ML297 (VU0456810), the First Potent and Selective Activator of the GIRK Potassium Channel, Displays Anti-Epileptic Properties in Mice.

ML297 (VU0456810), the first potent and selective activator of the GIRK potassium channel, displays anti-epileptic properties in mice.

ACS Chem Neurosci. 2013 Jun 3;
Kaufmann KW, Romaine IM, Days E, Pascual C, Malik A, Yang L, Zou B, Du Y, Sliwoski G, Morrison RD, Denton J, Niswender CM, Daniels JS, Sulikowski GA, Xie X, Lindsley CW, Weaver CD

The G-protein activated, inward-rectifying potassium (K+) channels, “GIRKs”, are a family of ion channels (Kir3.1-Kir3.4) that has been the focus of intense research interest for nearly two decades. GIRKs are comprised of various homo and heterotetrameric combinations of four different subunits. These subunits are expressed in different combinations in a variety of regions throughout the central nervous system and in the periphery. The body of GIRK research implicates GIRK in processes as diverse as controlling heart rhythm, to effects on reward/addiction, to modulation of response to analgesics. Despite years of GIRK research, very few tools exist to selectively modulate GIRK channels’ activity and until now no tools existed that potently and selectively activated GIRKs. Here we report the development and characterization of the first truly potent, effective, and selective GIRK activator, ML297 (VU0456810). We further demonstrate that ML297 is active in two in vivo models of epilepsy, a disease where up to 40% of patients remain with symptoms refractory to present treatments. The development of ML297 represents a truly significant advancement in our ability to selectively probe GIRK’s role in physiology as well as providing the first tool for beginning to understand GIRK’s potential as a target for a diversity of therapeutic indications. HubMed – addiction

Leveraging tobacco control research in India: the need for setting up a tobacco control research network.

Addiction. 2013 Jun 4;
Panda R, Persai D, Arora M

HubMed – addiction

The systems genetics resource: a web application to mine global data for complex disease traits.

Front Genet. 2013; 4: 84
van Nas A, Pan C, Ingram-Drake LA, Ghazalpour A, Drake TA, Sobel EM, Papp JC, Lusis AJ

The Systems Genetics Resource (SGR) (http://systems.genetics.ucla.edu) is a new open-access web application and database that contains genotypes and clinical and intermediate phenotypes from both human and mouse studies. The mouse data include studies using crosses between specific inbred strains and studies using the Hybrid Mouse Diversity Panel. SGR is designed to assist researchers studying genes and pathways contributing to complex disease traits, including obesity, diabetes, atherosclerosis, heart failure, osteoporosis, and lipoprotein metabolism. Over the next few years, we hope to add data relevant to deafness, addiction, hepatic steatosis, toxin responses, and vascular injury. The intermediate phenotypes include expression array data for a variety of tissues and cultured cells, metabolite levels, and protein levels. Pre-computed tables of genetic loci controlling intermediate and clinical phenotypes, as well as phenotype correlations, are accessed via a user-friendly web interface. The web site includes detailed protocols for all of the studies. Data from published studies are freely available; unpublished studies have restricted access during their embargo period. HubMed – addiction

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