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14-September-2008 18:02:41 - Adrenergic receptor Adrenaline Adrenaline Noradrenaline Noradrenaline 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 United States, and are activated by these. Many cells possess these receptors, and the binding of an agonist will generally cause a sympathetic response ie the fight-or-flight response. For instance, the heart rate will increase and the pupils will dilate, energy will be mobilized, and blood flow diverted from other non-essential organs to skeletal muscle. Contents 1 Subtypes 1.1 Roles in circulation 1.2 Comparison 1.3 α receptors 1.3.1 α1 receptor 1.3.2 α2 receptor 1.4 β receptors 1.4.1 β1 receptor 1.4.2 β2 receptor 1.4.3 β3 receptor 2 See also 3 References 4 Further reading 5 External links Subtypes There are two main groups of adrenergic receptors, α and β, with several subtypes. α receptors have the subtypes α1 a Gq coupled receptor and α2 a Gi coupled receptor. Phenylephrine is a selective agonist of the α receptor. β receptors have the subtypes β1, β2 and β3. All three 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. Isoprenaline is a selective agonist. Epinephrine 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... Epinephrine 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... The mechanism of adrenergic receptors. Adrenaline or noradrenaline are receptor ligands to either α1, α2 or β-adrenergic receptors. α1 couples to Gq, which results in increased intracellular Ca2+ which results in e.g. smooth muscle contraction. α2, on the other hand, couples to Gi, which causes a decrease of cAMP activity, resulting in e.g. smooth muscle contraction. β receptors couple to Gs, and increases intracellular cAMP activity, resulting in e.g. heart muscle contraction, smooth muscle relaxation and glycogenolysis. The mechanism of adrenergic receptors. Adrenaline or noradrenaline are receptor ligands to either α1, α2 or β-adrenergic receptors. α1 couples to Gq, which results in increased intracellular Ca2+ which results in e.g. smooth muscle contraction. α2, on the other hand, couples to Gi, which causes a decrease of cAMP activity, resulting in e.g. smooth muscle contraction. β receptors couple to Gs, and increases intracellular cAMP activity, resulting in e.g. heart muscle contraction, smooth muscle relaxation and glycogenolysis. Roles in circulation Epinephrine reacts with both α- and β-adrenoreceptors, causing vasoconstriction and vasodilation, respectively. Although α receptors are less sensitive to epinephrine, when activated, they override the vasodilation mediated by β-adrenoreceptors. The result is that high levels of circulating epinephrine cause vasoconstriction. At lower levels of circulating epinephrine, β-adrenoreceptor stimulation dominates, producing an overall vasodilation. Comparison Receptor type Agonist potency order Selected action of agonist Mechanism Agonists Antagonists α1: A, B, D†adrenaline ≥ noradrenaline isoprenaline smooth muscle contraction Gq: phospholipase C PLC activated, IP3 and calcium up Alpha-1 agonists Noradrenaline Phenylephrine Methoxamine Cirazoline Xylometazoline Alpha-1 blockers Doxazosin Phenoxybenzamine Phentolamine Prazosin Tamsulosin Terazosin α2: A, B, C adrenaline ≥ noradrenaline isoprenaline smooth muscle contraction and neurotransmitter inhibition Gi: adenylate cyclase inactivated, cAMP down Alpha-2 agonists Dexmedetomidine Clonidine Lofexidine Xylazine Tizanidine Guanfacine Alpha-2 blockers Yohimbine Idazoxan β1 isoprenaline adrenaline = noradrenaline heart muscle contraction Gs: adenylate cyclase activated, cAMP up Noradrenaline Isoprenaline Dobutamine Beta blockers Metoprolol Atenolol β2 isoprenaline adrenaline noradrenaline smooth muscle relaxation Gs: adenylate cyclase activated, cAMP up Short/long Salbutamol Albuterol in USA Bitolterol mesylate Formoterol Isoprenaline Levalbuterol Metaproterenol Salmeterol Terbutaline Ritodrine Beta blockers Butoxamine Propranolol β3 isoprenaline = noradrenaline adrenaline Enhance lipolysis Gs: adenylate cyclase activated, cAMP up L-796568 1 Amibegron Solabegron †There is no α1C receptor. At one time, there was a subtype known as C, but was found to be identical to one of the previously discovered subtypes. To avoid confusion, naming was continued with the letter D. α receptors α receptors have several functions in common, but also individual effects. Common or still unspecified effects include: Vasoconstriction of arteries to heart coronary artery.2 Vasoconstriction of veins3 Decrease motility of smooth muscle in gastrointestinal tract4 α1 receptor Main article: Alpha-1 adrenergic receptor Alpha1-adrenergic receptors are members of the G protein-coupled receptor superfamily. Upon activation, a heterotrimeric G protein, Gq, activates phospholipase C PLC, which causes an increase in IP3 and calcium. This triggers all other effects. Specific actions of the α1 receptor mainly involves smooth muscle contraction. It causes vasoconstriction in many blood vessels including those of the skin gastrointestinal system and to kidney renal artery5 and brain.6. Other areas of smooth muscle contraction are for instance: ureter vas deferens hairs erector pili muscles uterus when pregnant urethral sphincter bronchioles although minor to the relaxing effect of β2 receptor on bronchioles Further effects include glycogenolysis and gluconeogenesis from adipose tissue7 and liver, as well as secretion from sweat glands7 and Na+ reabsorption from kidney.7 Antagonists may be used in hypertension. α2 receptor Main article: Alpha-2 adrenergic receptor There are 3 highly homologous subtypes of α2 receptors: α2A, α2Î’, and α2C. Specific actions of the α2 receptor include: inhibition of insulin release in pancreas.7 induction of glucagon release from pancreas. contraction of sphincters of the gastrointestinal tract β receptors β1 receptor Main article: Beta-1 adrenergic receptor Specific actions of the β1 receptor include: Increase cardiac output, both by raising heart rate and increasing the volume expelled with each beat increased ejection fraction. Renin release from juxtaglomerular cells.7 Lipolysis in adipose tissue.7 β2 receptor Main article: Beta-2 adrenergic receptor The 3D crystallographic structure of the β2-adrenergic receptor has been determined PDB 2R4R, 2R4S, 2RH1.8910 Specific actions of the β2 receptor include: Smooth muscle relaxation, e.g. in bronchi.7 Lipolysis in adipose tissue.11 Anabolism in skeletal muscle.1213 Relax non-pregnant uterus. Relax detrusor urinae muscle‎ of bladder wall Dilate arteries to skeletal muscle Glycogenolysis and gluconeogenesis Contract sphincters of GI tract Thickened secretions from salivary glands.7 Inhibit histamine-release from mast cells Increase renin secretion from kidney β3 receptor Main article: Beta-3 adrenergic receptor Specific actions of the β3 receptor include: Enhancement of lipolysis in adipose tissue. CNS effects Clarify See also Beta adrenergic receptor kinase Beta adrenergic receptor kinase-2 References ^ Nisoli E, Tonello C, Landi M, Carruba MO 1996. Functional studies of the first selective β3-adrenergic receptor antagonist SR 59230A in rat brown adipocytes. Mol. Pharmacol. 49 1: 7-14. PMID 8569714. ^ Woodman OL, Vatner SF 1987. Coronary vasoconstriction mediated by α1- and α2-adrenoceptors in conscious dogs. Am. J. Physiol. 253 2 Pt 2: H388-93. PMID 2887122. ^ Elliott J 1997. Alpha-adrenoceptors in equine digital veins: evidence for the presence of both α1- and α2-receptors mediating vasoconstriction. J. Vet. Pharmacol. Ther. 20 4: 308-17. doi:10.1046/j.1365-2885.1997.00078.x. PMID 9280371. ^ Sagrada A, Fargeas MJ, Bueno L 1987. Involvement of α1 and α2 adrenoceptors in the postlaparotomy intestinal motor disturbances in the rat. Gut 28 8: 955-9. PMID 2889649. ^ Schmitz JM, Graham RM, Sagalowsky A, Pettinger WA 1981. Renal α1 and α2 adrenergic receptors: biochemical and pharmacological correlations. J. Pharmacol. Exp. Ther. 219 2: 400-6. PMID 6270306. ^ Circulation Lung Physiology I M.A.S.T.E.R. Learning Program, UC Davis School of Medicine ^ a b c d e f g h Fitzpatrick, David; Purves, Dale; Augustine, George 2004. Table 20:2, Neuroscience, Third ion, Sunderland, Mass: Sinauer. ISBN 0-87893-725-0. ^ Rasmussen SG, Choi HJ, Rosenbaum DM, Kobilka TS, Thian FS, Edwards PC, Burghammer M, Ratnala VR, Sanishvili R, Fischetti RF, Schertler GF, Weis WI, Kobilka BK 2007. Crystal structure of the human β2-adrenergic G-protein-coupled receptor. Nature 450 7168: 383-7. doi:10.1038/nature06325. PMID 17952055. ^ Cherezov V, Rosenbaum DM, Hanson MA, Rasmussen SG, Thian FS, Kobilka TS, Choi HJ, Kuhn P, Weis WI, Kobilka BK, Stevens RC 2007. High-resolution crystal structure of an engineered human β2-adrenergic G protein-coupled receptor. Science 318 5854: 1258-65. doi:10.1126/science.1150577. PMID 17962520. ^ Rosenbaum DM, Cherezov V, Hanson MA, Rasmussen SG, Thian FS, Kobilka TS, Choi HJ, Yao XJ, Weis WI, Stevens RC, Kobilka BK 2007. GPCR engineering yields high-resolution structural insights into β2-adrenergic receptor function. Science 318 5854: 1266-73. doi:10.1126/science.1150609. PMID 17962519. ^ Large V, Hellström L, Reynisdottir S, et al December 1997. Human beta-2 adrenoceptor gene polymorphisms are highly frequent in obesity and associate with altered adipocyte beta-2 adrenoceptor function. J. Clin. Invest. 100 12: 3005-13. doi:10.1172/JCI119854. PMID 9399946. ^ Kline WO, Panaro FJ, Yang H, Bodine SC February 2007. Rapamycin inhibits the growth and muscle-sparing effects of clenbuterol. J. Appl. Physiol. 102 2: 740-7. doi:10.1152/japplphysiol.00873.2006. PMID 17068216. ^ Kamalakkannan G, Petrilli CM, George I, et al April 2008. Clenbuterol increases lean muscle mass but not endurance in patients with chronic heart failure. J. Heart Lung Transplant. 27 4: 457-61. doi:10.1016/j.healun.2008.01.013. PMID 18374884. Further reading 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 The Adrenergic Receptors IUPHAR GPCR Database - Adrenoceptors Basic Neurochemistry: α- and β-Adrenergic Receptors Brief overview of functions of the beta-3 receptor Theory of receptor activation Desensitization of beta-1-receptors UMich Orientation of Proteins in Membranes protein/pdbid-2rh1 - 3D structure of beta-2 adrenergic receptor in membrane This transmembrane receptor-related article is a stub. v d e Adrenergic agonists models/most important in CAPS α α1 METHOXAMINE · Methylnorepinephrine · Oxymetazoline · PHENYLEPHRINE · Metaraminol · Tamsulosin α2 4-NEMD · CLONIDINE · Guanfacine · Guanabenz · Guanoxabenz · Guanethidine · Xylazine · METHYLDOPA · Apraclonidine · Brimonidine · Detomidine · Dexmedetomidine · Lofexidine · Romifidine · Tizanidine · Xylometazoline Undetermined/ unsorted Amidephrine · Amitraz · Anisodamine · Ergotamine · Indanidine · Medetomidine · Mephentermine · Midodrine · Mivazerol · Naphazoline · Norfenefrine · Octopamine · Phenylpropanolamine · Rilmenidine · Synephrine · Talipexole · Tetrahydrozoline · Xylometazoline β β1 DOBUTAMINE · Dopamine · Denopamine · Xamoterol β2 Short acting β2-agonists: SALBUTAMOL albuterol/Levosalbutamol · Fenoterol · TERBUTALINE · Pirbuterol · Procaterol · Bitolterol · Rimiterol · Carbuterol · Tulobuterol · Reproterol · Dopexamine Long acting β2-agonists LABA: Arformoterol · Bambuterol · Clenbuterol · Formoterol · Salmeterol Orciprenaline metaproterenol · Ritodrine · Hexoprenaline · Indacaterol β3 Amibegron · Solabegron Undetermined/ unsorted Arbutamine · Befunolol · Isoxsuprine · Nylidrin · Oxyfedrine · Prenalterol · Ractopamine · Bromoacetylalprenololmenthane · Broxaterol · Cimaterol · Higenamine · Mabuterol · Methoxyphenamine · Tretoquinol · Zinterol Nonselective β ISOPRENALINE/ISOPROTERENOL α and β Epinephrine α1+2, β1+2 · Norepinephrine α1+2, β1 · Cirazoline · Etilefrine Indirect/ mixed Indirect presynaptic norepinephrine release: Amphetamine · Tyramine Mixed: Ephedrine · Pseudoephedrine Cocaine see also monoamine oxidase inhibitor v d e Transmembrane receptor: G protein-coupled receptors Class A: Rhodopsin like Adrenergic α1 A, B, D, α2 A, B, C, β1, β2, β3 Eicosanoid CysLT 1, 2, LTB4 1, 2, FPRL1, OXE, Prostaglandin DP, EP 1, 2, 3, 4, PGF, Prostacyclin, Thromboxane Neuropeptide B/W 1, 2, FF 1, 2, S, Y 1, 2, 4, 5 Orphan GPR 1, 3, 4, 6, 12, 15, 17, 18, 19, 20, 21, 22, 23, 25, 26, 27, 31, 32, 33, 34, 35, 37, 39, 42, 44, 45, 50, 52, 55, 61, 62, 63, 65, 68, 75, 77, 78, 79, 82, 83, 84, 85, 87, 88, 92, 101, 103, 119, 120, 132, 135, 139, 141, 142, 146, 148, 149, 150, 151, 152, 153, 160, 161, 162, 171, 172, 173, 174, 176, 177, 182 Purinergics Adenosine A1, A2a, A2b, A3, P2Y, 1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14 Serotonin all but 5-HT3 5-HT1 A, B, D, E, F, 5-HT2 A, B, C, 5-HT 4, 5A, 6, 7 Other Acetylcholine M1, M2, M3, M4, M5 - Adrenomedullin - Anaphylatoxin C3a, C5a - Angiotensin 1, 2 - Apelin - Bile acid - Bombesin BRS3, GRPR, NMBR - Bradykinin B1, B2 - Cannabinoid CB1, CB2 - Chemokine - Cholecystokinin A, B - Dopamine D1, D2, D3, D4, D5 - EBI2 - Endothelin A, B - Estrogen - Formyl peptide 1, L1, L2 - Free fatty acid 1, 2, 3, 4 - FSH - Galanin 1, 2, 3 - Gonadotropin-releasing hormone 1, 2 - Ghrelin - Histamine H1, H2, H3, H4 - Kisspeptin - Luteinizing hormone/choriogonadotropin - Lysophospholipid 1, 2, 3, 4, 5, 6, 7, 8 - MAS 1, 1L, D, E, F, G, X1, X2, X3, X4 - Melanocortin 1, 2, 3, 4, 5 - MCHR 1, 2 - Melatonin 1A, 1B- Motilin - neuromedin B, U 1, 2 - Neurotensin 1, 2 - Opioid Delta, Kappa, Mu, Nociceptin, but not Sigma - Olfactory - Opsin 3, 4, 5, 1LW, 1MW, 1SW, RGR, RRH - Orexin 1, 2 - Oxytocin - Oxoglutarate - PAF - Prokineticin 1, 2 - Prolactin-releasing peptide - Protease-activated 1, 2, 3, 4 - Relaxin 1, 2, 3, 4 - Somatostatin 1, 2, 3, 4, 5 - SREB - Succinate - TAAR 1, 2, 3, 5, 6, 8, 9 - Tachykinin 1, 2, 3 - Thyrotropin - Thyrotropin-releasing hormone - Urotensin-II - Vasopressin 1A, 1B, 2 Class B: Secretin like Brain-specific angiogenesis inhibitor 1, 2, 3 - Cadherin 1, 2, 3 - Calcitonin - CD97 - Corticotropin-releasing hormone 1, 2 - EMR 1, 2, 3 - Glucagon GR, GIPR, GLP1R, GLP2R - Growth hormone releasing hormone - PACAPR1- GPR 56, 64, 97, 98, 110, 111, 112, 113, 114, 115, 116, 123, 124, 125, 126, 128, 133, 143, 144, 157 - Latrophilin 1, 2, 3, ELTD1 - Parathyroid hormone 1, 2 - Secretin - Vasoactive intestinal peptide 1, 2 Class C: Metabotropic glutamate / pheromone Calcium-sensing receptor - GABA B 1, 2 - Glutamate receptor Metabotropic glutamate 1, 2, 3, 4, 5, 6, 7, 8 - GPRC6A - GPR 156, 158, 179 - RAIG 1, 2, 3, 4 - Taste receptors TAS1R 1, 2, 3 TAS2R 1, 3, 4, 5, 8, 9, 10, 12, 13, 14, 16, 38, 39, 40, 41, 43, 44, 45, 46, 47, 48, 49, 50 Frizzled / Smoothened Frizzled 1, 2, 3, 4, 5, 6, 7, 8, 9, 10 - Smoothened Retrieved from http://en..org/wiki/Adrenergic_receptor Categories: Transmembrane receptor stubs | Adrenergic receptors | G protein coupled receptors Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page Languages Deutsch Español Français Italiano 日本語 Polski Português РуÑ?Ñ?кий Suomi This page was last modified on 11 September 2008, at 21:4
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