Ion channels as therapeutic targets. Part A
Free download. Book file PDF easily for everyone and every device. You can download and read online Ion channels as therapeutic targets. Part A file PDF Book only if you are registered here. And also you can download or read online all Book PDF file that related with Ion channels as therapeutic targets. Part A book. Happy reading Ion channels as therapeutic targets. Part A Bookeveryone. Download file Free Book PDF Ion channels as therapeutic targets. Part A at Complete PDF Library. This Book have some digital formats such us :paperbook, ebook, kindle, epub, fb2 and another formats. Here is The CompletePDF Book Library. It's free to register here to get Book file PDF Ion channels as therapeutic targets. Part A Pocket Guide.
Contents:
Table of Contents: Ion channels as therapeutic targets.
You have also an option to screen the library directly at Enamine. In this case, we will be happy to offer you discount on library cost depending on the collaboration scope. We applied multipronged approach in rational library design to gain a qualitative set of molecules focused on ion channel targets.
A major contribution was made in the lead-oriented synthesis program at Enamine focused on increasing novelty and structural diversity.
- Organ Theft Legends.
- Acid-sensing ion channels: potential therapeutic targets for neurologic diseases!
- Navigation menu?
- Phagosomal Ion Channels as Therapeutic Targets - Deborah Nelson.
The project has already yielded 36 lead-like compounds built on novel scaffolds featuring saturated rings that have been recognized as potential ion channel blockers. Additional compounds were added to the library after analysis of privileged motives of known ion channel blockers and after morphing of some recently discovered ion channel and TRPV1 modulators.
General Medicinal Chemistry overview finalized the library profile: favorable physicochemical parameters and solubility requirements. Send a message. Using our Libraries for hit identification you receive multiple benefits allowing you to save on time and costs in lead generation: Dry stock of over 2.
Purchase Ion Channels as Therapeutic Targets, Part A, Volume - 1st Edition. Print Book & E-Book. ISBN , Purchase Ion Channels as Therapeutic Targets, Part B, Volume - 1st Edition. Print Book & E-Book. ISBN ,
Most popular library formats Item. Item 1.
Catalog No. Compounds 36 Plates The readers detect a change in the concentration of certain ions that is the result of ion channel activity or a change in the voltage across the cell membrane, also caused by the flow of ion through the channel.
Join Kobo & start eReading today
The main benefits of these methods are their high throughput and low cost per data point. The main limitations of the methods are low accuracy and sensitivity, and lack of control of the voltage across the cell membrane, making it possible to study only certain types of ion channels and rather simple ways of drugs interacting with the ion channels. QPatch and Qube operate automatically and these systems increase patch clamp throughput due to the high degree of parallelism.
QPatch and Qube therefore combine the accuracy of traditional patch clamp with the high throughput of indirect methods.
Login using
The drug discovery process in pharmaceutical companies can begin either with a certain target, e. One important class of targets comprises ion channels. After a target validation phase, a test system an assay is developed to measure interactions with the target.
Pharmaceutical companies have huge libraries of chemical compounds, the largest of which contain up to a couple of million compounds. One or more of these compounds may be identified as so-called hits with a desired effect on a specific target. This process is iterative and called lead optimization. For every modification, new patch clamp tests are needed to check that the desired effect is preserved or improved. Further tests in disease relevant animal-models and safety test are carried out before the development in the clinical trials test in humans can lead to an approval by health authorities to market a new drug.
Finding the hits is like finding a needle in a haystack! For the last 20 years it has been routine to test either the entire compound library, or part of it, with indirect methods in a so-called High Throughput Screening HTS department in the pharmaceutical company that identifies the initial hits.
1st Edition
When opting-in for our newsletter you will receive newsletters per year. You can always opt-out directly from the newsletters. For more information see our privacy policy. Examples of such processes are: Generation of electrical activity in nerves Control of contractile activity in the heart and muscles Nutrient uptake Hormone secretion There are many ion channels A typical cell has ion channels of different types.
Ion channels play a role in many diseases A number of human diseases, including pathological pain conditions, epilepsy, cystic fibrosis and a variety of neural and muscular disorders, are caused by defects in the function of ion channels. Many drugs affect ion channels The large number of physiological processes regulated by ion channels and their role in many diseases make ion channels highly interesting as targets for new drugs.
Ion channels are difficult to explore Ion channels are important targets in drug discovery, but they are also difficult to study.
They are also equipped with liquid handling systems that allow fast compound perfusion, making them particularly useful for screening ligand-gated channels which generally have very fast kinetics. American Journal of Drug Discovery and Development, 1: Molecular identification and characterisation of the human eag2 potassium channel. Neuron 41, — Potential functional and pathological side effects related to off-target pharmacological activity. The medicinal chemistry of the P2 receptor family. Biomolecular Modelling and Simulations volume 96 Volume
Methods to explore ion channels There are two main methods to investigate ion channels: direct and indirect methods. Direct methods — Patch clamping The patch clamp technique is considered the gold standard in ion channel research.