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A series of 2-piperazinyl-5-alkoxypyridines were synthesized and screened against human GPR119 receptor. Through SAR analysis, compounds containing 2-alkylsulfonylpiperazinyl-5-alkoxypyridines were discovered and found to be potent agonists of the human GPR119 receptor.
High-throughput methods were applied to the production, analysis, and characterization of libraries of natural products in order to accelerate the drug discovery process for high-throughput screening in the pharmaceutical and biotechnology industries. Library production integrates automated flash chromatography, solid-phase extraction, filtration, and… (More)
Electroencephalogram depth of anaesthesia monitors are increasingly being used, with the aim of reducing awareness during anaesthesia. Most literature concentrates on the ability of these monitors to predict when a patient is likely to be aware. This case report highlights the opposite problem, where the monitor (M-Entropy) indicated an awake state but the… (More)
The stability of baclofen in an extemporaneously compounded oral liquid formulation for 35 days was studied. A suspension was prepared by grinding commercially available 20-mg baclofen tablets and adding Glycerin, USP, to form a paste. Simple Syrup, NF, was added as necessary to make a final volume of 60 mL. A control solution was prepared from… (More)
A unique method of intermittent positive pressure ventilation of the lungs during general anaesthesia for bronchoscopy, which leaves the view and access of the endoscopist unhampered, has been described by Sanders (1967). A venturi effect is created at the open end of a Negus bronchoscope by passing oxygen at a pressure of 50 Lb./sq.in. through an… (More)
SUMMARY Brain hypoxia during the acute stage of a head injury may result from the injury itself, an inadequate airway, associated injuries and blood loss. The maintenance of a clear airway is a major responsibility of the anaesthetist and some of the difficulties involved are discussed. Artificial ventilation of the lungs will become necessary when other… (More)
High-throughput isolation, purification and analysis methods applied to natural products libraries from plants gave rise to the discovery of two novel acylated caprylic alcohol glycosides (1, 2) produced by Arctostaphylos pumila. The NMR spectra were acquired using the CapNMR probe and performed on mass-limited samples, which enabled us to elucidate the… (More)