major neurotransmitters. H3 inverse agonists (IAs) may be efficacious treatment various disorders, including excessive daytime sleepiness, attention deficit hyperactivity disorder, Alzheimer disease, ethanol addiction, obesity. <b>Methods:</b> Using PET novel high-affinity selective radioligand <sup>11</sup>C-MK-8278, we studied tracer...
Calcitonin gene related peptide (CGRP) receptor antagonists are effective acute migraine treatments. A capsaicin-induced dermal vasodilatation (CIDV) model has been developed to provide target-engagement information in healthy volunteers. In the model, CGRP release is provoked after capsaicin application, by activating transient potential vanilloid-type-1 (TRPV1) receptors at peripheral sensory nerves. Laser Doppler imaging used quantify CIDV and subsequent inhibition antagonists. We sought...
Montelukast, a cysteinyl leukotriene receptor antagonist, is being developed for the treatment of asthma and related diseases. This study was designed to evaluate whether montelukast at clinically used dosage levels would interfere with anticoagulant effect warfarin. In two‐period, double‐blind, randomized crossover study, 12 healthy male subjects received single oral dose 30 mg warfarin on 7th day 12‐day montelukast, 10 daily by mouth, or placebo. Montelukast had no significant area under...
Traditional assays of the coagulation status patients, bleeding time assessment (BT) and light transmission aggregometry (LTA), are useful in clinical drug development. However, these both labor intensive expensive. BT results can be operator dependent by its nature inhibit subject enrollment a trial. The preparation platelet-rich plasma necessary for LTA requires specialized training laboratory support. Alternatives to methods desirable. goal this study was identification quantitative,...
Decreased glutamatergic neurotransmission is hypothesized to be involved in the pathophysiology of schizophrenia. Inhibition glycine transporter Type-1 (GlyT1) reuptake expected increase and may serve as treatment for cognitive negative symptoms In this article, we present human data from a novel GlyT1 PET tracer, [(18) F]MK-6577. process developing inhibitor therapeutic, tracer can assist determining dose with high probability sufficiently testing mechanism action. This article reports...
Article Effect of Clopidogrel on Naproxen-Induced Gastrointestinal Blood Loss in Healthy Volunteers was published March 1, 1998 the journal Drug Metabolism and Personalized Therapy (volume 14, issue 3).
Objective The objective of this article is to assess the effects sumatriptan monotherapy, telcagepant and their combination on blood pressure (BP) in migraine patients during a headache-free period. Methods A double-blind, placebo-controlled, four-period, single-dose, randomized crossover study 24 was conducted. In each period, received single oral dose 100 mg alone, 600 coadministered with mg, or placebo. Semi-recumbent BP measured pre-dose at seven post-dose timepoints over period six...
MK-886, a leukotriene biosynthesis inhibitor, was evaluated in double-blind, placebo-controlled, randomized single- and multiple-dose studies 12 24 healthy male subjects, respectively. The effects of single dose (250, 500, 750 mg) multiple doses (100 mg 250 every 8 hours) MK-886 on calcium ionophore stimulated B4 synthesis ex vivo whole blood were evaluated. Inhibition occurred dose-related manner up to 500 dose, hours. A significantly inhibited by maximum 60% at 2 hours after the (p <...
Background/Hypothesis: Atogepant, an oral calcitonin gene-related peptide receptor antagonist, is approved for the preventive treatment of migraine in adults. This manuscript characterizes safety, tolerability, pharmacokinetics and pharmacokinetic/pharmacodynamic relationship atogepant healthy males. Methods: Data from two single-ascending dose phase 1 studies were utilized to characterize demonstrate proof activity a capsaicin-induced dermal vasodilatation model determine dosage(s) that...