PURPOSE Microdialysis is a valuable technique for studying the distribution of drugs into interstitial fluid, the target site for a pharmacologic effect. Due to incomplete equilibrium, retrodialysis is a method used to correct for relative recovery. The impact of two-drug combinations on probe recovery, however, remains unknown. METHODS In vitro microdialysis was conducted for five antibiotic...

Clinically observed drug interactions with cytochrome p450 (p450) enzymes have increased the need to assess drug interactions of new chemical entities early in the discovery process. To meet this need, fluorogenic substrates have been commercialized. However, only limited evaluations of their utility and comparisons to drug probes have been reported. This study examines the correlation between ...

Inhibition of cytochrome P450 (CYP450) enzymes can result in potential clinical drug-drug interaction liabilities. Because of the safety and economic concern leading to clinical failure or product withdrawal, screening of lead molecules for CYP450 inhibition potential is nowadays conducted much earlier in the drug development process. At this early phase, a large number of lead molecules are in...

Impaired brain connectivity is a hallmark of schizophrenia brain dysfunction. However, the effect of drug treatment and challenges on the dysconnectivity of functional networks in schizophrenia is an understudied area. In this review, we provide an overview of functional magnetic resonance imaging studies examining dysconnectivity in schizophrenia and discuss the few studies which have also att...

Control of the global epidemic tuberculosis is severely hampered by the emergence of drug-resistant Mycobacterium tuberculosis strains. Molecular methods offer a more rapid means of characterizing resistant strains than phenotypic drug susceptibility testing. We have developed a molecular method for detection of rifampicin-resistant M. tuberculosis based on padlock probes and magnetic nanobeads...

Image guided technique is playing an increasingly important role in the investigation of the biodistribution and pharmacokinetics of drugs or drug delivery systems in various diseases, especially cancers. Besides anatomical imaging modalities such as computed tomography (CT), magnetic resonance imaging (MRI), molecular imaging strategy including optical imaging, positron emission tomography (PE...

BACKGROUND High attrition rates in drug discovery call for new approaches to improve target validation. Academia is filling gaps, but often lacks the experience and resources of the pharmaceutical industry resulting in poorly characterized tool compounds. DISCUSSION The SGC has established an open access chemical probe consortium, currently encompassing ten pharmaceutical companies. One of it...

Susceptibility-weighted imaging (SWI) has continued to develop into a powerful clinical tool to visualize venous structures and iron in the brain and to study diverse pathologic conditions. It is a new art which evaluates and exploits the properties of blood, iron and other tissues. It is a magnitude or filtered phase images or combination of both, obtained with high-resolution 3D fully velocit...