Sodium Channel
Sodium channels are integral membrane proteins that form ion channels, conducting sodium ions (Na+) through a cell's plasma membrane. They are classified according to the trigger that opens the channel for such ions, i.e. either a voltage-change ("Voltage-gated", "voltage-sensitive", or "voltage-dependent" sodium channel also called "VGSCs" or "Nav channel") or a binding of a substance (a ligand) to the channel (ligand-gated sodium channels). In excitable cells such as neurons, myocytes, and certain types of glia, sodium channels are responsible for the rising phase of action potentials.
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Amiloride hydrochloride dihydrate is a potent epithelial sodium channel blocker. Amilorida is the hydrochloride dehydrate of amiloride. Amiloride hydrochloride dihydrate works by directly blocking the epithelial sodium channel thereby inhibiting sodium reabsorption in the late distal convoluted tubules, connecting tubules, and collecting ducts in the kidneys (this mechanism is the same for triamterene). This promotes the loss of sodium and water from the body, but without depleting potassium. Amiloride hydrochloride dihydrate also carries the risk of developing an acidosis. A fraction of the effects of amiloride is inhibition of cyclic GMP-gated cation channels in the inner medullary collecting duct. Amiloride hydrochloride dihydrate has a second action on the heart, blocking Na+/H+ exchangers Sodium-hydrogen antiporter 1 or NHE-1. This minimizes reperfusion injury in ischemic attacks. Acid-Sensing ion channels are also sensitive to inhibition by Amiloride hydrochloride dihydrate.
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Riluzole (利鲁唑) 是谷氨酸盐拮抗剂。
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Clemastine Fumarate是一种选择性组胺H1受体拮抗剂，IC50为3 nM。
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Oxibendazole是广谱的驱虫剂。
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Tripelennamine盐酸盐是H1受体拮抗剂。
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