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Calcium Channel Opener
A calcium channel opener is a type of drug which facilitates ion transmission through calcium channels. An example is Bay K8644, which is an analogue of nifedipine that specifically and directly activates L-type voltage-dependent calcium channels. In contrast to Bay K8644, which is not for clinical use, ambroxol is a frequently used mucolytic drug that triggers lysosomal secretion by mobilizing calcium from acidic calcium stores. This effect does most likely not occur by a direct interaction between the drug and a lysosomal calcium channel, but indirectly by neutralizing the acidic pH within lysosomes. Calcium permeable ion channels in lysosomal membranes that may be activated by a luminal pH increase include two pore channels (TPCs), mucolipin TRP channels (TRPMLs) and purinergic receptors of the P2X channel type. See also * Calcium channel blocker Calcium channel blockers (CCB), calcium channel antagonists or calcium antagonists are a group of medications that disrupt ...
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Drug
A drug is any chemical substance other than a nutrient or an essential dietary ingredient, which, when administered to a living organism, produces a biological effect. Consumption of drugs can be via insufflation (medicine), inhalation, drug injection, injection, smoking, ingestion, absorption (skin), absorption via a dermal patch, patch on the skin, suppository, or sublingual administration, dissolution under the tongue. In pharmacology, a drug is a chemical substance, typically of known structure, which, when administered to a living organism, produces a biological effect. A pharmaceutical drug, also called a medication or medicine, is a chemical substance used to pharmacotherapy, treat, cure, preventive healthcare, prevent, or medical diagnosis, diagnose a disease or to promote well-being. Traditionally drugs were obtained through extraction from medicinal plants, but more recently also by organic synthesis. Pharmaceutical drugs may be used for a limited duration, or on a re ...
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Calcium Channel
A calcium channel is an ion channel which shows selective permeability to calcium ions. It is sometimes synonymous with voltage-gated calcium channel, which are a type of calcium channel regulated by changes in membrane potential. Some calcium channels are regulated by the binding of a ligand.Striggow F, Ehrlich BE (August 1996). "Ligand-gated calcium channels inside and out". ''Current Opinion in Cell Biology''. 8 (4): 490–495. Doi (identifier), doi:doi:10.1016/S0955-0674(96)80025-1, 10.1016/S0955-0674(96)80025-1. PMID (identifier), PMID]8791458 Other calcium channels can also be regulated by both voltage and ligands to provide precise control over ion flow. Some cation channels allow calcium as well as other cations to pass through the membrane. Calcium channels can participate in the creation of Action potential, action potentials across cell membranes. Calcium channels can also be used to release calcium ions as Second messenger system, second messengers within the cell, affec ...
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Bay K8644
Bay K8644 is a chemical compound that functions as an L-type calcium channel agonist An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an R .... Bay K8644 is used primarily as a biochemical research tool for this effect. It is a structural analog of nifedipine with positive inotropic activity, and as an aromatic it is highly lipid soluble. Mechanism of action Bay K8644 targets L-type voltage-gated calcium channels. It is the first positive inotropic agent shown to act specifically and directly on calcium channels. References Dihydropyridines Trifluoromethyl compounds Methyl esters Calcium channel openers Nitro compounds {{cardiovascular-drug-stub ...
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Structural Analog
A structural analog, also known as a chemical analog or simply an analog, is a chemical compound, compound having a chemical structure, structure similar to that of another compound, but differing from it in respect to a certain component. It can differ in one or more atoms, functional groups, or substructures, which are replaced with other atoms, groups, or substructures. A structural analog can be imagined to be formed, at least theoretically, from the other compound. Structural analogs are often isoelectronicity, isoelectronic. Despite a high chemical similarity, structural analogs are not necessarily functional analog (chemistry), functional analogs and can have very different physical, chemical, biochemical, or pharmacological properties. In drug discovery, either a large series of structural analogs of an initial lead compound are created and tested as part of a structure–activity relationship study or a database is virtual screening, screened for structural analogs of a ...
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Nifedipine
Nifedipine ( ), sold under the brand name Procardia among others, is a calcium channel blocker medication used to manage angina, high blood pressure, Raynaud's phenomenon, and premature labor. It is one of the treatments of choice for Prinzmetal angina. It may be used to treat severe high blood pressure in pregnancy. Its use in preterm labor may allow more time for steroids to improve the baby's lung function and provide time for transfer of the mother to a well qualified medical facility before delivery. It is a calcium channel blocker of the dihydropyridine type. Nifedipine is taken by mouth and comes in fast- and slow-release formulations. Common side effects include lightheadedness, headache, feeling tired, leg swelling, cough, and shortness of breath. Serious side effects may include low blood pressure and heart failure. Nifedipine is considered safe in pregnancy and breastfeeding. Nifedipine was patented in 1967, and approved for use in the United States in 1981. I ...
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L-type Calcium Channel
The L-type calcium channel (also known as the dihydropyridine channel, or DHP channel) is part of the high-voltage activated family of voltage-dependent calcium channel. "L" stands for long-lasting referring to the length of activation. This channel has four isoforms: Cav1.1, Cav1.2, Cav1.3, and Cav1.4. L-type calcium channels are responsible for the excitation- contraction coupling of skeletal, smooth, cardiac muscle, and for aldosterone secretion in endocrine cells of the adrenal cortex. They are also found in neurons, and with the help of L-type calcium channels in endocrine cells, they regulate neurohormones and neurotransmitters. They have also been seen to play a role in gene expression, mRNA stability, neuronal survival, ischemic-induced axonal injury, synaptic efficacy, and both activation and deactivation of other ion channels. In cardiac myocytes, the L-type calcium channel passes inward Ca2+ current (ICaL) and triggers calcium release from the sarcoplasmic ...
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Voltage-dependent Calcium Channel
Voltage-gated calcium channels (VGCCs), also known as voltage-dependent calcium channels (VDCCs), are a group of voltage-gated ion channels found in the membrane of excitable cells (''e.g.'' muscle, glial cells, neurons) with a permeability to the calcium ion Ca2+. These channels are slightly permeable to sodium ions, so they are also called Ca2+–Na+ channels, but their permeability to calcium is about 1000-fold greater than to sodium under normal physiological conditions. At physiologic or resting membrane potential, VGCCs are normally closed. They are activated (''i.e.'': opened) at depolarized membrane potentials and this is the source of the "voltage-gated" epithet. The concentration of calcium (Ca2+ ions) is normally several thousand times higher outside the cell than inside. Activation of particular VGCCs allows a Ca2+ influx into the cell, which, depending on the cell type, results in activation of calcium-sensitive potassium channels, muscular contraction, excit ...
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Ambroxol
Ambroxol is a drug that breaks up phlegm, used in the treatment of respiratory diseases associated with viscid or excessive mucus. Ambroxol is often administered as an active ingredient in cough syrup. It was patented in 1966 and came into medical use in 1979. Medical uses Ambroxol is indicated as "secretolytic therapy in bronchopulmonary diseases associated with abnormal mucus secretion and impaired mucus transport. It promotes mucus clearance, facilitates expectoration and eases productive cough, allowing patients to breathe freely and deeply". There are many different formulations developed since the first marketing authorisation in 1978. Ambroxol is available as syrup, tablets, pastilles, dry powder sachets, inhalation solution, drops and ampules as well as effervescent tablets. Ambroxol also provides pain relief in acute sore throat. Pain in sore throat is the hallmark of acute pharyngitis. Sore throat is usually caused by a viral infection. The infection is se ...
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Calcium Channel Blocker
Calcium channel blockers (CCB), calcium channel antagonists or calcium antagonists are a group of medications that disrupt the movement of calcium () through calcium channels. Calcium channel blockers are used as antihypertensive drugs, i.e., as medications to decrease blood pressure in patients with hypertension. CCBs are particularly effective against large vessel stiffness, one of the common causes of elevated Systole, systolic blood pressure in elderly care, elderly patients. Calcium channel blockers are also frequently used to alter heart rate (especially from atrial fibrillation), to prevent peripheral and cerebral vasospasm, and to reduce chest pain caused by angina pectoris. N-type calcium channel, N-type, L-type calcium channel, L-type, and T-type calcium channel, T-type voltage-dependent calcium channels are present in the zona glomerulosa of the adrenal gland, human adrenal gland, and CCBs can directly influence the biosynthesis of aldosterone in adrenal cortex, adreno ...
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