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Enkephalinase Inhibitor
An enkephalinase inhibitor is a type of enzyme inhibitor which inhibits one or more members of the enkephalinase class of enzymes that break down the endogenous enkephalin opioid peptides. Examples include racecadotril, ubenimex (bestatin), RB-101, and D-phenylalanine, as well as the endogenous opioid peptides opiorphin and spinorphin. It also includes RB-3007, Semax and Selank. Analgesic, anticraving, antidepressant, anxiolytic, and antidiarrheal effects are common properties of enkephalinase inhibitors. See also * Enkephalinase * Enkephalin An enkephalin is a pentapeptide involved in regulating nociception in the body. The enkephalins are termed endogenous ligands, as they are internally derived and bind to the body's opioid receptors. Discovered in 1975, two forms of enkephal ... References Analgesics Antidiarrhoeals {{analgesic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Enzyme Inhibitor
An enzyme inhibitor is a molecule that binds to an enzyme and blocks its activity. Enzymes are proteins that speed up chemical reactions necessary for life, in which substrate molecules are converted into products. An enzyme facilitates a specific chemical reaction by binding the substrate to its active site, a specialized area on the enzyme that accelerates the most difficult step of the reaction. An enzyme inhibitor stops ("inhibits") this process, either by binding to the enzyme's active site (thus preventing the substrate itself from binding) or by binding to another site on the enzyme such that the enzyme's catalysis of the reaction is blocked. Enzyme inhibitors may bind reversibly or irreversibly. Irreversible inhibitors form a chemical bond with the enzyme such that the enzyme is inhibited until the chemical bond is broken. By contrast, reversible inhibitors bind non-covalently and may spontaneously leave the enzyme, allowing the enzyme to resume its function. Reve ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Semax
Semax is a drug which is used mostly in Russia and Ukraine for a broad range of conditions but predominantly for its purported nootropic, neuroprotective, and neurorestorative properties. Semax has not been evaluated, approved for use, or marketed in most other countries. Medical uses Semax has undergone extensive study in Russia and is on the Russian ''List of Vital & Essential Drugs'' approved by the Russian Federation government on December 7, 2011. Medical uses for Semax include treatment of stroke, transient ischemic attack, memory and cognitive disorders, peptic ulcers, optic nerve disease, and to boost the immune system. Pharmacology Pharmacodynamics In animals, Semax rapidly elevates the levels and expression of brain-derived neurotrophic factor (BDNF) and its signaling receptor TrkB in the hippocampus, and rapidly activates serotonergic and dopaminergic brain systems. Accordingly, it has been found to produce antidepressant-like and anxiolytic-like effects, attenu ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Analgesics
An analgesic drug, also called simply an analgesic (American English), analgaesic (British English), pain reliever, or painkiller, is any member of the group of drugs used to achieve relief from pain (that is, analgesia or pain management). It is typically used to induce cooperation with a medical procedure. Analgesics are conceptually distinct from anesthetics, which temporarily reduce, and in some instances eliminate, sensation, although analgesia and anesthesia are neurophysiologically overlapping and thus various drugs have both analgesic and anesthetic effects. Analgesic choice is also determined by the type of pain: For neuropathic pain, traditional analgesics are less effective, and there is often benefit from classes of drugs that are not normally considered analgesics, such as tricyclic antidepressants and anticonvulsants. Various analgesics, such as many NSAIDs, are available over the counter in most countries, whereas various others are prescription drugs owing t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Enkephalin
An enkephalin is a pentapeptide involved in regulating nociception in the body. The enkephalins are termed endogenous ligands, as they are internally derived and bind to the body's opioid receptors. Discovered in 1975, two forms of enkephalin have been found, one containing leucine ("leu"), and the other containing methionine ("met"). Both are products of the proenkephalin gene. * Met-enkephalin is Tyr-Gly-Gly-Phe-Met. * Leu-enkephalin has Tyr-Gly-Gly-Phe-Leu. Endogenous opioid peptides There are three well-characterized families of opioid peptides produced by the body: enkephalins, B-endorphin, and dynorphins. The met-enkephalin peptide sequence is coded for by the enkephalin gene; the leu-enkephalin peptide sequence is coded for by both the enkephalin gene and the dynorphin gene. The proopiomelanocortin gene (POMC) also contains the met-enkephalin sequence on the N-terminus of beta-endorphin, but the endorphin peptide is not processed into enkephalin. Effects on stre ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Enkephalinase
Enkephalinases are enzymes that degrade endogenous enkephalin opioid peptides. They include: * Aminopeptidase N (APN) * Neutral endopeptidase (NEP) * Dipeptidyl peptidase 3 (DPP3) * Carboxypeptidase A6 (CPA6) * Leucyl/cystinyl aminopeptidase (LNPEP) * Angiotensin-converting enzyme (ACE) See also * Enkephalinase inhibitor * Oxytocinase Oxytocinase is a type of enzyme that metabolizes the endogenous neuropeptide, oxytocin. The most well-characterized oxytocinase is leucyl/cystinyl aminopeptidase, which is also an enkephalinase. Other oxytocinases are also known. During pregnancy, o ... References Hydrolases Human proteins Nociception {{Enzyme-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antidiarrheal
An anti-diarrhoeal drug (or anti-diarrheal drug in American English) is any medication which provides symptomatic relief for diarrhoea. Types * Electrolyte solutions, while not true antidiarrhoeals, are used to replace lost fluids and salts in acute cases. * Bulking agents like methylcellulose, guar gum or plant fibre (bran, sterculia, isabgol, etc.) are used for diarrhoea in functional bowel disease and to control ileostomy output. * Absorbents absorb toxic substances that cause infective diarrhoea, methylcellulose is an absorbent. * Anti-inflammatory compounds such as bismuth subsalicylate. * Anticholinergics reduce intestinal movement and are effective against both diarrhoea and accompanying cramping. * Opioids' classical use besides pain relief is as an anti-diarrhoeal drug. Opioids have agonist actions on the intestinal opioid receptors, which when activated cause constipation. Drugs such as morphine or codeine can be used to relieve diarrhoea this way. A notable opioid fo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Anxiolytic
An anxiolytic (; also antipanic or antianxiety agent) is a medication or other intervention that reduces anxiety. This effect is in contrast to anxiogenic agents which increase anxiety. Anxiolytic medications are used for the treatment of anxiety disorders and their related psychological and physical symptoms. Nature of anxiety Anxiety is a naturally-occurring emotion and an innate response of the body to the environmental stimuli. Mild to moderate anxiety would increase level of performance. However, when anxiety levels exceed the tolerability of a person, anxiety disorders may occur. People with anxiety disorders can exhibit fear responses such as defensive behaviors, high levels of alertness and negative emotions, without external stimuli which induce anxiety within an individual. Those with anxiety disorders are also often found to have concurrent psychological disorders, most commonly depression. Anxiety disorders are divided into 6 types in clinical recognition. They are a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antidepressant
Antidepressants are a class of medication used to treat major depressive disorder, anxiety disorders, chronic pain conditions, and to help manage addictions. Common Side effect, side-effects of antidepressants include Xerostomia, dry mouth, weight gain, dizziness, headaches, sexual dysfunction, and emotional blunting. There is a slight increased risk of suicidal thinking and behavior when taken by children, adolescents, and young adults. Antidepressant discontinuation syndrome, Discontinuation syndrome may occur after stopping any antidepressant which resembles recurrent depression. Some research regarding the effectiveness of antidepressants for depression in adults has found benefits, whilst other research has not. Evidence of benefit in children and adolescents is unclear. The twenty-one most commonly prescribed antidepressant medications are more effective than placebo for the short-term (acute) treatments of adults with major depressive disorder. There is debate in the medic ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Anticraving
Substance dependence, also known as drug dependence, is a biopsychological situation whereby an individual's functionality is dependent on the necessitated re-consumption of a psychoactive substance because of an adaptive state that has developed within the individual from psychoactive substance consumption that results in the experience of withdrawal and that necessitates the re-consumption of the drug. A ''drug addiction'', a distinct concept from substance dependence, is defined as compulsive, out-of-control drug use, despite negative consequences. An ''addictive drug'' is a drug which is both rewarding and reinforcing. ΔFosB, a gene transcription factor, is now known to be a critical component and common factor in the development of virtually all forms of behavioral and drug addictions, but not dependence. The International Classification of Diseases classifies substance dependence as a mental and behavioural disorder. Within the framework of the 4th edition of the '' Diag ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Analgesic
An analgesic drug, also called simply an analgesic (American English), analgaesic (British English), pain reliever, or painkiller, is any member of the group of drugs used to achieve relief from pain (that is, analgesia or pain management). It is typically used to induce cooperation with a medical procedure. Analgesics are conceptually distinct from anesthetics, which temporarily reduce, and in some instances eliminate, sensation, although analgesia and anesthesia are neurophysiologically overlapping and thus various drugs have both analgesic and anesthetic effects. Analgesic choice is also determined by the type of pain: For neuropathic pain, traditional analgesics are less effective, and there is often benefit from classes of drugs that are not normally considered analgesics, such as tricyclic antidepressants and anticonvulsants. Various analgesics, such as many NSAIDs, are available over the counter in most countries, whereas various others are prescription drugs owi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Selank
Selank ( Russian: Cеланк) is a nootropic, anxiolytic peptide based drug developed by the Institute of Molecular Genetics of the Russian Academy of Sciences. Selank is a heptapeptide with the sequence Thr-Lys-Pro-Arg-Pro-Gly-Pro (TKPRPGP). It is a synthetic analogue of human tuftsin. Pharmacology Selank is a synthetic analogue of the immunomodulatory peptide tuftsin; as such, it mimics many of its effects. It has been shown to modulate the expression of Interleukin-6 (IL-6) and affect the balance of T helper cell cytokines. It has been shown to influence the concentration of monoamine neurotransmitters and induce metabolism of serotonin. Selank has also been found to rapidly elevate the expression of brain-derived neurotrophic factor (BDNF) in the hippocampus of rats. Selank, as well as a related peptide drug, Semax, have been found to inhibit enzymes involved in the degradation of enkephalins and other endogenous regulatory peptides, and this action may be involved in th ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
RB-3007
RB-3007 is an orally active analogue of RB-101. It acts as an enkephalinase inhibitor, which is used in scientific research. See also * RB-101 - enkephalinase inhibitor that produces analgesia without respiratory depression * Phenylalanine, D/DL-Phenylalanine - D-phenylalanine blockage of enkephalin degradation may be responsible for the reputed analgesic, analgesic effect of DL-Phenylalanine * Racecadotril - an antidiarrheal, antidiarrheal drug which acts as a peripheral enkephalinase inhibitor * Ecadotril - a neutral endopeptidase inhibitor References {{reflist Enkephalinase inhibitors Organophosphates ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
