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Encyclopedia > Alpha adrenergic receptor

The adrenergic receptors (or adrenoceptors) are a class of G protein-coupled receptors that are targets of the catecholamines. Adrenergic receptors specifically bind their endogenous ligands, the catecholamines adrenaline and noradrenaline (called epinephrine and norepinephrine in the USA), and are activated by these. Image File history File links Adrenaline. ... Image File history File links Adrenaline. ... “Adrenaline” redirects here. ... Image File history File links No higher resolution available. ... Image File history File links No higher resolution available. ... Norepinephrine (INN)(abbr. ... A Mu-opioid G protein-coupled receptor with its agonist Figure 1. ... tyrosine is the precursor of catecholamines epinephrine norepinephrine dopamine Synthesis Catecholamines are chemical compounds derived from the amino acid tyrosine containing catechol and amine groups. ... In biochemistry, a receptor is a protein on the cell membrane or within the cytoplasm or cell nucleus that binds to a specific molecule (a ligand), such as a neurotransmitter, hormone, or other substance, and initiates the cellular response to the ligand. ... Look up Endogenous in Wiktionary, the free dictionary. ... In chemistry, a ligand is an atom, ion, or molecule (see also: functional group) that generally donates one or more of its electrons through a coordinate covalent bond to, or shares its electrons through a covalent bond with, one or more central atoms or ions (these ligands act as a... Epinephrine (INN) or adrenaline (BAN) is a hormone and a neurotransmitter. ... Norepinephrine, known as noradrenaline outside the USA, is a catecholamine and a phenethylamine with chemical formula C8H11NO3. ... “Adrenaline” redirects here. ... Norepinephrine (INN)(abbr. ...


Many cells possess these receptors, and the binding of an agonist will generally cause the cell to respond in a fight-or-flight manner. For instance, the heart rate will increase and the pupils will dilate, energy will be mobilized, and blood flow diverted from other organs to skeletal muscle.(Note: Sympathetic activity will result in vasoDILATION of coronary arteries via the Beta-2 adrenergic receptors.) Agonists An agonist is a substance that binds to a receptor and triggers a response in the cell. ... The fight-or-flight response, also called the acute stress response, was first described by Walter Cannon in 1929. ... Heart rate is a term used to describe the frequency of the cardiac cycle. ... The human eye The pupil is the central transparent area (showing as black). ... This article or section does not cite any references or sources. ...

Contents

Subtypes of adrenergic receptors

There are several types of adrenergic receptors, but there are two main groups: α-Adrenergic and β-Adrenergic.

  • α receptors bind norepinephrine and epinephrine, though norepinephrine has higher affinity. Phenylephrine is a selective agonist of the α receptor.
  • β receptors are linked to Gs proteins, which in turn are linked to adenylyl cyclase. Agonist binding thus causes a rise in the intracellular concentration of the second messenger cAMP. Downstream effectors of cAMP include cAMP-dependent protein kinase (PKA), which mediates some of the intracellular events following hormone binding.

Phenylephrine or neosynephrine is an α-adrenergic receptor agonist used primarily as a decongestant, as an agent to dilate the pupil and, rarely, to increase blood pressure. ... G-proteins, short for guanine nucleotide binding proteins, are a family of proteins involved in second messenger cascades. ... Adenylate cyclase (EC 4. ... Structure of cAMP Cyclic adenosine monophosphate (cAMP, cyclic AMP or 3-5-cyclic adenosine monophosphate) is a molecule that is important in many biological processes; it is derived from adenosine triphosphate (ATP). ... In cell biology, cAMP-dependent protein kinase (cAPK), also known as protein kinase A (PKA, EC 2. ...

Comparison

Receptor type Agonist potency order Location / Action Mechanism Agonists Antagonists
α1:
ADRA1A, ADRA1B, ADRA1D
noradrenaline≥ adrenaline >> isoprenaline Smooth muscle. In blood vessels the principal effect is vasoconstriction. Blood vessels with α1 receptors are present in the skin and the gastrointestinal system, and during the fight-or-flight response vasoconstriction results in the decreased blood flow to these organs. This accounts for an individual's skin appearing pale when frightened. In the GI tract, the effect is relaxation. Gq: phospholipase C (PLC) activated, IP3 and calcium up noradrenaline
phenylephrine
Cirazoline
(Alpha blockers)
phenoxybenzamine
phentolamine
prazosin
tamsulosin
terazosin
α2:
ADRA2A, ADRA2B, ADRA2C
adrenaline > noradrenaline >> isoprenaline Pre- and postsynaptic nerve terminals. Mediates synaptic transmission. Gi: adenylate cyclase inactivated, cAMP down clonidine
lofexidine
xylazine
Tizanidine
Guanfacine
(Alpha blockers)
yohimbine
rauwolscine
idazoxan
β1:
ADRB1
isoprenaline > noradrenaline > adrenaline Heart and cerebral cortex. In heart, agonists enhance myocardial contractility and increase heart rate. Also found on juxtaglomerular cells, activation results in renin release. Gs: adenylate cyclase activated, cAMP up noradrenaline
isoprenaline
dobutamine
(Beta blockers)
metoprolol
atenolol
β2:
ADRB2
isoprenaline > adrenaline > noradrenaline Lung, smooth muscle, cerebellum, skeletal muscle. In lung, agonists cause bronchiole dilation. Agonists can be useful in treating asthma. In smooth muscle, relaxes walls. Relaxes uterine muscle and promotes release of insulin. Gs: adenylate cyclase activated, cAMP up (Short/long)
salbutamol (albuterol in USA)
bitolterol mesylate
formoterol
isoproterenol
levalbuterol
metaproterenol
salmeterol
terbutaline
(Beta blockers)
butoxamine
propranolol
β3:
ADRB3
isoprenaline > noradrenaline = adrenaline Adipose tissue. Agonists enhance lipolysis. Gs: adenylate cyclase activated, cAMP up L-796568
CL 316,243
LY 368842
Ro 40-2148
(Beta blockers)
SR 59230A

The absence of "ADRA1C" is intentional. At one time, there was a subtype known as C, but was found to be one of the previously discovered subtypes. To avoid confusion, it was decided that there would never be a C subtype again and so if any new subtypes were discovered, naming would start with D. In cell physiology, a secondary messenger system (also known as a second messenger system) is a method of cellular signalling where the signalling molecule does not enter the cell, but rather utilizes a cascade of events that transduces the signal into a cellular change. ... An Adrenergic antagonist is a pharmaceutical substance that acts to inhibit the action of the adrenergic receptors. ... Isoprenaline is a synthetic derivative of noradrenaline that is not found in the body. ... Cultured Smooth muscle of the aorta. ... f you all The blood vessels are part of the circulatory system and function to transport blood throughout the body. ... The blood vessels are part of the circulatory system and function to transport blood throughout the body. ... Beyond overall skin structure, refer below to: See-also. ... For the Physics term GUT, please refer to Grand unification theory The gastrointestinal or digestive tract, also referred to as the GI tract or the alimentary canal or the gut, is the system of organs within multicellular animals which takes in food, digests it to extract energy and nutrients, and... The fight-or-flight response, also called the acute stress response, was first described by Walter Cannon in 1929. ... Upper and Lower gastrointestinal tract The gastrointestinal tract (GI tract), also called the digestive tract, or the alimentary canal, is the system of organs within multicellular animals that takes in food, digests it to extract energy and nutrients, and expels the remaining waste. ... This heterotrimeric G protein is illustrated with its theoretical lipid anchors. ... Phospholipase C is a key enzyme in phosphatidylinositol (PIP2) metabolism and lipid signaling pathways. ... Inositol triphosphate (also commonly known as inositol trisphosphate or triphosphoinositol; abbreviated InsP3 or IP3), together with diacylglycerol, is a second messenger molecule used in signal transduction in biological cells. ... General Name, Symbol, Number calcium, Ca, 20 Chemical series alkaline earth metals Group, Period, Block 2, 4, s Appearance silvery white Standard atomic weight 40. ... Norepinephrine, known as noradrenaline outside the USA, is a catecholamine and a phenethylamine with chemical formula C8H11NO3. ... Phenylephrine or neosynephrine is an α-adrenergic receptor agonist used primarily as a decongestant, as an agent to dilate the pupil and, rarely, to increase blood pressure. ... Alpha blockers (also called alpha-adrenergic blocking agents) constitute a variety of drugs which block alpha-adrenergic receptors in arteries and smooth muscles. ... Phenoxybenzamine is a non-specific, irreversible alpha blocker used in the treatment of hypertension, and specifically that caused by pheochromocytoma. ... Phentolamine is a competitive nonselective alpha adrenergic receptor antagonist. ... Prazosin, brand name Minipress®, is a medication used to treat high blood pressure (hypertension). ... Tamsulosin (rINN) (IPA: ) is an α1a-selective alpha blocker used in the symptomatic treatment of benign prostatic hyperplasia (BPH). ... Terazosin (Hytrin) is an alpha blocker used for treatment of symptoms of prostate enlargement (BPH). ... Illustration of the major elements in a prototypical synapse. ... Mediate is a song by INXS from their 1987 album, Kick. ... Synapses allow nerve cells to communicate with one another through axons and dendrites, converting electrical signals into chemical ones. ... This heterotrimeric G protein is illustrated with its theoretical lipid anchors. ... Epinephrine binds its receptor, that associates with an heterotrimeric G protein. ... Structure of cAMP cAMP represented in three ways, the left with sticks-representation, the middle with structure formula, and the right with space filled representation. ... Clonidine is a direct-acting adrenergic agonist prescribed historically as an anti-hypertensive agent. ... Lofexidine is an alpha2-adrenergic receptor agonist, can be used as a short acting (short half life) anti-hypertensive, but mostly used to help with relief from symptoms of heroin or opiate withdrawal in opiate dependency. ... Xylazine is a drug that is used for sedation, anesthesia, muscle relaxation, and analgesia. ... Tizanidine (Zanaflex, Sirdalud) is a centrally acting α-2 adrenergic agonist. ... Guanfacine is a centrally acting antihypertensive agent. ... Alpha blockers (also called alpha-adrenergic blocking agents) constitute a variety of drugs which block alpha-adrenergic receptors in arteries and smooth muscles. ... Yohimbine, also known under the outdated names quebrachin, aphrodin, corynine, yohimvetol and hydroergotocin, is the principal alkaloid of the bark of the West-African tree Pausinystalia yohimbe Pierre (formerly Corynanthe yohimbe), family Rubiaceae (Madder family). ... The heart and lungs, from an older edition of Grays Anatomy. ... Location of the cerebral cortex Slice of the cerebral cortex, ca. ... Renin, also known as angiotensinogenase, is a circulating enzyme (EC 3. ... This heterotrimeric G protein is illustrated with its theoretical lipid anchors. ... Epinephrine binds its receptor, that associates with an heterotrimeric G protein. ... Structure of cAMP cAMP represented in three ways, the left with sticks-representation, the middle with structure formula, and the right with space filled representation. ... Norepinephrine, known as noradrenaline outside the USA, is a catecholamine and a phenethylamine with chemical formula C8H11NO3. ... Isoprenaline is a synthetic derivative of noradrenaline that is not found in the body. ... Dobutamine is a beta-1 adrenergic agonist. ... Beta blockers or beta-adrenergic blocking agents are a class of drugs used to treat a variety of cardiovascular conditions and some other diseases. ... “Minax” redirects here. ... Atenolol is a drug belonging to the group of beta blockers, a class of drugs used primarily in cardiovascular diseases. ... Human respiratory system The lungs flank the heart and great vessels in the chest cavity. ... Cultured Smooth muscle of the aorta. ... The cerebellum (Latin: little brain) is a region of the brain that plays an important role in the integration of sensory perception and motor output. ... This article or section does not cite any references or sources. ... The bronchioles are the first airway branches that no longer contain cartilage. ... Cultured Smooth muscle of the aorta. ... This heterotrimeric G protein is illustrated with its theoretical lipid anchors. ... Epinephrine binds its receptor, that associates with an heterotrimeric G protein. ... Structure of cAMP cAMP represented in three ways, the left with sticks-representation, the middle with structure formula, and the right with space filled representation. ... Beta2-adrenergic receptor agonists are a class of drugs used to treat asthma. ... Salbutamol (INN) or albuterol (USAN) is a short-acting β2-adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma and COPD. Salbutamol sulphate is usually given by the inhaled route for direct effect on bronchial smooth muscle. ... Salbutamol (INN) or albuterol (USAN) is a short-acting β2-adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma and COPD. It is marketed by the Allen & Hanburys respiratory division of GlaxoSmithKline under the trade name Ventolin. ... Bitolterol mesylate (Tornalate®) is a β2-adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma and COPD. Bitolterol has a rapid onset of action (2-5 minutes) and may last up to 6-8 hours. ... Formoterol belongs to the family of prescription-only medicines known as beta 2-agonists. ... Isoproterenol hydrochloride (Medihaler-Iso®) is a beta adrenergic receptor agonist medication, used as an inhaled aerosol to treat asthma. ... Levalbuterol (Xopenex®) is the R-enantiomer of the short-acting β2-adrenergic receptor agonist albuterol. ... Metaproterenol is used as a bronchodialator in the treatment of asthma. ... Salmeterol is a long-acting beta2-adrenergic receptor agonist drug that is currently prescribed for the treatment of asthma and chronic obstructive pulmonary disease COPD. It is currently available in both dry-powder inhalers (DPIs) and pressurised metered dose inhalers (pMDIs). ... The drug Terbutaline (trade names Brethine, Bricanyl, or Brethaire) is a β2-adrenergic receptor agonist, used as a fast-acting bronchodilator and off-label to delay premature labour as a tocolytic. ... Beta blockers or beta-adrenergic blocking agents are a class of drugs used to treat a variety of cardiovascular conditions and some other diseases. ... This page meets Wikipedias criteria for speedy deletion. ... Propranolol (INN) (IPA: ) is a non-selective beta blocker mainly used in the treatment of hypertension. ... It has been suggested that Subcutaneous fat be merged into this article or section. ... Lipolysis is the breakdown of fat stored in fat cells. ... This heterotrimeric G protein is illustrated with its theoretical lipid anchors. ... Epinephrine binds its receptor, that associates with an heterotrimeric G protein. ... Structure of cAMP cAMP represented in three ways, the left with sticks-representation, the middle with structure formula, and the right with space filled representation. ... Beta blockers or beta-adrenergic blocking agents are a class of drugs used to treat a variety of cardiovascular conditions and some other diseases. ...


Diagrams

Labels in German, but most ideas can be understood. "Glatter" = "smooth", "hemmung" = "inhibition", "herzmuskels" = "heart muscle".
Labels in German, but most ideas can be understood. "Glatter" = "smooth", "hemmung" = "inhibition", "herzmuskels" = "heart muscle".
Epinephrin binds its receptor, that associates with an heterotrimeric G protein. The G protein associates with adenylate cyclase that converts ATP to cAMP, spreading the signal (more details...)
Epinephrin binds its receptor, that associates with an heterotrimeric G protein. The G protein associates with adenylate cyclase that converts ATP to cAMP, spreading the signal (more details...)


Image File history File links No higher resolution available. ... Image File history File links No higher resolution available. ... Image File history File links Download high-resolution version (837x481, 71 KB) File links The following pages on the English Wikipedia link to this file (pages on other projects are not listed): Adenylate cyclase Cyclic adenosine monophosphate Epinephrine Adrenergic receptor ... Image File history File links Download high-resolution version (837x481, 71 KB) File links The following pages on the English Wikipedia link to this file (pages on other projects are not listed): Adenylate cyclase Cyclic adenosine monophosphate Epinephrine Adrenergic receptor ...


See also

// Upon stimulation of the B-adrenergic receptor by epinephrine, Gs will be activated. ...

References

  • Rang HP, Dale MM, Ritter JM, Moore PK (2003). "Ch. 11", Pharmacology. Elsevier Churchill Livingstone. ISBN 0-443-07145-4. 
  • Rang HP, Dale MM, Ritter JM, Flower RJ (2007). "Ch. 11", Rang and Dale's Pharmacology. Elsevier Churchill Livingstone, 169-170. ISBN 0-443-06911-5. 

External links


  Results from FactBites:
 
Patents in Class 514/929 (0 words)
The present invention is directed to nitrosated or nitrosylated.alpha.-adrenergic receptor antagonists, compositions comprising.alpha.-adrenergic receptor antagonists that are optionally substituted with at least one NO or NO.sub.2 moi...
There are provided a method to screen agonist or antagonist of the maxadilan receptor participating in vasodilating action, wherein a receptor of maxadilan is used, compounds which specifically bind to the receptor, and a tissue preparat...
The present invention describes novel compositions and kits comprising alpha-adrenergic receptor antagonists and compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, o...
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