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14-September-2008 18:02:41 - adrenergic receptor The α2 receptor is a type of adrenergic receptor. Contents 1 Effect 1.1 General 1.2 Individual 2 Mechanism 3 Agonists 4 Antagonists 5 Types 6 See also 7 References Effect The α2 receptor has several, general, functions in common with other α-receptors, but also has individual effects. General Common or still unspecified effects include: Vasodilation of arteries α2A; ADRA2A1 Vasoconstriction of arteries α2B; ADRA2B to heart coronary artery.2 Vasoconstriction of veins3 Decrease motility of smooth muscle in gastrointestinal tract4 Contraction of male genitalia during ejaculation Individual Individual actions of the α2 receptor include: Mediates synaptic transmission in pre- and postsynaptic nerve terminals. Decrease release of acetylcholine5 Decrease release of noradrenaline5 Inhibit noradrenaline system in brain Inhibition6 of lipolysis in adipose tissue.7 inhibition of insulin release in pancreas.7 induction of glucagon release from pancreas. platelet aggregation contraction of sphincters of the gastrointestinal tract ↓ Secretion from salivary gland8 relax gastrointestinal tractpresynaptic effect Mechanism A G protein - Gi renders adenylate cyclase inactivated, resulting in decrease of cAMP. The relaxation of gastrointestinal tract motility is by presynaptic inhibition5, where transmitters inhibit further release by homotropic effects. Agonists Adrenaline has higher affinity for the alpha-2 receptor than has noradrenaline, which, in turn, has much higher affinity than has isoprenaline.5 Other agonists include: clonidine5 antihypertensive -- see below for alternative mechanism -- dexmedetomidine lofexidine antihypertensive xylazine veterinary; in non-human species this is an immobilizing and anesthetic drug, presumptively also mediated by alpha-2 adrenergic receptors because it is reversed by yohimbine tizanidine in spasms, cramping guanfacine antihypertensive denotes selective agonists to the receptor. Clonidine is an Alpha 2 Agonist ; initially thought act via presynaptic Alpha 2 receptors -- reduced NE discharge. However! It binds to imidazoline receptors with a much greater affinity than Alpha 2s . Imidazoline Receptors occur in the Nucleus Tractus Solitarius Ventrolateral Medulla. Clonidine is now thought to decrease BP via this central mechanism. Antagonists Alpha blockers yohimbine5 purported aphrodisiac mirtazapine NaSSA mianserin tetracyclic antidepressant idazoxan5experimental9 denotes selective agonists to the receptor. Types There are three types of α2 receptors: ADRA2A, ADRA2B, ADRA2C. See also Other adrenergic receptors Alpha-1 adrenergic receptor Beta-1 adrenergic receptor Beta-2 adrenergic receptor Beta-3 adrenergic receptor References ^ Goodman Gilman, Alfred. Goodman Gilman's The Pharmacological Basis of Therapeutics. Tenth ion. McGraw-Hill 2001: Page 140. ^ 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. doi:10.1136/gut.28.8.955. PMID 2889649. ^ a b c d e f g Rang, H. P. 2003. Pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4. Page 163 ^ Wright EE, Simpson ER 1981. Inhibition of the lipolytic action of beta-adrenergic agonists in human adipocytes by alpha-adrenergic agonists. J. Lipid Res. 22 8: 1265-70. PMID 6119348. ^ a b Fitzpatrick, David; Purves, Dale; Augustine, George 2004. Table 20:2, Neuroscience, Third ion, Sunderland, Mass: Sinauer. ISBN 0-87893-725-0. ^ Khan ZP, Ferguson CN, Jones RM 1999. alpha-2 and imidazoline receptor agonists. Their pharmacology and therapeutic role. Anaesthesia 54 2: 146-65. doi:10.1046/j.1365-2044.1999.00659.x. PMID 10215710. ^ online-medical-dictionary.org This transmembrane receptor-related article is a stub. 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/Alpha-2_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 Español This page was last modified on 29 August 2008, at 22:01
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