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Updated: Apr 25, 2026
Systemic and Local Drug Delivery for Treating Diseases of the Central Nervous System in Rodent Models
Published on: August 16, 2010
Recent patents on calcium channel blockers: emphasis on CNS diseases
Juan-Alberto Arranz-Tagarro1, Cristóbal de los Ríos, Antonio G García
1Instituto Teófilo Hernando, Universidad Autónoma de Madrid , Madrid , Spain.
Introduction:
Altered homeostasis of cell calcium movement is a central stage in multiple diseases of CNS. This explains the great therapeutic interest in blockers for the various subtypes of voltage-activated calcium channels (VACCs) expressed in neurons. Mitigation of Ca(2+) entry excess elicited by those blockers may restore the altered synaptic transmission, synaptic plasticity and gene expression to normal parameters, ending the enhanced neuronal vulnerability.
Areas Covered:
This review summarize 23 patents on ligands for L-, N- or T-type channels, claimed to have potential therapeutic interest in epilepsy, pain, migraine and neurodegenerative diseases.
Expert Opinion:
Collections of compounds are generally screened in cell lines expressing a given subtype of VACCs. IC50 to block such channels are often, but not always, provided. In few instances, compounds exhibiting the highest potency in in vitro experiments are also tested in animal models of pain, behavior, epilepsy or Alzheimer's disease. Attempts to develop selectivity for a given VACC subtype with non-peptidic organic ligands have so far failed. Due to their wide tissue expression, such selectivity is crucial for minimizing possible side effects. However, the few data reported by patents does not allow prediction of selectivity of the new compounds in many cases.
Insights
This review examines 23 patents on voltage-activated calcium channel (VACC) blockers for CNS diseases. Current non-peptidic ligands lack subtype selectivity, hindering therapeutic development for conditions like epilepsy and pain.
Area of Science:
- Neuroscience
- Pharmacology
- Biochemistry
Background:
- Altered calcium homeostasis is central to CNS diseases.
- Voltage-activated calcium channels (VACCs) in neurons are key therapeutic targets.
- Blocking excessive calcium influx can restore neuronal function.
Purpose of the Study:
- To review patents on VACC ligands for neurological disorders.
- To assess the therapeutic potential of these VACC blockers.
Main Methods:
- Summarized 23 patents on ligands targeting L-, N-, or T-type calcium channels.
- Reviewed in vitro screening data (IC50 values) and in vivo animal model testing.
Main Results:
- Compounds were screened in cell lines expressing specific VACC subtypes.
- In vitro potency data was often provided, with some in vivo testing.
- Non-peptidic ligands have thus far failed to achieve VACC subtype selectivity.
Conclusions:
- Selectivity for VACC subtypes is crucial for minimizing side effects due to wide tissue expression.
- Current patent data is insufficient to predict the selectivity of new compounds.
- Further research is needed to develop selective VACC modulators for CNS diseases.
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