CNS
Psychiatric disorders affect many people and encompass a long list of conditions. The disorders range in severity from mild over socially debilitating to life-threatening. A growing body of evidence has established that ion channels play an important role in these diseases. Neuronal excitability, neurotransmitter release, gene transcription and brain plasticity hinge on ion channel functionality and hence can be harmed by malfunctioning ion channels.
Selected ion channels involved in psychiatric disorders:
Key ion channels
Nav1.1, 1.2 & 1.3
Cav1.2
GABA
Kv1.1, 3.x, 7.3 & 11.1
Kir3.1 & 4.1
KCa1.1 & 3.1
TASK3
Nav1.1, 1.2 and 1.3
Posters
- View Adaptive voltage protocols increase precision of voltage-gated ion channel measurements on highthroughput automated patch clamp platforms Year: 2019
- View Structure-based identification of novel KNa1.1 inhibitors Year: 2019
- View HT Automation for patch clamp based primary screen for Nav1.1 using Qube 384 Year: 2018
- View Biophysical and pharmacological characterization of multiple Nav subtypes on Qube Year: 2016
- View Biophysical and pharmacological profiling of multiple Nav subtypes on QPatch HT Year: 2016
- View Biophysical and pharmacological profiling of multiple voltage-gated sodium channel subtypes on QPatch II Year: 2019
- View Exploring stem cell-derived cardiomyocytes with automated patch clamp techniques Year: 2012
- View Data quality is not affected by cell suspension density Year: 2006
- View Evaluation of throughput and data quality Year: 2009
- View Pharmacological characterization of voltage- and ligand-gated ion channels Year: 2006
- View Characterization of hiPSC-derived neurological disease models using automated patch clamp (Qube and QPatch) Year: 2019
Papers
- View Venom Peptides with Dual Modulatory Activity on the Voltage-Gated Sodium Channel NaV1.1 Provide Novel Leads for Development of Antiepileptic Drugs Year: 2019
- View Personalized medicine: Vinpocetine to reverse effects of GABRB3 mutation Year: 2019
- View Biophysical and pharmacological profiling of multiple voltage-gated sodium channel subtypes on QPatch II Year: 2019
- View 4-Substituted carbamazepine derivatives: conformational analysis and sodium channel-blocking properties Year: 2018
- View The sodium channel activator Lu AE98134 normalizes the altered firing properties of fast spiking interneurons in Dlx5/6+/− mice Year: 2017
- View Automated Planar Electrode Electrophysiology in Drug Discovery: Examples of the Use of QPatch in Basic Characterization and High Content Screening on Nav, KCa2.3, and Kv11.1 Channels Year: 2009
- View Stable response for ligand and voltage-gated ion channels on QPatch Year: 2010
- View QPatch: the missing link between HTS and ion channel drug discovery. Year: 2009
- View Automated Patch Clamping Using the QPatch Year: 2009
- View A small molecule activator of Nav1.1 channels increases fast-spiking interneuron excitability and GABAergic transmission in vitro and has anti-convulsive effects in vivo Year: 2017
- View A Selective Nav1.1 Activator with Potential for Treatment of Dravet Syndrome Epilepsy Year: 2020
- View EST64454: a Highly Soluble σ 1 Receptor Antagonist Clinical Candidate for Pain Management Year: 2020
Reports
Cav1.2
Posters
Papers
- View A new classifier-based strategy for in-silico ion-channel cardiac drug safety assessment Year: 2015
- View Screening system for drug-induced arrhythmogenic risk combining a patch clamp and heart simulator Year: 2015
- View MICE Models: Superior to the HERG Model in Predicting Torsade de Pointes Year: 2013
Reports
Kv1.1, Kv2.1, Kv3.x, Kv7.3 and Kv11.1
Posters
- View Validation of B’SYS KV3.x cell lines using automated and manual patch-clamp electrophysiology Year: 2019
- View Enhancing throughput with multiple cell lines per well Year: 2006
- View Strategies for enhancing throughput in ion channel drug screening Year: 2008
- View Pharmacological characterization of voltage- and ligand-gated ion channels Year: 2006
- View Qube as a tool for assay optimization of CiPA cells and protocols by using multiple IC, EC solutions and hERG, Nav1.5 and Cav1.2 on the same QChip Year: 2016
- View Characterization of hERG blockers using the automated QPatch 16 screening system Year: 2005
- View Data quality is not affected by cell suspension density Year: 2006
- View “Clip Detecting” with series resistance compensation using an automated patch clamp system Year: 2012
- A dipolar cycloaddition reaction to access 6-methyl-4,5,6,7-tetrahydro-1H-[1,2,3]triazolo[4,5-c]pyridines enables the discovery synthesis and preclinical profiling of a P2X7 antagonist clinical candidate Year: 2017
Papers
- View Synthesis and biological evaluation of a series of multi-target N-substituted cyclic imide derivatives with potential antipsychotic effect Year: 2018
- View Arrangement of Kv1 α subunits dictates sensitivity to tetraethylammonium Year: 2010
- View Porphyrin derivatives as potent and selective blockers of neuronal Kv1 channels Year: 2014
- View MICE Models: Superior to the HERG Model in Predicting Torsade de Pointes Year: 2013
- View Characterization of Potassium Channel Modulators with QPatch™ Automated Patch-Clamp Technology: System Characteristics and Performance To cite this article: Year: 2004
- View Automated Patch Clamping Using the QPatch Year: 2009
- View Automated Planar Electrode Electrophysiology in Drug Discovery: Examples of the Use of QPatch in Basic Characterization and High Content Screening on Nav, KCa2.3, and Kv11.1 Channels Year: 2009
- View Synthesis and biological evaluation of novel 6,11-dihydro-5H-benzo[e]pyrimido- [5,4-b][1,4]diazepine derivatives as potential c-Met inhibitors Year: 2017
- View QPatch: the missing link between HTS and ion channel drug discovery. Year: 2009
- View A new classifier-based strategy for in-silico ion-channel cardiac drug safety assessment Year: 2015
- View Screening system for drug-induced arrhythmogenic risk combining a patch clamp and heart simulator Year: 2015
- View Identification of Selective Inhibitors of the Potassium Channel Kv1.1–1.2(3) by High-Throughput Virtual Screening and Automated Patch Clamp Year: 2012
- View Disruption of Myelin Leads to Ectopic Expression of KV1.1 Channels with Abnormal Conductivity of Optic Nerve Axons in a Cuprizone-Induced Model of Demyelination Year: 2019
- View Development of a selective inhibitor for Kv1.1 channels prevalent in demyelinated nerves Year: 2020
Reports
- View Stable Vhalf values and reliable potentiation of Kv7.3/7.2 currents on Qube 384 Year: 2019
- View Reliable Kv2.1 assasy and pharmacology on the QPatch Year: 2017
- View CHO-hERG Duo characterization and functional validation on QPatch Year: 2011
- View CHO-hERG Duo in multi-hole mode on QPatch Year: 2011
- View Stable response for ligand and voltage-gated ion channels on QPatch Year: 2010
Kir
Reports
- View HEK-hKir2.1 on QPatch Year: 2013
Kca1.1 & 3.1
Papers
- View Development of a QPatch Automated Electrophysiology Assay for Identifying KCa3.1 Inhibitors and Activators Year: 2013
- View New positive Ca2+-activated K+ channel gating modulators with selectivity for KCa3.1 Year: 2014
- View Inhibition of the potassium channel KCa3.1 by senicapoc reverses tactile allodynia in rats with peripheral nerve injury Year: 2016
Reports
GABA
Posters
- View Ligand-activation of GABAA receptors on the automated patch clamp platforms QPatch and Qube 384 using conventional electrophysiology and optopharmacology Year: 2018
- View GABA-A receptor pharmacology evaluated in overexpressing HEK cells and primary astrocytes on QPatch Year: 2018
- View Application of QPatch 16 for drug screening of ligand-gated ion channels Year: 2005
- View Assessing functional properties of ligand-gated ion channels with automated whole-cell patch clamp technology Year: 2006
- View Development and validation of ligand-gated ion channel assays using the Qube 384 automated electrophysiology platform Year: 2019
Papers
- View A small molecule activator of Nav1.1 channels increases fast-spiking interneuron excitability and GABAergic transmission in vitro and has anti-convulsive effects in vivo Year: 2017
- View Rescue of deficient amygdala tonic γ-aminobutyric acidergic currents in the Fmr–/y mouse model of fragile X syndrome by a novel γ-aminobutyric acid type A receptor-positive allosteric modulator Year: 2015
- View Electrophysiological Studies of GABA-A Receptors Using QPatch II, the Next Generation of Automated Patch‐Clamp Instruments Year: 2020
- View Hybrid molecules combining GABA-A and serotonin 5-HT6 receptors activity designed to tackle neuroinflammation associated with depression Year: 2022
Reports
Stem cells
Posters
- View Characterization of hiPSC-derived neurological disease models using automated patch clamp (Qube and QPatch) Year: 2019