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Rescooped by Jocelyn Stoller from Neuroscience_topics
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Modulation of NMDA receptor at the synapse: Promising therapeutic interventions in disorders of the nervous system

Modulation of NMDA receptor at the synapse: Promising therapeutic interventions in disorders of the nervous system | Social Neuroscience Advances | Scoop.it

[Review] There is general agreement that excessive activation of N-methyl-D-aspartate (NMDA) receptors plays a key role in mediating at least some aspects of synaptic dysfunction in several central nervous system disorders. On this view, in the last decades, research focused on the discovery of different compounds able to reduce NMDA receptor activity, such as classical and/or subunit-specific antagonists. However, the increasing body of knowledge on specific signaling pathways downstream NMDA receptors led to the identification of new pharmacological targets for NMDA receptor-related pathological conditions. Moreover, besides over-activation, several studies indicated that also abnormal NMDA receptor trafficking, resulting in the modification of the receptor subunit composition at the synapse, has a major role in the pathogenesis of several brain disorders. For this reason, the discovery of the molecular mechanisms regulating the abundance of synaptic versus extra-synaptic NMDA receptors as well as the activation of the specific signaling pathways downstream the different NMDA receptor subtypes is needed for the development of novel therapeutic approaches for NMDA receptor-dependent synaptic dysfunction. (...) - Mellone M. & Gardoni FEuropean Journal of Pharmacology

Volume 719, Issues 1–3, 5 November 2013, Pages 75–83


Via Julien Hering, PhD
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Rescooped by Jocelyn Stoller from Neuroscience_topics
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A golden approach to ion channel inhibition

A golden approach to ion channel inhibition | Social Neuroscience Advances | Scoop.it

Drugs are often used in combination and, for pharmacologists, the manner of their interactions can cast light on drug mechanisms and biological processes. Here we provide simplified descriptions of commonly used analytical methods for analysing drug combinations and describe a new and practical experimental solution to address the mechanistic question: Do two channel-blocking drugs bind at the same site? We define two simple mathematical models that describe the effects of two channel blockers acting simultaneously at either the same (Syntopic Model) or different (Allotopic Model) binding sites within a channel pore. We find that the optimum concentrations of two drugs for distinguishing between the two models are related to the mathematical Golden Ratio. - by Jarvis GE & Thompson AJTrends in Pharmacological SciencesVolume 34, Issue 9, 481-488, 23 August 2013


Via Julien Hering, PhD
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