Abstract
Despite their presence in many tissues and their potential implication in various disease states, low-voltage activated T-type calcium channels (T-channels) have only recently become targets of interest. Unfortunately, the lack of selective T-channel blockers has hampered further characterisation of these channels. The recent availability of cloned T-channels, the Ca(V)3 proteins, facilitates identification of novel T-channel blockers. Also, studies performed in knockout animals have fostered novel interest. Selective inhibition of T-channels may have clinical importance in cardiovascular diseases, some forms of epilepsy, sleep disorders, pain and possibly cancer. This review focuses on novel research approaches to discover potent and selective T-channel modulators. These molecules may be potential drugs for treating human diseases, as well as important tools to decipher the physiological role of these channels.
Publication types
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Research Support, Non-U.S. Gov't
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Review
MeSH terms
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Analgesics / pharmacology
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Analgesics / therapeutic use
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Animals
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Anticonvulsants / pharmacology
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Anticonvulsants / therapeutic use
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Arachidonic Acids / physiology
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Autistic Disorder / drug therapy
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Autistic Disorder / metabolism
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Calcium / physiology
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Calcium Channel Blockers / classification
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Calcium Channel Blockers / pharmacology*
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Calcium Channel Blockers / therapeutic use
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Calcium Channels, T-Type / deficiency
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Calcium Channels, T-Type / drug effects*
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Calcium Channels, T-Type / genetics
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Calcium Channels, T-Type / physiology
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Cardiovascular Agents / pharmacology
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Cardiovascular Agents / therapeutic use
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Cardiovascular Diseases / drug therapy
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Cardiovascular Diseases / metabolism
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Cations / pharmacology
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Drug Design
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Endocannabinoids
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Epilepsy / drug therapy
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Epilepsy / metabolism
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Humans
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Mice
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Mice, Knockout
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Polyunsaturated Alkamides
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Scorpion Venoms / pharmacology
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Sleep Disorders, Intrinsic / drug therapy
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Sleep Disorders, Intrinsic / metabolism
Substances
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Analgesics
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Anticonvulsants
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Arachidonic Acids
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CACNA1H protein, human
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Calcium Channel Blockers
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Calcium Channels, T-Type
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Cardiovascular Agents
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Cations
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Endocannabinoids
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Polyunsaturated Alkamides
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Scorpion Venoms
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kurtoxin
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Calcium
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anandamide