Disease areas - Pain

Pain

Pain is usually defined as an unpleasant sensory and emotional experience associated with actual or potential tissue damage, so pain serves as an important mechanism to prevent injury. The sense of pain occurs as the brain’s response to input from the periphery. Electrical and chemical changes that appear because of an injury, disease or damage to the body are conducted centrally by means of a whole array of ion channels, some initiate the stimulus, some conduct electrically and some transmit chemically across synapses.

 

There are two basic types of pain: neuropathic (nerve injury) pain and nociceptive (tissue) pain.
Neuropathic pain is caused by a primary lesion or dysfunction in the nervous system and it lasts long after healing of the damaged tissues and can turn into chronic pain. The nociceptive pain occurs when nociceptors are substance stimulated by damaged or inflamed tissue. The pain is usually time limited and serves a protective purpose.

 

There are many examples of ion channels involved in pain and they play different roles. Voltage gated Na+ channels are important for conduction along afferent nerve fibers, voltage gated Ca2+ channels are important for releasing neurotransmitters in the synaptic cleft and transient receptor potential ion channels (TRP), acid-sensing ion channels (ASIC), glutamate receptors (KA, NMDA and AMPA ligand gated ion channels) are involved in the primary response at the free terminals placed under the skin.

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Selection of ion channels involved in pain sensation and transmission:

 

Key Pain Ion Channels

Nav1.1, 1.6, 1.7 & 1.8 (1.3 after injury)
Cav1.2
TRP
P2X
NMDA, AMPA and KA
ASIC1-3

 

 


Nav1.1, 1.3, 1,4, 1.6, 1.7 & 1.8

Posters

  • View Biophysical and pharmacological characterization of multiple Nav subtypes on Qube
    Year: 2016 First author: Lindqvist et Al
  • View CHO-hNav1.7 assay on Qube pharmacology, biophysical characterization and the effect of internal fluoride
    Year: 2017 First author: Sauter et al., 2017
  • View Sophion analyzer as a tool for biophysical and pharmacological characterization of eight Nav subtypes evaluated in parallel on Qube
    Year: 2016 First author: Korsgaard et al., 2016
  • View Biophysical and pharmacological profiling of multiple Nav subtypes on QPatch HT
    Year: 2016 First author: Lindqvist et al., 2016
  • View “Clip Detecting” with series resistance compensation using an automated patch clamp system
    Year: 2012 First author: Løjkner et al., 2012
  • 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

Papers

  • View High-Throughput Screening of Nav1.7 Modulators Using a Giga-Seal Automated Patch Clamp Instrument
    Year: 2016 First author: Chambers et al., 2016
  • View Identification and Electrophysiological Evaluation of 2-Methylbenzamide Derivatives as Nav1.1 Modulators
    Year: 2015 First author: Crestey et al., 2015
  • View Characterization of Endogenous Sodium Channels in the ND7-23 Neuroblastoma Cell Line: Implications for Use as a Heterologous Ion Channel Expression System Suitable for Automated Patch Clamp Screening
    Year: 2016 First author: Rogers et al., 2016
  • View Engineering Highly Potent and Selective Microproteins Against Nav1.7 Sodium Channel for Treatment of Pain
    Year: 2016 First author: Shcherbatko et al., 2016
  • View Rational engineering defines a molecular switch that is essential for activity of spider-venom peptides against the analgesics target Nav1.7
    Year: 2015 First author: Klint et al., 2015
  • View Using automated patch clamp electrophysiology platforms in pain-related ion channel research: insights from industry and academia
    Year: 2017 First author: Bell

Reports

  • View CHO-hNav1.7 assay on Qube pharmacology, biophysical characterization and the effect of internal fluoride
    Year: 2017 First author: Sauter et al., 2017
  • View High throughput screening for mode-of-action on Nav1.4
    Year: 2017 First author: Sauter

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 Cav1.2 on Qube 384
    Year: 2017 First author: Schupp, M
  • View CHO Cav1.2 on QPatch (ChanTest)
    Year: 2011 First author: Friis et al., 2011
  • View Cor.At cells embryonic stem cell derived cardiomyocytes on QPatch
    Year: 2009 First author: Schrøder et al., 2009

TRP

Posters

  • View TRP’ing in multi-hole mode
    Year: 2010 First author: Jacobsen et al., 2010

Papers

  • View The development of automated patch clamp assays for canonical transient receptor potential channels TRPC3, 6, and 7
    Year: 2014 First author: McPate et Al.
  • View Study of TRP Channels by Automated Patch Clamp Systems
    Year: 2010 First author: Sunesen et al., 2010
  • View QPatch: the missing link between HTS and ion channel drug discovery.
    Year: 2009 First author: Mathes

Reports

  • View TRPM8 cold sensitive ion channels
    Year: 2012 First author: Jensen
  • View HEK293-TRPV1 on QPatch
    Year: 2011 First author: Jacobsen et al., 2011

P2X

Posters

  • View Pharmacological characterization of voltage- and ligand-gated ion channels
    Year: 2006 First author: Olsen et al., 2006

Papers

  • View Modulation of P2X3 and P2X2/3 Receptors by Monoclonal Antibodies
    Year: 2016 First author: Shcherbatko et al., 2016
  • View QPatch: the missing link between HTS and ion channel drug discovery.
    Year: 2009 First author: Mathes

Reports

  • View Validation of ligand-gated ion channels in multi-hole mode on QPatch
    Year: 2012 First author: Jacobsen et al., 2012
  • View CHO TREx-P2X3 on QPatch
    Year: 2008 First author: Schrøder et al., 2008

NMDA, AMPA and KA

Papers

  • View A novel substituted aminoquinoline selectively targets voltage-sensitive sodium channel isoforms and NMDA receptor subtypes and alleviates chronic inflammatory and neuropathic pain
    Year: 2016 First author: Tabakoff et al., 2016
  • View Positive allosteric modulators of α7 nicotinic acetylcholine receptors affect neither the function of other ligand- and voltage-gated ion channels and acetylcholinesterase, nor β-amyloid content
    Year: 2016 First author: Ariasa et al., 2016

ASIC1-3

Posters

  • View Application of QPatch 16 for drug screening of ligand-gated ion channels
    Year: 2005 First author: Andersen et al., 2005

Reports

  • View Ligand-gated ion channels on QPatch
    Year: 2012 First author: Jacobsen et al., 2012
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