GABAA Receptor Antagonist
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GABAA Receptor Antagonist
GABA receptor antagonists are drugs that inhibit the action of GABA. In general these drugs produce stimulant and convulsant effects, and are mainly used for counteracting overdoses of sedative drugs. Examples include bicuculline, securinine and metrazol, and the benzodiazepine GABAA receptor antagonist flumazenil. Other agents which may have GABAA receptor antagonism include the antibiotic ciprofloxacin, tranexamic acid, thujone, ginkgo biloba, and kudzu Kudzu (), also called Japanese arrowroot or Chinese arrowroot, is a group of climbing, coiling, and trailing deciduous perennial vines native to much of East Asia, Southeast Asia, and some Pacific islands. It is invasive species, invasive in .... See also * GABAA receptor negative allosteric modulators External links * References Biochemistry {{nervous-system-drug-stub ...
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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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Ciprofloxacin
Ciprofloxacin is a fluoroquinolone antibiotic used to treat a number of bacterial infections. This includes bone and joint infections, intra-abdominal infections, certain types of infectious diarrhea, respiratory tract infections, skin infections, typhoid fever, and urinary tract infections, among others. For some infections it is used in addition to other antibiotics. It can be taken by mouth, as eye drops, as ear drops, or intravenously. Common side effects include nausea, vomiting, and diarrhea. Severe side effects include tendon rupture, hallucinations, and nerve damage. In people with myasthenia gravis, there is worsening muscle weakness. Rates of side effects appear to be higher than some groups of antibiotics such as cephalosporins but lower than others such as clindamycin. Studies in other animals raise concerns regarding use in pregnancy. No problems were identified, however, in the children of a small number of women who took the medication. It appear ...
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GABAA Receptor Negative Allosteric Modulator
A GABAA receptor negative allosteric modulator is a negative allosteric modulator (NAM), or inhibitor, of the GABAA receptor, a ligand-gated ion channel of the major inhibitory neurotransmitter γ-aminobutyric acid (GABA). They are closely related and similar to GABAA receptor antagonists. The effects of GABAA receptor NAMs are functionally the opposite of those of GABAA receptor positive allosteric modulators (PAMs) like the benzodiazepines, barbiturates, and ethanol (alcohol). Non-selective GABAA receptor NAMs can produce a variety of effects including convulsions, neurotoxicity, and anxiety, among others. Selective NAMs (or "inverse agonists") of α5 subunit-containing GABAA receptors, such as basmisanil and α5IA, do not have convulsant or anxiogenic effects but instead show cognitive- and memory-enhancing or nootropic-like effects. They are under investigation for the treatment of cognitive impairment in conditions like Down syndrome and schizophrenia. In addition, th ...
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Harvard Review Of Psychiatry
The ''Harvard Review of Psychiatry'' is a peer-reviewed medical journal covering all aspects of psychiatry. The editor-in-chief is Joshua L. Roffman. According to the ''Journal Citation Reports'', the journal has a 2017 impact factor The impact factor (IF) or journal impact factor (JIF) of an academic journal is a type of journal ranking. Journals with higher impact factor values are considered more prestigious or important within their field. The Impact Factor of a journa ... of 3.264. References External links * Academic journals established in 1993 Harvard University academic journals Psychiatry journals Bimonthly journals Lippincott Williams & Wilkins academic journals English-language journals {{psychiatry-journal-stub ...
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Kudzu
Kudzu (), also called Japanese arrowroot or Chinese arrowroot, is a group of climbing, coiling, and trailing deciduous perennial vines native to much of East Asia, Southeast Asia, and some Pacific islands. It is invasive species, invasive in many parts of the world, primarily North America. The vine densely climbs over other plants and trees and grows so rapidly that it smothers and kills them by blocking most of the sunlight and taking root space. The plants are in the genus ''Pueraria'', in the pea family Fabaceae, subfamily Faboideae. The name is derived from the Japanese language, Japanese name for the plant East Asian arrowroot, (''Pueraria montana'' var. ''lobata''), . Where these plants are Naturalisation (biology), naturalized, they can be invasive and are considered noxious weeds. The plant is edible, but often sprayed with herbicides. Taxonomy The name kudzu describes one or more species in the genus ''Pueraria'' that are closely related, and some of them are cons ...
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Journal Of Biological Chemistry
The ''Journal of Biological Chemistry'' (''JBC'') is a weekly peer-reviewed scientific journal that was established in 1905., jbc.org Since 1925, it is published by the American Society for Biochemistry and Molecular Biology. It covers research in areas of biochemistry and molecular biology. The editor is Alex Toker. the journal is fully open access. In press articles are available free on its website immediately after acceptance. Editors The following individuals have served as editors of the journal: * 1906–1909: John Jacob Abel and Christian Archibald Herter * 1909–1910: Christian Archibald Herter * 1910–1914: Alfred Newton Richards * 1914–1925: Donald D. Van Slyke * 1925–1936: Stanley R. Benedict. After Benedict died, John T. Edsall served as temporary editor until the next editor was appointed. * 1937–1958: Rudolph J. Anderson * 1958–1967: John T. Edsall * 1968–1971: William Howard Stein * 1971–2011: Herbert Tabor * 2011–2015: Martha Fedor * ...
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Ginkgo Biloba
''Ginkgo biloba'', commonly known as ginkgo or gingko ( ), also known as the maidenhair tree, is a species of gymnosperm tree native to East Asia. It is the last living species in the order Ginkgoales, which first appeared over 290 million years ago. Fossil, Fossils very similar to the living species, belonging to the genus ''Ginkgo'', extend back to the Middle Jurassic epoch approximately 170 million years ago. The tree was cultivated early in human history, remains commonly planted, and is widely regarded as a living fossil. ''G. biloba'' is a long-lived, Disease resistance, disease-resistant, Dioecy, dioecious tree with unique fan-shaped Leaf, leaves, capable of Cloning, clonal reproduction, and known for its striking yellow autumn foliage and resilience in disturbed environments. It was known historically as “silver fruit” or “white fruit” in Chinese language, Chinese and called “ginkgo” due to a centuries-old transcription error. It is closely related to Cycad, ...
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PNAS
''Proceedings of the National Academy of Sciences of the United States of America'' (often abbreviated ''PNAS'' or ''PNAS USA'') is a peer-reviewed multidisciplinary scientific journal. It is the official journal of the National Academy of Sciences, published since 1915, and publishes original research, scientific reviews, commentaries, and letters. According to '' Journal Citation Reports'', the journal has a 2022 impact factor of 9.4. ''PNAS'' is the second most cited scientific journal, with more than 1.9 million cumulative citations from 2008 to 2018. In the past, ''PNAS'' has been described variously as "prestigious", "sedate", "renowned" and "high impact". ''PNAS'' is a delayed open-access journal, with an embargo period of six months that can be bypassed for an author fee ( hybrid open access). Since September 2017, open access articles are published under a Creative Commons license. Since January 2019, ''PNAS'' has been online-only, although print issues are avail ...
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Thujone
Thujone () is a ketone and a terpene, monoterpene that occurs predominantly in two diastereomeric (epimeric) forms: (−)-α-thujone and (+)-β-thujone. Though it is best known as a chemical compound in the spirit absinthe, it is only present in trace amounts and is unlikely to be responsible for the spirit's purported stimulant and psychoactive effects. Thujone acts on the GABAA receptor, GABAA receptor as an antagonist. As a competitive antagonist of GABAA receptor, thujone alone is considered to be convulsant, though by interfering with the inhibitory transmitter GABA, it may convey stimulating, mood-elevating effects at low doses. It is also found in perfumery as a component of several essential oils. In addition to the naturally occurring (−)-α-thujone and (+)-β-thujone, two other forms are possible: (+)-α-thujone and (−)-β-thujone. In 2016, they were found in nature as well, in ''Salvia officinalis''. File:(-)-alpha-Thujon.svg, (−)-α-thujone File:Alpha-(+)-Thu ...
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Journal Of Pharmacology And Experimental Therapeutics
A journal, from the Old French ''journal'' (meaning "daily"), may refer to: *Bullet journal, a method of personal organization *Diary, a record of personal secretive thoughts and as open book to personal therapy or used to feel connected to oneself. A record of what happened over the course of a day or other period *Daybook, also known as a general journal, a daily record of financial transactions *Logbook, a record of events important to the operation of a vehicle, facility, or otherwise * Transaction log, a chronological record of data processing * Travel journal, a record of the traveller's experience during the course of their journey In publishing, ''journal'' can refer to various periodicals or serials: *Academic journal, an academic or scholarly periodical ** Scientific journal, an academic journal focusing on science ** Medical journal, an academic journal focusing on medicine ** Law review, a professional journal focusing on legal interpretation *Magazine, non-academic ...
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Tranexamic Acid
Tranexamic acid is a medication used to treat or prevent excessive blood loss from major trauma, postpartum bleeding, surgery, tooth removal, nosebleeds, and heavy menstruation. It is also used for hereditary angioedema. It is taken either by mouth, injection into a vein, or by intramuscular injection. Tranexamic acid is a synthetic analog of the amino acid lysine. It serves as an antifibrinolytic by reversibly binding four to five lysine receptor sites on plasminogen. This decreases the conversion of plasminogen to plasmin, preventing fibrin degradation and preserving the framework of fibrin's matrix structure. Tranexamic acid has roughly eight times the antifibrinolytic activity of an older analogue, ε-aminocaproic acid. Tranexamic acid also directly inhibits the activity of plasmin with weak potency ( IC50 = 87 mM), and it can block the active-site of urokinase plasminogen activator (uPA) with high specificity ( Ki = 2 mM), one of the highest among all the serine ...
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Flumazenil
Flumazenil, also known as flumazepil, is a selective GABAA receptor, GABAA receptor antagonist administered via injection, otic insertion, or intranasally. Therapeutically, it acts as both an antagonist and antidote to benzodiazepines (particularly in cases of overdose), through competitive inhibition. It was first characterized in 1981, and was first marketed in 1987 by Hoffmann-La Roche under the trade name Anexate. However, it did not receive FDA approval until December 1991. The developer lost its exclusive patent rights in 2008 and generic formulations are available. Intravenous therapy, Intravenous flumazenil is primarily used to treat benzodiazepine overdoses and to help reverse anesthesia. Administration of flumazenil by sublingual administration, sublingual lozenge and topical cream has also been tested. Medical uses Flumazenil benefits people who become excessively drowsy after use of benzodiazepines for either medical diagnosis, diagnostic or therapeutic procedures ...
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