Introduction
Ion channels expressed in the central nervous system (CNS) are closely linked to hereditary epilepsy. Gain-of-function mutations in excitatory ion channels—such as voltage-gated sodium channels (Nav1.1, Nav1.2, Nav1.3 and Nav1.6), the voltage-gated calcium channel Cav3.2, and hyperpolarization-activated HCN1 and HCN2 channels—have been shown to cause sustained depolarizing currents, leading to excessive neuronal excitability. This hyperexcitability serves as a key driver of epileptic seizures and convulsions.
Similarly, loss-of-function mutations in inhibitory channels, including the voltage-gated potassium channel KCNQ, calcium-activated potassium channel BK, and the ligand-gated chloride channel GABAA, can also result in hyperexcitability. Drug-induced side effects that mimic these mutation-related alterations in ion channel function can exacerbate neurological complications.
Other Relevant Channels: Chloride Channel (CLC-2): Helps maintain chloride homeostasis and neuronal stability; Ligand-Gated NMDA Receptors: Modulate excitatory neurotransmission, often implicated in seizure activity.
On the other hand, antiepileptic drugs often counteract these effects by inhibiting excitatory channels or activating inhibitory channels. Therefore, the ion channels included in our seizure-convulsion panel represent promising therapeutic targets for managing hyperexcitability-related conditions, including seizures, pain, neurodegeneration, anxiety, migraines, and psychosis, as well as for reducing the risk of adverse neurological events.
Seizure-Convulsion ion channel Portfolio
Our seizure-Convulsion Ion Channel Portfolio targets ion channels associated with the central nervous system (CNS), which play a critical role in the hyperexcitability underlying seizures and convulsions. This panel includes key excitatory and inhibitory ion channels linked to inherited forms of epilepsy and offers a platform for evaluating potential. this Seizure-Convulsion Ion Channel Portfolio provides a comprehensive framework for understanding and targeting the mechanisms of neuronal hyperexcitability in epilepsy and related conditions. By integrating key excitatory and inhibitory ion channels, this panel facilitates the development of targeted therapies to manage seizures with greater precision.
Ion channel Family | Target | Method | Species | Mode |
---|---|---|---|---|
Voltage-gated sodium channel | Nav1.1 | Manual patch clamp | human | Agonist or Antagonist |
Nav1.2 | Manual patch clamp | human | Agonist or Antagonist | |
Nav1.3 | Manual patch clamp | human | Agonist or Antagonist | |
Nav1.6 | Manual patch clamp | human | Agonist or Antagonist | |
Nav1.7 | Manual patch clamp | human | Agonist or Antagonist | |
Voltage-gated calcium channel | Cav2.1 | Manual patch clamp | human | Agonist or Antagonist |
Cav3.2 | Manual patch clamp | human | Agonist or Antagonist | |
Voltage-gated potassium channel | Kv1.2 | Manual patch clamp | human | Agonist or Antagonist |
Kv2.1 | Manual patch clamp | human | Agonist or Antagonist | |
Kv4.2 | Manual patch clamp | human | Agonist or Antagonist | |
Kv4.3 | Manual patch clamp | human | Agonist or Antagonist | |
KCNQ2/3 | Manual patch clamp | human | Agonist or Antagonist | |
Potassium channel, calcium activated | BK | Manual patch clamp | human | Agonist or Antagonist |
IK | Manual patch clamp | human | Agonist or Antagonist | |
SK2 | Manual patch clamp | human | Agonist or Antagonist | |
SK3 | Manual patch clamp | human | Agonist or Antagonist | |
Ligand-gated ion channel | GABAα1β2γ2 | Manual patch clamp | human | Agonist or Antagonist |
GABAα2β2γ2 | Manual patch clamp | human | Agonist or Antagonist | |
GABAα6β3γ2 | Manual patch clamp | human | Agonist or Antagonist | |
nAChRα4β2 | Manual patch clamp | human | Agonist or Antagonist | |
NR1/NR2A | Manual patch clamp | human | Agonist or Antagonist | |
NR1/NR2B | Manual patch clamp | human | Agonist or Antagonist | |
Hyperpolarization-activated channel | HCN1 | Manual patch clamp | human | Agonist or Antagonist |
HCN2 | Manual patch clamp | human | Agonist or Antagonist | |
Transient receptor potential channel | TRPV1 | Manual patch clamp | human | Agonist or Antagonist |
TRPV4 | Manual patch clamp | human | Agonist or Antagonist | |
TRPC6 | Manual patch clamp | human | Agonist or Antagonist | |
TRPM8 | Manual patch clamp | human | Agonist or Antagonist |
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