Syntheses of a radiolabelled CXCR2 antagonist AZD5069 and its major human metabolite.

The CXCR2 antagonist AZD5069 has been synthesized in tritium and carbon-14-labelled forms. [(3) H]AZD5069 was prepared via reductive dehalogenation of an iodinated precursor with tritium gas to provide material with a specific activity of 25.1 Ci/mmol.

The synthesis of [(14) C]AZD5122. Incorporation of an IV (14) C-microtracer dose into a first in human study to determine the absolute oral bioavailability of AZD5122.

AZD5122, N-(2-(2,3-difluorobenzylthio)-6-((2R,3R)-3,4-dihydroxybutan-2-ylamino)pyrimidin-4-yl)azetidine-1-sulfonamide was under investigation as a potential chemokine receptor CXCR2 antagonist for the treatment for inflammatory diseases. To gain a better understanding of the human pharmacokinetic profile, an exploratory phase I IV microtracer study was conducted using carbon-14 radiolabelled AZD5122. [(14) C]AZD5122 was carbon-14 labelled in the pyrimidine ring in five steps in an overall radiochemical yield of 19% from [(14) C]thiourea.

A short expedient synthesis of [(14)C]Ticlopidine.

To support the development of a reactive metabolite strategy, the preparation of several radiolabelled compounds such as [(14)C] Ticlopidine was required. In this report, we describe a facile and rapid synthesis of [(14)C] Ticlopidine starting from [(14)C] carbon dioxide. The compound was radiolabelled in the 2-chloromethyl portion of the molecule with a specific activity of 53.

Waiting for the pain to get worse: characteristics of a pediatric population with acute dental pain.

Purpose: The purpose of this study was to examine how acute dental pain in children is managed.

Methods: A prospective 18-item cross-sectional survey was administered to 300 parent-child dyads seeking care at a large urban tertiary care hospital emergency walk-in dental clinic.

Results: The children's mean age was 8 years, 6 months (±3 years, 2 months).

Fatigue and health in a seafaring population.

Background: Occupational fatigue is relatively common within the general population and has been linked to reduced performance, injury and longer term ill-health. Despite growing acknowledgement of this problem in the maritime sector, little research has been conducted into the risk factors, prevalence and consequences of seafarers' fatigue.

Aims: To examine the prevalence of fatigue among seafarers, identify potential risk factors and assess possible links with poor performance and ill-health.

Patterns of fatigue among seafarers during a tour of duty.

Background: Work-related fatigue is associated with sickness absence and mental and physical health problems, and may increase the risk of accidents and injuries at work. Relatively little is known about fatigue among seafarers, particularly during a tour of duty. The aim of this study was to describe the pattern of day to day fatigue among seafarers during a tour at sea.