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N-type Calcium Channel
N-type calcium channels, also called Cav2.2 channels, are voltage gated calcium channels that are localized primarily on the nerve terminals and dendrites as well as neuroendocrine cells. The calcium N-channel consists of several subunits: the primary subunit α1B and the auxiliary subunits α2δ and β. The α1B subunit forms the pore through which the calcium enters and helps to determine most of the channel's properties. These channels play an important role in the neurotransmission during development. In the adult nervous system, N-type calcium channels are critically involved in the release of neurotransmitters, and in pain pathways. N-type calcium channels are the target of ziconotide, the drug prescribed to relieve intractable pain, intractable cancer pain. There are many known N-type calcium channel blockers that function to inhibit channel activity, although the most notable blockers are Conotoxin, ω-conotoxins. Structure N-type calcium channels are categorized as high ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Voltage Gated Calcium Channels
Voltage-gated calcium channels (VGCCs), also known as voltage-dependent calcium channels (VDCCs), are a group of voltage-gated ion channels found in the Cell membrane, membrane of excitable cells (''e.g.'' Muscle cell, muscle, glial cells, neurons) with a Permeability (electromagnetism), 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 depolarization, 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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Norepinephrine
Norepinephrine (NE), also called noradrenaline (NA) or noradrenalin, is an organic compound, organic chemical in the catecholamine family that functions in the brain and human body, body as a hormone, neurotransmitter and neuromodulator. The name "noradrenaline" (from Latin '':wikt:ad-, ad'', "near", and '':wikt:ren, ren'', "kidney") is more commonly used in the United Kingdom and the rest of the world, whereas "norepinephrine" (from Ancient Greek :wikt:ἐπί, ἐπῐ́ (''epí''), "upon", and :wikt:νεφρός, νεφρός (''nephrós''), "kidney") is usually preferred in the United States. "Norepinephrine" is also the international nonproprietary name given to norepinephrine (drug), the drug. Regardless of which name is used for the substance itself, parts of the body that produce or are affected by it are referred to as noradrenergic. The general function of norepinephrine is to mobilize the brain and body for action. Norepinephrine release is lowest during sleep, rise ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Desipramine
Desipramine, sold under the brand name Norpramin among others, is a tricyclic antidepressant (TCA) used in the treatment of depression. It acts as a relatively selective norepinephrine reuptake inhibitor, though it does also have other activities such as weak serotonin reuptake inhibitory, α1-blocking, antihistamine, and anticholinergic effects. The drug is not considered a first-line treatment for depression since the introduction of selective serotonin reuptake inhibitor (SSRI) antidepressants, which have fewer side effects and are safer in overdose. Medical uses Desipramine is primarily used for the treatment of depression. It may also be useful to treat symptoms of attention-deficit hyperactivity disorder (ADHD). Evidence of benefit is only in the short term, and with concerns of side effects its overall usefulness is not clear. Desipramine at very low doses is also used to help reduce the pain associated with functional dyspepsia. It has also been tried, albeit with littl ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cilnidipine
Cilnidipine is a calcium channel blocker. Cilnidipine is approved for use in Japan, China, India, Nepal, and Korea for hypertension. It is a calcium antagonist accompanied with L-type and N-type calcium channel blocking functions. Unlike other calcium antagonists, cilnidipine can act on the N-type calcium channel in addition to acting on the L-type calcium channel. It was patented in 1984 and approved for medical use in 1995. Cilnidipine is currently being repurposed and developed for use in patients with Raynaud's phenomenon and systemic sclerosis by Aisa Pharma, a US biopharma development company. Medical uses Cilnidipine decreases blood pressure and is used to treat hypertension and its comorbidities. Due to its blocking action at the N-type and L-type calcium channel, cilnidipine dilates both arterioles and venules, reducing the pressure in the capillary bed. Cilnidipine is vasoselective and has a weak direct dromotropic effect, a strong vasodepressor effect, and an a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Caroverine
Caroverine is an antispasmodic drug used in Austria and Switzerland to relieve spasms in smooth muscles, as well as to treat cerebrovascular diseases and tinnitus. Chemically, it is a quinoxalineone and is available in both a base and hydrochloric acid forms. Pharmacology Pharmacologically, it has been described as a nonspecific calcium channel blocker and as an antagonist of the NMDA receptor The ''N''-methyl-D-aspartate receptor (also known as the NMDA receptor or NMDAR), is a glutamate receptor and predominantly Ca2+ ion channel found in neurons. The NMDA receptor is one of three types of ionotropic glutamate receptors, the other ... and other receptors. History It was discovered in Austria in the 1950s and was developed by Austrian company Phafag AG. Its international nonproprietary name (INN), caroverine, was proposed in 1972. Society and culture Brand names As of 2018, it was marketed under the brand names Spasmium and Tinnitin in Austria, and under ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cadmium
Cadmium is a chemical element; it has chemical symbol, symbol Cd and atomic number 48. This soft, silvery-white metal is chemically similar to the two other stable metals in group 12 element, group 12, zinc and mercury (element), mercury. Like zinc, it demonstrates oxidation state +2 in most of its compounds, and like mercury, it has a lower melting point than the transition metals in group 3 element, groups 3 through group 11 element, 11. Cadmium and its Congener (chemistry), congeners in group 12 are often not considered transition metals, in that they do not have partly filled ''d'' or ''f'' electron shells in the elemental or common oxidation states. The average concentration of cadmium in Earth's crust is between 0.1 and 0.5 parts per million (ppm). It was discovered in 1817 simultaneously by Friedrich Stromeyer, Stromeyer and Karl Samuel Leberecht Hermann, Hermann, both in Germany, as an impurity in zinc carbonate. Cadmium occurs as a minor component in most zinc ores and i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Conotoxin
A conotoxin is one of a group of neurotoxic peptides isolated from the venom of the marine cone snail, genus '' Conus''. Conotoxins, which are peptides consisting of 10 to 30 amino acid residues, typically have one or more disulfide bonds. Conotoxins have a variety of mechanisms of actions, most of which have not been determined. However, it appears that many of these peptides modulate the activity of ion channels. Over the last few decades conotoxins have been the subject of pharmacological interest. The LD50 of conotoxin ranges from 5-25 μg/kg. Hypervariability Conotoxins are hypervariable even within the same species. They do not act within a body where they are produced (endogenously) but act on other organisms. Therefore, conotoxin genes experience less selection against mutations (like gene duplication and nonsynonymous substitution), and mutations remain in the genome longer, allowing more time for potentially beneficial novel functions to arise. Variability ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Central Nervous System
The central nervous system (CNS) is the part of the nervous system consisting primarily of the brain, spinal cord and retina. The CNS is so named because the brain integrates the received information and coordinates and influences the activity of all parts of the bodies of bilateria, bilaterally symmetric and triploblastic animals—that is, all multicellular animals except sponges and Coelenterata, diploblasts. It is a structure composed of nervous tissue positioned along the Anatomical_terms_of_location#Rostral,_cranial,_and_caudal, rostral (nose end) to caudal (tail end) axis of the body and may have an enlarged section at the rostral end which is a brain. Only arthropods, cephalopods and vertebrates have a true brain, though precursor structures exist in onychophorans, gastropods and lancelets. The rest of this article exclusively discusses the vertebrate central nervous system, which is radically distinct from all other animals. Overview In vertebrates, the brain and spinal ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ziconotide 1DW5
Ziconotide, sold under the brand name Prialt, also called intrathecal ziconotide (ITZ) because of its administration route, is an atypical analgesic agent for the amelioration of severe and chronic pain. Derived from ''Conus magus'', a cone snail, it is the synthetic form of an ω-conotoxin peptide. In December 2004 the US Food and Drug Administration (FDA) approved ziconotide when delivered as an infusion into the cerebrospinal fluid using an intrathecal pump system. Medical uses Due to the profound side effects or lack of efficacy when delivered through more common routes, such as orally or intravenously, ziconotide must be administered intrathecally (i.e., directly into the spinal fluid). As this is the most expensive and invasive method of drug delivery and involves additional risks of its own, ziconotide therapy is generally considered appropriate (as evidenced by the range of use approved by the FDA in the US) only for "management of severe chronic pain in patients for ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alcoholism
Alcoholism is the continued drinking of alcohol despite it causing problems. Some definitions require evidence of dependence and withdrawal. Problematic use of alcohol has been mentioned in the earliest historical records. The World Health Organization (WHO) estimated there were 283 million people with alcohol use disorders worldwide . The term ''alcoholism'' was first coined in 1852, but ''alcoholism'' and ''alcoholic'' are considered stigmatizing and likely to discourage seeking treatment, so diagnostic terms such as ''alcohol use disorder'' and ''alcohol dependence'' are often used instead in a clinical context. Alcohol is addictive, and heavy long-term alcohol use results in many negative health and social consequences. It can damage all the organ systems, but especially affects the brain, heart, liver, pancreas, and immune system. Heavy alcohol usage can result in trouble sleeping, and severe cognitive issues like dementia, brain damage, or Wernicke–Kors ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Intrathecal
Intrathecal administration is a route of administration for drugs via an injection into the spinal canal, or into the subarachnoid space (sin. ''intrathecal space'') so that it reaches the cerebrospinal fluid (CSF). It is useful in several applications, such as for spinal anesthesia, chemotherapy, or pain management. This route is also used to introduce drugs that fight certain infections, particularly post-neurosurgical. Typically, the drug is given this way to avoid being stopped by the blood–brain barrier, as it may not be able to pass into the brain when given orally. Drugs given by the intrathecal route often have to be compounded specially by a pharmacist or technician because they cannot contain any preservative or other potentially harmful inactive ingredients that are sometimes found in standard injectable drug preparations. Intrathecal pseudodelivery is a technique where the drug is encapsulated in a porous capsule that is placed in communication with the CSF. In this ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
G-protein
G proteins, also known as guanine nucleotide-binding proteins, are a family of proteins that act as molecular switches inside cells, and are involved in transmitting signals from a variety of stimuli outside a cell to its interior. Their activity is regulated by factors that control their ability to bind to and hydrolyze guanosine triphosphate (GTP) to guanosine diphosphate (GDP). When they are bound to GTP, they are 'on', and, when they are bound to GDP, they are 'off'. G proteins belong to the larger group of enzymes called GTPases. There are two classes of G proteins. The first function as monomeric small GTPases (small G-proteins), while the second function as heterotrimeric G protein complexes. The latter class of complexes is made up of ''alpha'' (Gα), ''beta'' (Gβ) and ''gamma'' (Gγ) subunits. In addition, the beta and gamma subunits can form a stable dimeric complex referred to as the beta-gamma complex . Heterotrimeric G proteins located within the cell ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
