β-adrenergic
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β-adrenergic
The adrenergic receptors or adrenoceptors are a class of G protein-coupled receptors that are targets of many catecholamines like norepinephrine (noradrenaline) and epinephrine (adrenaline) produced by the body, but also many medications like beta blockers, beta-2 (β2) agonists and alpha-2 (α2) agonists, which are used to treat high blood pressure and asthma, for example. Many cells have these receptors, and the binding of a catecholamine to the receptor will generally stimulate the sympathetic nervous system (SNS). The SNS is responsible for the fight-or-flight response, which is triggered by experiences such as exercise or fear-causing situations. This response dilates pupils, increases heart rate, mobilizes energy, and diverts blood flow from non-essential organs to skeletal muscle. These effects together tend to increase physical performance momentarily. History By the turn of the 19th century, it was agreed that the stimulation of sympathetic nerves could cause dif ...
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Beta-2 Adrenergic Receptor
The beta-2 adrenergic receptor (β2 adrenoreceptor), also known as ADRB2, is a cell membrane-spanning beta-adrenergic receptor that binds epinephrine (adrenaline), a hormone and neurotransmitter whose signaling, via adenylate cyclase stimulation through trimeric Gs proteins, increases cAMP, and, via downstream L-type calcium channel interaction, mediates physiologic responses such as smooth muscle relaxation and bronchodilation. Robert Lefkowitz and Brian Kobilka's study of the beta-2 adrenergic receptor as a model system earned them the 2012 Nobel Prize in Chemistry "for studies of G-protein-coupled receptors". The official symbol for the human gene encoding the β2 adrenoreceptor is ''ADRB2''. Gene The gene is intronless. Different polymorphic forms, point mutations, and/or downregulation of this gene are associated with nocturnal asthma, obesity and type 2 diabetes. Structure The 3D crystallographic structure (see figure and links to the right) of the β2-adrener ...
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Beta Blocker
Beta blockers, also spelled β-blockers, are a class of medications that are predominantly used to manage abnormal heart rhythms ( arrhythmia), and to protect the heart from a second heart attack after a first heart attack ( secondary prevention). They are also widely used to treat high blood pressure, although they are no longer the first choice for initial treatment of most people. Beta blockers are competitive antagonists that block the receptor sites for the endogenous catecholamines epinephrine (adrenaline) and norepinephrine (noradrenaline) on adrenergic beta receptors, of the sympathetic nervous system, which mediates the fight-or-flight response. Beta-adrenergic receptors are found on cells of the heart muscles, smooth muscles, airways, arteries, kidneys, and other tissues that are part of the sympathetic nervous system and lead to stress responses, especially when they are stimulated by epinephrine (adrenaline). Beta blockers interfere with the binding to th ...
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Epinephrine
Adrenaline, also known as epinephrine, is a hormone and medication which is involved in regulating visceral functions (e.g., respiration). It appears as a white microcrystalline granule. Adrenaline is normally produced by the adrenal glands and by a small number of neurons in the medulla oblongata. It plays an essential role in the fight-or-flight response by increasing blood flow to muscles, heart output by acting on the SA node, pupil dilation response, and blood sugar level. It does this by binding to alpha and beta receptors. It is found in many animals, including humans, and some single-celled organisms. It has also been isolated from the plant '' Scoparia dulcis'' found in Northern Vietnam. Medical uses As a medication, it is used to treat several conditions, including allergic reaction anaphylaxis, cardiac arrest, and superficial bleeding. Inhaled adrenaline may be used to improve the symptoms of croup. It may also be used for asthma when other treatments are ...
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100-AdrenergicReceptors-2rh1
1 (one, unit, unity) is a number, numeral, and glyph. It is the first and smallest positive integer of the infinite sequence of natural numbers. This fundamental property has led to its unique uses in other fields, ranging from science to sports, where it commonly denotes the first, leading, or top thing in a group. 1 is the unit of counting or measurement, a determiner for singular nouns, and a gender-neutral pronoun. Historically, the representation of 1 evolved from ancient Sumerian and Babylonian symbols to the modern Arabic numeral. In mathematics, 1 is the multiplicative identity, meaning that any number multiplied by 1 equals the same number. 1 is by convention not considered a prime number. In digital technology, 1 represents the "on" state in binary code, the foundation of computing. Philosophically, 1 symbolizes the ultimate reality or source of existence in various traditions. In mathematics The number 1 is the first natural number after 0. Each natural numbe ...
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Adrenoreceptor Signal Transduction
The adrenergic receptors or adrenoceptors are a class of G protein-coupled receptors that are targets of many catecholamines like norepinephrine (noradrenaline) and epinephrine (adrenaline) produced by the body, but also many medications like beta blockers, beta-2 (β2) agonists and alpha-2 (α2) agonists, which are used to treat high blood pressure and asthma, for example. Many cells have these receptors, and the binding of a catecholamine to the receptor will generally stimulate the sympathetic nervous system (SNS). The SNS is responsible for the fight-or-flight response, which is triggered by experiences such as exercise or fear-causing situations. This response dilates pupils, increases heart rate, mobilizes energy, and diverts blood flow from non-essential organs to skeletal muscle. These effects together tend to increase physical performance momentarily. History By the turn of the 19th century, it was agreed that the stimulation of sympathetic nerves could cause dif ...
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Arturo Rosenblueth
Arturo Rosenblueth Stearns (October 2, 1900 Chihuahua – September 20, 1970 Mexico City) was a Mexican researcher, physician and physiologist, who is known as one of the pioneers of cybernetics. Biography Rosenblueth was born in 1900 in Ciudad Guerrero, Chihuahua. He began his studies in Mexico City, then traveled to Berlin and Paris where he obtained his medical degree. Returning to Mexico City in 1927, he engaged in teaching and research in physiology. In 1930, he obtained a Guggenheim Scholarship and moved to Harvard University, to work in the department of Physiology, then directed by Walter Cannon. With Cannon he explored the chemical mediation of homeostasis. Rosenblueth cowrote research papers with both Cannon and Norbert Wiener, pioneers of cybernetics. Notably he was the lead author for the 1943 article 'Behavior, Purpose and Teleology' that was co-written by Wiener and Julian Bigelow and which was published in ''Philosophy of Science''. Rosenblueth was an influent ...
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Henry Hallett Dale
Sir Henry Hallett Dale (9 June 1875 – 23 July 1968) was an English pharmacologist and physiologist. For his study of acetylcholine as agent in the chemical transmission of nerve pulses (neurotransmission) he shared the 1936 Nobel Prize in Physiology or Medicine with Otto Loewi. Early life and education Henry Hallett Dale was born in Islington, London, to Charles James Dale, a pottery manufacturer from Staffordshire, and his wife, Frances Anne Hallett, daughter of a furniture manufacturer, from South Devon.Feldberg W, rev. Tansey EM (2004–2011)Dale, Sir Henry Hallett (1875–1968) ''Oxford Dictionary of National Biography'', Oxford University Press, 2004; online edn, Jan 2011. Retrieved 2011-07-08. Henry was the third of seven children, one of whom (his younger brother, Benjamin Dale) became an accomplished composer and warden of the Royal Academy of Music. Henry was educated at the local Tollington Park College and then The Leys School Cambridge (one of the school's hou ...
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Ergot
Ergot ( ) or ergot fungi refers to a group of fungi of the genus ''Claviceps''. The most prominent member of this group is '' Claviceps purpurea'' ("rye ergot fungus"). This fungus grows on rye and related plants, and produces alkaloids that can cause ergotism in humans and other mammals who consume grains contaminated with its fruiting structure (called ''ergot sclerotium''). ''Claviceps'' includes about 50 known species, mostly in the tropical regions. Economically significant species include ''C. purpurea'' (parasitic on grasses and cereals), ''C. fusiformis'' (on pearl millet, buffel grass), '' C. paspali'' (on dallis grass), ''C. africana'' (on sorghum) and ''C. lutea'' (on paspalum). ''C. purpurea'' most commonly affects outcrossing species such as rye (its most common host), as well as triticale, wheat and barley. It affects oats only rarely. ''C. purpurea'' has at least three races or varieties, which differ in their host specificity: *G1 – land grasses of op ...
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Raymond Ahlquist
Raymond Perry Ahlquist (July 26, 1914 – April 15, 1983) was an American pharmacist and pharmacologist. He published seminal work in 1948 that divided adrenoceptors into Adrenergic receptor#.CE.B1 receptors, α- and Adrenergic receptor#.CE.B2 receptors, β-adrenoceptor subtypes. This discovery explained the activity of several existing drugs and also laid the groundwork for new drugs including the widely prescribed beta blockers. Early life and education Ahlquist was born on July 26, 1914, in Missoula, Montana. Both of his parents came from Sweden. His father was an auditor at the railway company Northern Pacific Railway. In 1940, Ahlquist graduated with a Ph.D. degree in pharmacology from the University of Washington in Seattle, the first person to be awarded such a degree from that institution. Career and research Ahlquist spent four years as a faculty member at South Dakota State University in Brookings. In 1944 he became assistant professor of pharmacology at the Medica ...
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Gq Alpha Subunit
Gq protein alpha subunit is a family of heterotrimeric G protein alpha subunits. This family is also commonly called the Gq/11 (Gq/G11) family or Gq/11/14/15 family to include closely related family members. G alpha subunits may be referred to as Gq alpha, Gαq, or Gqα. Gq proteins couple to G protein-coupled receptors to activate beta-type phospholipase C (PLC-β) enzymes. PLC-β in turn hydrolyzes phosphatidylinositol 4,5-bisphosphate (PIP2) to diacyl glycerol (DAG) and inositol trisphosphate (IP3). IP3 acts as a second messenger to release stored calcium into the cytoplasm, while DAG acts as a second messenger that activates protein kinase C (PKC). Family members In humans, there are four distinct proteins in the Gq alpha subunit family: * Gαq is encoded by the gene GNAQ. * Gα11 is encoded by the gene GNA11. * Gα14 is encoded by the gene GNA14. * Gα15 is encoded by the gene GNA15. Function The general function of Gq is to activate intracellular signalin ...
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Receptor Ligands
In biochemistry and pharmacology, a ligand is a substance that forms a complex with a biomolecule to serve a biological purpose. The etymology stems from Latin ''ligare'', which means 'to bind'. In protein-ligand binding, the ligand is usually a molecule which produces a signal by binding to a site on a target protein. The binding typically results in a change of conformational isomerism (conformation) of the target protein. In DNA-ligand binding studies, the ligand can be a small molecule, ion, or protein which binds to the DNA double helix. The relationship between ligand and binding partner is a function of charge, hydrophobicity, and molecular structure. Binding occurs by intermolecular forces, such as ionic bonds, hydrogen bonds and Van der Waals forces. The association or docking is actually reversible through dissociation. Measurably irreversible covalent bonding between a ligand and target molecule is atypical in biological systems. In contrast to the definition of ...
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