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Modulation of Neuronal T-Type Calcium Channels
CNS & Neurological Disorders - Drug Targets, 2006As T-type calcium channels open near resting membrane potential and markedly influence neuronal excitability their activity needs to be tightly regulated. Few neuronal T-current regulations have been described so far, but interestingly some of them involve unusual mechanisms like G protein-independent but receptor-coupled modulation, while the use of ...
R C, Lambert, T, Bessaih, N, Leresche
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Regulation of neuronal T-type calcium channels
Trends in Pharmacological Sciences, 2009T-type calcium channels are critically important for regulating neuronal excitability, both in the central and peripheral nervous system, and are essential mediators of hormone secretion. Conversely, T-type channel hyperactivity has been linked to neurological disorders such as absence epilepsy and neuropathic pain.
Mircea C, Iftinca, Gerald W, Zamponi
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Discovery of potent T-type calcium channel blocker
Bioorganic & Medicinal Chemistry Letters, 2007The intensive SAR study of 3,4-dihydroquinazoline series led to the most potent compound 10 (KYS05090: IC(50)=41+/-1 nM) against T-type calcium channel and its potency is nearly comparable to that of Kurtoxin. As a small organic molecule, this compound showed the highest blocking activity reported to date.
Han Na, Seo +8 more
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Cardiovascular T-type calcium channels
Journal of Hypertension, 1997CELLULAR CALCIUM REGULATION: A variety of Ca2+ control processes are responsible for Ca2+ homeostasis and signaling. Voltage-gated Ca2+ channels are dominant in the cardiovascular system. VOLTAGE-GATED Ca2+ CHANNELS: There are several distinct subclasses of Ca2+ channels, distinguished by location, biophysical, structural and pharmacological ...
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T-type Calcium Channels in Health and Disease
Current Medicinal Chemistry, 2020Low Voltage-Activated (LVA) T-type calcium channels are characterized by transient current and Low Threshold Spikes (LTS) that trigger neuronal firing and oscillatory behavior. Combined with their preferential localization in dendrites and their specific “window current”, T-type calcium channels are considered ...
Dan, Wang +2 more
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A T-type calcium channel from mouse brain
Pfl�gers Archiv European Journal of Physiology, 1999A member of the low-voltage-activated calcium channel family was identified in mouse brain by taking advantage of amino acid sequences that have been evolutionary conserved. The identified sequence is similar to that of the recently cloned rat alpha1G T-type calcium channel, but there are differences in two insertions in the intracellular connecting ...
N, Klugbauer +3 more
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T-type calcium channels: The never ending story
Cell Calcium, 2006T-type, or low-voltage-activated (LVA), tiny and transient Ca2+ currents pare more and more recognised as universal players in a plethora of cell functions and are also more and more connected to several diseases. This short introduction reviews the discovery of T-type Ca2+ channels, describes its basic properties and sketches its cloning and ...
Nilius, Bernd +2 more
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Mibefradil Block of Cloned T-Type Calcium Channels
The Journal of Pharmacology and Experimental Therapeutics, 2000Mibefradil is a tetralol derivative chemically distinct from other calcium channel antagonists. It is a very effective antihypertensive agent that is thought to achieve its action via a higher affinity block for low-voltage-activated (T) than for high-voltage-activated (L) calcium channels.
R L, Martin +4 more
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[T-type calcium channel blockers].
Clinical calcium, 2005T-type calcium channels play an important role in regulating cell function in various kinds of organs, especially in cardiovascular systems. They have been recently clarified to be involved in various pathophysiological conditions, and clinically used for treatment of a variety of diseases.
Toshiaki, Nakajima +2 more
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T‐type Calcium Channels in Pulmonary Vascular Endothelium
Microcirculation, 2006ABSTRACTThe expression of low‐voltage‐gated T‐type calcium channel α1G‐subunit (Cav3.1) has recently been revealed in pulmonary microvascular endothelial cells (PMVECs). In endothelial cells, changes in membrane potential may be caused by a variety of physiological or pathophysiological vascular stimuli.
Chun, Zhou, Songwei, Wu
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