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Beta3-adrenergic Agonist
The β3 (beta 3) adrenergic receptor agonist or β3-adrenoceptor agonist, also known as β3-AR agonist, are a class of medicine that bind selectively to β3-adrenergic receptors. β3-AR agonists for the treatment of obesity and type 2 diabetes have been in developmental stages within many large pharmaceutical companies since the early 1990s without successfully delivering an anti-obesity product to the market. More recently pharmaceutical companies have developed selective β3-AR agonists targeted at urinary inconsistencies and in 2012 Mirabegron (trade name Myrbetriq and Betmiga) was the first β3-AR agonist to be approved in the United States and Europe for the treatment of overactive bladder (OAB) syndrome. Medical Uses In 2018 only one β3-AR agonist is approved by the European Medicines Agency (EMA) and the Food and drug Administration (FDA) as a medicine. The medicine is called Mirabegron and is used to treat OAB. Urinary bladder Mirabegron is a selective β3-AR agon ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Mirabegron
Mirabegron, sold under the brand name Myrbetriq among others, is a medication used to treat overactive bladder. Its benefits are similar to antimuscarinic medication such as solifenacin or tolterodine. It is taken by mouth. Common side effects include high blood pressure, headaches, and urinary tract infections. Other significant side effects include urinary retention, irregular heart rate, and angioedema. It works by activating the β3 adrenergic receptor in the bladder, resulting in its relaxation. Mirabegron is the first clinically available beta-3 agonist with approval for use in adults with overactive bladder. Mirabegron was approved for medical use in the United States and in the European Union in 2012. Text was copied from this source which is © European Medicines Agency. Reproduction is authorized provided the source is acknowledged. In 2020, it was the 160th most commonly prescribed medication in the United States, with more than 3million prescriptions. It is ava ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Skeletal Muscle
Skeletal muscles (commonly referred to as muscles) are organs of the vertebrate muscular system and typically are attached by tendons to bones of a skeleton. The muscle cells of skeletal muscles are much longer than in the other types of muscle tissue, and are often known as muscle fibers. The muscle tissue of a skeletal muscle is striated – having a striped appearance due to the arrangement of the sarcomeres. Skeletal muscles are voluntary muscles under the control of the somatic nervous system. The other types of muscle are cardiac muscle which is also striated and smooth muscle which is non-striated; both of these types of muscle tissue are classified as involuntary, or, under the control of the autonomic nervous system. A skeletal muscle contains multiple muscle fascicle, fascicles – bundles of muscle fibers. Each individual fiber, and each muscle is surrounded by a type of connective tissue layer of fascia. Muscle fibers are formed from the cell fusion, fusion of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Beta-2 Adrenergic Receptor
The beta-2 adrenergic receptor (β2 adrenoreceptor), also known as ADRB2, is a cell membrane-spanning beta-adrenergic receptor 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 ... that binds epinephrine (adrenaline), a hormone and neurotransmitter whose signaling, via adenylate cyclase stimulation through trimeric Gs proteins, increased Cyclic adenosine monophosphate, cAMP, and downstream L-type calcium channel interaction, mediates physiologic responses such as smooth muscle relaxation and bronchodilation. Robert J.Lefkowitz and Brian Kobilka studied beta 2 adrenergic receptor as a model system which rewarded them the 2012 Nobel Prize in Chemistry “for groundbreaking discoveries that reveal the inner workings of an important family of such receptors: G-protein-coupled-receptors†... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Beta-1 Adrenergic Receptor
The beta-1 adrenergic receptor (β1 adrenoceptor), also known as ADRB1, is a beta-adrenergic receptor, and also denotes the human gene encoding it. It is a G-protein coupled receptor associated with the Gs heterotrimeric G-protein and is expressed predominantly in cardiac tissue. Receptor Actions Actions of the β1 receptor include: The receptor is also present in the cerebral cortex. Agonists Isoprenaline has higher affinity for β1 than adrenaline, which, in turn, binds with higher affinity than noradrenaline at physiologic concentrations. Selective agonists to the beta-1 receptor are: *Denopamine *Dobutamine (in cardiogenic shock) *Xamoterol (cardiac stimulant) Antagonists ''(Beta blockers)'' β1-selective antagonists include: *Acebutolol (in hypertension, angina pectoris and arrhythmias) *Atenolol (in hypertension, coronary heart disease, arrhythmias and myocardial infarction) * Betaxolol (in hypertension and glaucoma) *Bisoprolol (in hypertension, coronary heart disea ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Intracellular
This glossary of biology terms is a list of definitions of fundamental terms and concepts used in biology, the study of life and of living organisms. It is intended as introductory material for novices; for more specific and technical definitions from sub-disciplines and related fields, see Glossary of genetics, Glossary of evolutionary biology, Glossary of ecology, and Glossary of scientific naming, or any of the organism-specific glossaries in :Glossaries of biology. A B C D E ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cyclic Adenosine Monophosphate
Cyclic adenosine monophosphate (cAMP, cyclic AMP, or 3',5'-cyclic adenosine monophosphate) is a second messenger important in many biological processes. cAMP is a derivative of adenosine triphosphate (ATP) and used for intracellular signal transduction in many different organisms, conveying the cAMP-dependent pathway. History Earl Sutherland of Vanderbilt University won a Nobel Prize in Physiology or Medicine in 1971 "for his discoveries concerning the mechanisms of the action of hormones", especially epinephrine, via second messengers (such as cyclic adenosine monophosphate, cyclic AMP). Synthesis Cyclic adenosine monophosphate, AMP is synthesized from Adenosine triphosphate, ATP by adenylate cyclase located on the inner side of the plasma membrane and anchored at various locations in the interior of the cell. Adenylate cyclase is ''activated'' by a range of signaling molecules through the activation of adenylate cyclase stimulatory G (Gs alpha subunit, Gs)-protein-coupled recep ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Adenylyl Cyclase
Adenylate cyclase (EC 4.6.1.1, also commonly known as adenyl cyclase and adenylyl cyclase, abbreviated AC) is an enzyme with systematic name ATP diphosphate-lyase (cyclizing; 3′,5′-cyclic-AMP-forming). It catalyzes the following reaction: :ATP = 3′,5′-cyclic AMP + diphosphate It has key regulatory roles in essentially all cells. It is the most polyphyletic known enzyme: six distinct classes have been described, all catalyzing the same reaction but representing unrelated gene families with no known sequence or structural homology. The best known class of adenylyl cyclases is class III or AC-III (Roman numerals are used for classes). AC-III occurs widely in eukaryotes and has important roles in many human tissues. All classes of adenylyl cyclase catalyse the conversion of adenosine triphosphate (ATP) to 3',5'-cyclic AMP (cAMP) and pyrophosphate.Magnesium ions are generally required and appear to be closely involved in the enzymatic mechanism. The cAMP produced by AC ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Enzyme
Enzymes () are proteins that act as biological catalysts by accelerating chemical reactions. The molecules upon which enzymes may act are called substrates, and the enzyme converts the substrates into different molecules known as products. Almost all metabolic processes in the cell need enzyme catalysis in order to occur at rates fast enough to sustain life. Metabolic pathways depend upon enzymes to catalyze individual steps. The study of enzymes is called ''enzymology'' and the field of pseudoenzyme analysis recognizes that during evolution, some enzymes have lost the ability to carry out biological catalysis, which is often reflected in their amino acid sequences and unusual 'pseudocatalytic' properties. Enzymes are known to catalyze more than 5,000 biochemical reaction types. Other biocatalysts are catalytic RNA molecules, called ribozymes. Enzymes' specificity comes from their unique three-dimensional structures. Like all catalysts, enzymes increase the reaction ra ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Gi Alpha Subunit
Gi protein alpha subunit is a family of heterotrimeric G protein alpha subunits. This family is also commonly called the Gi/o (Gi /Go ) family or Gi/o/z/t family to include closely related family members. G alpha subunits may be referred to as Gi alpha, Gαi, or Giα. Family members There are four distinct subtypes of alpha subunits in the Gi/o/z/t alpha subunit family that define four families of heterotrimeric G proteins: * Gi proteins: Gi1α, Gi2α, and Gi3α * Go protein: Goα (in mouse there is alternative splicing to generate Go1α and Go2α) * Gz protein: Gzα * Transducins (Gt proteins): Gt1α, Gt2α, Gt3α Giα proteins Gi1α Gi1α is encoded by the gene GNAI1. Gi2α Gi2α is encoded by the gene GNAI2. Gi3α Gi3α is encoded by the gene GNAI3. Goα protein Go1α is encoded by the gene GNAO1. Gzα protein Gzα is encoded by the gene GNAZ. Transducin proteins Gt1α Transducin/Gt1α is encoded by the gene GNAT1. Gt2α Transducin 2/Gt ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Gs Alpha Subunit
The Gs alpha subunit (Gαs, Gsα) is a subunit of the heterotrimeric G protein Gs that stimulates the cAMP-dependent pathway by activating adenylyl cyclase. Gsα is a GTPase that functions as a cellular signaling protein. Gsα is the founding member of one of the four families of heterotrimeric G proteins, defined by the alpha subunits they contain: the Gαs family, Gαi/Gαo family, Gαq family, and Gα12/Gα13 family. The Gs-family has only two members: the other member is Golf, named for its predominant expression in the olfactory system. In humans, Gsα is encoded by the GNAS complex locus, while Golfα is encoded by the GNAL gene. Function The general function of Gs is to activate intracellular signaling pathways in response to activation of cell surface G protein-coupled receptors (GPCRs). GPCRs function as part of a three-component system of receptor-transducer-effector. The transducer in this system is a heterotrimeric G protein, composed of three subunits: a Gα ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
G Protein-coupled Receptor
G protein-coupled receptors (GPCRs), also known as seven-(pass)-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptors, and G protein-linked receptors (GPLR), form a large group of evolutionarily-related proteins that are cell surface receptors that detect molecules outside the cell and activate cellular responses. Coupling with G proteins, they are called seven-transmembrane receptors because they pass through the cell membrane seven times. Text was copied from this source, which is available under Attribution 2.5 Generic (CC BY 2.5) license. Ligands can bind either to extracellular N-terminus and loops (e.g. glutamate receptors) or to the binding site within transmembrane helices (Rhodopsin-like family). They are all activated by agonists although a spontaneous auto-activation of an empty receptor can also be observed. G protein-coupled receptors are found only in eukaryotes, including yeast, choanoflagellates, and ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nebivolol
Nebivolol is a beta blocker used to treat high blood pressure and heart failure. As with other β-blockers, it is generally a less preferred treatment for high blood pressure. It may be used by itself or with other blood pressure medication. It is taken by mouth. Common side effects include dizziness, feeling tired, nausea, and headaches. Serious side effects may include heart failure and bronchospasm. Its use in pregnancy and breastfeeding is not recommended. It works by blocking β1-adrenergic receptors in the heart and dilating blood vessels. Nebivolol was patented in 1983 and came into medical use in 1997. It is available as a generic medication in the United Kingdom. In 2020, it was the 239th most commonly prescribed medication in the United States, with more than 1million prescriptions. Medical uses It is used to treat high blood pressure and heart failure. Nebivolol is used in the treatment of angina, to decrease the heart rate and contractile force. This is releva ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
