T-type VDCC bind T-type VDCC blockers

Stable Identifier
R-HSA-9700701
Type
Reaction [binding]
Species
Homo sapiens
Compartment
extracellular region, plasma membrane
ReviewStatus
5/5
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T-type VDCC bind T-type VDCC blockers
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Voltage-dependent calcium channels (VDCCs) mediate the entry of calcium ions (Ca2+) into excitable cells as well as being involved in a variety of calcium-dependent processes, including muscle contraction, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. The CACN isoforms alpha-1G, alpha-1H and alpha1I give rise to T-type calcium currents which mediate pacemaking functions in both neurons and cardiac nodal cells and support calcium signaling in secretory cells and vascular smooth muscle.

Small molecules that block these channels (Perez-Reyes et al. 2009) are generally used to treat hypertension (Triggle 1997, Martin et al. 2000, Godfraind 2014), seizures in epilepsy (Zamponi 2016, Powell et al. 2014), vomiting, nausea and motion sickness (Zamponi et al. 2015).
Literature References
PubMed ID Title Journal Year
10991994 Mibefradil block of cloned T-type calcium channels

Martin, RL, Lee, JH, Cribbs, LL, Perez-Reyes, E, Hanck, DA

J. Pharmacol. Exp. Ther. 2000
26362469 The Physiology, Pathology, and Pharmacology of Voltage-Gated Calcium Channels and Their Future Therapeutic Potential

Zamponi, GW, Striessnig, J, Koschak, A, Dolphin, AC

Pharmacol. Rev. 2015
23834404 Low threshold T-type calcium channels as targets for novel epilepsy treatments

Powell, KL, Cain, SM, Snutch, TP, O'Brien, TJ

Br J Clin Pharmacol 2014
24872348 Calcium channel blockers in cardiovascular pharmacotherapy

Godfraind, T

J. Cardiovasc. Pharmacol. Ther. 2014
9481611 Cardiovascular T-type calcium channels: physiological and pharmacological significance

Triggle, DJ

J Hypertens Suppl 1997
18974361 Molecular pharmacology of human Cav3.2 T-type Ca2+ channels: block by antihypertensives, antiarrhythmics, and their analogs

Perez-Reyes, E, Van Deusen, AL, Vitko, I

J. Pharmacol. Exp. Ther. 2009
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Orthologous Events
T-type VDCC bind T-type VDCC blockers (Bos taurus)
T-type VDCC bind T-type VDCC blockers (Gallus gallus)
T-type VDCC bind T-type VDCC blockers (Saccharomyces cerevisiae)
T-type VDCC bind T-type VDCC blockers (Schizosaccharomyces pombe)
T-type VDCC bind T-type VDCC blockers (Sus scrofa)
Authored
Jassal, B  (2020-09-16)
Reviewed
Huddart, R  (2022-03-01)
Created
Jassal, B  (2020-09-16)
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