CNS - Sophion

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 First author: Williams et Al., 2019
  • View Structure-based identification of novel KNa1.1 inhibitors
    Year: 2019 First author: Cole et Al., 2019
  • View HT Automation for patch clamp based primary screen for Nav1.1 using Qube 384
    Year: 2018 First author: Klint et Al.
  • View Biophysical and pharmacological characterization of multiple Nav subtypes on Qube
    Year: 2016 First author: Lindqvist et Al
  • View Biophysical and pharmacological profiling of multiple Nav subtypes on QPatch HT
    Year: 2016 First author: Lindqvist et al., 2016
  • View Biophysical and pharmacological profiling of multiple voltage-gated sodium channel subtypes on QPatch II
    Year: 2019 First author: Sauter et Al.
  • View Exploring stem cell-derived cardiomyocytes with automated patch clamp techniques
    Year: 2012 First author: Schrøder et al., 2012
  • View Data quality is not affected by cell suspension density
    Year: 2006 First author: Mathes et al., 2006
  • View Evaluation of throughput and data quality
    Year: 2009 First author: Olsen et al., 2009
  • View Pharmacological characterization of voltage- and ligand-gated ion channels
    Year: 2006 First author: Olsen et al., 2006
  • View Characterization of hiPSC-derived neurological disease models using automated patch clamp (Qube and QPatch)
    Year: 2019 First author: Rosholm et Al.

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 First author: Chow et Al.
  • View Personalized medicine: Vinpocetine to reverse effects of GABRB3 mutation
    Year: 2019 First author: Billakota et Al.
  • View Biophysical and pharmacological profiling of multiple voltage-gated sodium channel subtypes on QPatch II
    Year: 2019 First author: Sauter et Al.
  • View 4-Substituted carbamazepine derivatives: conformational analysis and sodium channel-blocking properties
    Year: 2018 First author: Kanase et Al.
  • View The sodium channel activator Lu AE98134 normalizes the altered firing properties of fast spiking interneurons in Dlx5/6+/− mice
    Year: 2017 First author: von Schoubye et Al.
  • 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 First author: Korsgaard et al., 2009
  • View Stable response for ligand and voltage-gated ion channels on QPatch
    Year: 2010 First author: Olsen et al., 2010
  • View QPatch: the missing link between HTS and ion channel drug discovery.
    Year: 2009 First author: Mathes
  • View Automated Patch Clamping Using the QPatch
    Year: 2009 First author: Jones et al. 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 First author: K Frederiksen
  • View A Selective Nav1.1 Activator with Potential for Treatment of Dravet Syndrome Epilepsy
    Year: 2020 First author: Chow et Al.
  • View EST64454: a Highly Soluble σ 1 Receptor Antagonist Clinical Candidate for Pain Management
    Year: 2020 First author: Diaz et al., 2020

Reports

  • View Electrophysiological characterization of human iPSC-derived motor neurons using Qube 384 and QPatch
    Year: 2019 First author: Rosholm et Al.
  • View Pharmacological evaluation of GABAA receptor subtypes on Qube 384
    Year: 2019 First author: Boddum et Al., 2019
  • View Nav1.1 currents on Qube
    Year: 2018 First author: Klint et Al.

Cav1.2

Posters

  • 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 First author: Schupp et al., 2016
  • View Exploring stem cell-derived cardiomyocytes with automated patch clamp techniques
    Year: 2012 First author: Schrøder et al., 2012

Papers

  • View A new classifier-based strategy for in-silico ion-channel cardiac drug safety assessment
    Year: 2015 First author: Mistry et al., 2015
  • View Screening system for drug-induced arrhythmogenic risk combining a patch clamp and heart simulator
    Year: 2015 First author: Okada et al., 2015
  • View MICE Models: Superior to the HERG Model in Predicting Torsade de Pointes
    Year: 2013 First author: Kramer et al., 2013

Reports

  • View hCav1.2 recordings using QPatch
    Year: 2018 First author: Rosholm et Al.
  • View hCav1.2 recordings on Qube 384 using step, train and CiPA protocols
    Year: 2018 First author: Schupp
  • View Cav1.2 on Qube 384
    Year: 2017 First author: Schupp, M

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 First author: Braksator et Al.
  • View Enhancing throughput with multiple cell lines per well
    Year: 2006 First author: Olsen et al.
  • View Strategies for enhancing throughput in ion channel drug screening
    Year: 2008 First author: Jacobsen et al., 2008
  • View Pharmacological characterization of voltage- and ligand-gated ion channels
    Year: 2006 First author: Olsen et al., 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 First author: Schupp et al., 2016
  • View Characterization of hERG blockers using the automated QPatch 16 screening system
    Year: 2005 First author: Jacobsen et al., 2005
  • View Data quality is not affected by cell suspension density
    Year: 2006 First author: Mathes et al., 2006
  • View “Clip Detecting” with series resistance compensation using an automated patch clamp system
    Year: 2012 First author: Løjkner et al., 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 First author: Chrovian et Al.

Papers

  • View Synthesis and biological evaluation of a series of multi-target N-substituted cyclic imide derivatives with potential antipsychotic effect
    Year: 2018 First author: Mingshuo et Al.
  • View Arrangement of Kv1 α subunits dictates sensitivity to tetraethylammonium
    Year: 2010 First author: Al-Sabi et Al
  • View Porphyrin derivatives as potent and selective blockers of neuronal Kv1 channels
    Year: 2014 First author: Daly et al., 2014
  • View MICE Models: Superior to the HERG Model in Predicting Torsade de Pointes
    Year: 2013 First author: Kramer et al., 2013
  • View Characterization of Potassium Channel Modulators with QPatch™ Automated Patch-Clamp Technology: System Characteristics and Performance To cite this article:
    Year: 2004 First author: Kutchinsky et al., 2004
  • View Automated Patch Clamping Using the QPatch
    Year: 2009 First author: Jones et al. 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 First author: Korsgaard et al., 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 First author: Huang
  • View QPatch: the missing link between HTS and ion channel drug discovery.
    Year: 2009 First author: Mathes
  • View A new classifier-based strategy for in-silico ion-channel cardiac drug safety assessment
    Year: 2015 First author: Mistry et al., 2015
  • View Screening system for drug-induced arrhythmogenic risk combining a patch clamp and heart simulator
    Year: 2015 First author: Okada et al., 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 First author: Søren J Wacker et Al.
  • 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 First author: Bagchi et Al.
  • View Development of a selective inhibitor for Kv1.1 channels prevalent in demyelinated nerves
    Year: 2020 First author: Al-Sabi et Al.

Reports

  • View Stable Vhalf values and reliable potentiation of Kv7.3/7.2 currents on Qube 384
    Year: 2019 First author: Schupp
  • View Reliable Kv2.1 assasy and pharmacology on the QPatch
    Year: 2017 First author: Schupp et Al.
  • View CHO-hERG Duo characterization and functional validation on QPatch
    Year: 2011 First author: Jacobsen et al., 2011
  • View CHO-hERG Duo in multi-hole mode on QPatch
    Year: 2011 First author: Jacobsen et al., 2011
  • View Stable response for ligand and voltage-gated ion channels on QPatch
    Year: 2010 First author: Olsen et al., 2010

Kir

Reports

  • View HEK-hKir2.1 on QPatch
    Year: 2013 First author: Olsen et al., 2013

Kca1.1 & 3.1

Papers

  • View Development of a QPatch Automated Electrophysiology Assay for Identifying KCa3.1 Inhibitors and Activators
    Year: 2013 First author: Jenkins et al., 2013
  • View New positive Ca2+-activated K+ channel gating modulators with selectivity for KCa3.1
    Year: 2014 First author: Coleman et al., 2014
  • View Inhibition of the potassium channel KCa3.1 by senicapoc reverses tactile allodynia in rats with peripheral nerve injury
    Year: 2016 First author: Staala et al., 2016

Reports

  • View The intermediate conductance Ca2+ – activated K+ channel on Qube 384
    Year: 2017 First author: Sauter
  • View HEK293-KCa on QPatch
    Year: 2008 First author: Jacobsen et al., 2008

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 First author: Schupp et Al., 2018
  • View GABA-A receptor pharmacology evaluated in overexpressing HEK cells and primary astrocytes on QPatch
    Year: 2018 First author: Boddum et. Al
  • View Application of QPatch 16 for drug screening of ligand-gated ion channels
    Year: 2005 First author: Andersen et al., 2005
  • View Assessing functional properties of ligand-gated ion channels with automated whole-cell patch clamp technology
    Year: 2006 First author: Olsen et al., 2006
  • View Development and validation of ligand-gated ion channel assays using the Qube 384 automated electrophysiology platform
    Year: 2019 First author: Marklew et Al., 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 First author: K Frederiksen
  • 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 First author: Martin et al., 2015
  • View Electrophysiological Studies of GABA-A Receptors Using QPatch II, the Next Generation of Automated Patch‐Clamp Instruments
    Year: 2020 First author: Schupp et Al.
  • View Hybrid molecules combining GABA-A and serotonin 5-HT6 receptors activity designed to tackle neuroinflammation associated with depression
    Year: 2022 First author: Marcinkowska et al.

Reports

  • View Pharmacological evaluation of GABAA receptor subtypes on Qube 384
    Year: 2019 First author: Boddum et Al., 2019
  • View Ligand gated ion channels: GABAA receptor pharmacology on QPatch
    Year: 2018 First author: Boddum et Al

Stem cells

Posters

  • View Characterization of hiPSC-derived neurological disease models using automated patch clamp (Qube and QPatch)
    Year: 2019 First author: Rosholm et Al.
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