BMC Pharmacology - Latest articlesThe latest articles from BMC Pharmacology (ISSN 1471-2210) published by BioMed CentralStructure-activity models of oral clearance, cytotoxicity, and LD50: a screen for promising anticancer compounds- June 13, 2008 Background: Quantitative structure-activity relationship (QSAR) models have become popular tools to help identify promising lead compounds in anticancer drug development. Few QSAR studies have investigated multitask learning, however. Multitask learning is an approach that allows distinct but related data sets to be used in training. In this paper, a suite of three QSAR models is developed to identify compounds that are likely to (a) exhibit cytotoxic behavior against cancer cells, (b)...http://www.biomedcentral.com/1471-2210/8/12 Pharmacological Properties of DOV 315,090, an ocinaplon metabolite.- June 13, 2008 Compounds targeting the benzodiazepine binding site of the GABAA-R are widely prescribed for the treatment of anxiety disorders, epilepsy, and insomnia as well as for pre-anesthetic sedation and muscle relaxation. It has been hypothesized that these various pharmacological effects are mediated by different GABAA-R subtypes. If this hypothesis is correct, then it may be possible to develop compounds targeting particular GABAA-R subtypes as, for example, selective anxiolytics with a diminished...http://www.biomedcentral.com/1471-2210/8/11 Benfotiamine, a synthetic S-acyl thiamine derivative, has different mechanisms of action and a different pharmacological profile than lipid-soluble th- June 12, 2008 Background: Lipid-soluble thiamine precursors have a much higher bioavailability than genuine thiamine and therefore are more suitable for therapeutic purposes. Benfotiamine (S-benzoylthiamine O-monophosphate), an amphiphilic S-acyl thiamine derivative, prevents the progression of diabetic complications, probably by increasing tissue levels of thiamine diphosphate and so enhancing transketolase activity. As the brain is particularly sensitive to thiamine deficiency, we wanted to test whether...http://www.biomedcentral.com/1471-2210/8/10 Antagonist affinity measurements at the Gi-coupled human histamine H3 receptor expressed in CHO cells- June 6, 2008 Background: The H3 histamine receptor is a Gi-coupled GPCR that has been proven to exist in different agonist-induced states, including that defined by the protean agonist proxyfan. Several GPCRs are now known to exist in different states. For some of these, antagonist affinity measurement remain constant regardless of the state of the receptor, for others e.g. the beta-adrenoceptors, the antagonist affinity measurements vary considerably depending on which agonist-dependent state is being...http://www.biomedcentral.com/1471-2210/8/9 |