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14-September-2008 18:02:41 - adrenergic receptor The alpha-1 adrenergic receptor α1-AR is an adrenergic receptor with the primary effect of vasoconstriction. Contents 1 Effect 1.1 General 1.2 Specific 1.2.1 Smooth muscle 1.2.2 Other 2 Activity During Exercise 3 Mechanism 4 Agonists 5 Antagonists 6 Subtypes 7 See also 8 References Effect The α1 receptor has several, general, functions in common with other α-receptors, but also has specific effects. General Common or still unspecified effects include: Vasoconstriction of arteries to heart coronary arteries.1 Venoconstriction of veins2 Decrease motility of smooth muscle in gastrointestinal tract3 Specific The primary effect is on smooth muscle, which mainly constrict. However, there are other functions as well. Smooth muscle In smooth muscle of blood vessels the principal effect is vasoconstriction. Blood vessels with α1 receptors are present in the skin, the sphincters4 of gastrointestinal system, kidney renal artery5 and brain.6 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. It also induces contraction of the urinary bladder78, although this effect is minor compared to the relaxing effect of β-2 adrenergic receptors. In other words, the overall effect of sympathetic stimuli on the bladder is relaxation, in order to delay micturition during stress. Other effects are on smooth muscle are contraction in: ureter hairs arrector pili muscles uterus when pregnant urethral sphincter bronchioles although minor to the relaxing effect of β2 receptor on bronchioles iris dilator muscle4 seminal tract4, resulting in ejaculation In a few areas the result on smooth muscle is relaxation. These include: The rest of the GI tract than the sphincters.4 Blood vessels of erectile tissue.9 Other Positive ionotropic effect on heart muscle.7 α1β1.7 ↑Secretion from salivary gland.7 Increase salivary potassium levels. Glycogenolysis and gluconeogenesis from adipose tissue7 and liver. Secretion from sweat glands.7 Na+ reabsorption from kidney.7 Stimulate proximal tubule NHE310 Stimulate proximal tubule basolateral Na-K ATPase10 Activate mitogenic responses and regulate growth and proliferation of many cells. Activity During Exercise During exercise these alpha-1 receptors can be selectively blocked by sympathetic nervous activity, allowing the beta-2 receptors which mediate vasodilation to dominate. Note that only the alpha-1 receptors in exercising muscle will be blocked. Resting muscle will not have its alpha-1 receptors blocked, and hence the overall effect there will be alpha-1 mediated vasocontriction. Mechanism 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. Agonists Agonists include: noradrenaline adrenaline isoprenaline phenylephrine4 decongestant methoxamine4 cirazoline denotes selective agonists to the receptor. Noradrenaline has higher receptor affinity than has adrenaline, which, in turn has much higher affinity than isoprenaline.4 Antagonists Antagonists are various alpha blockers: mirtazapine NaSSA phenoxybenzamine in hypertension phentolamine in hypertensive emergencies prazosin4 in hypertension tamsulosin in BPH terazosin in BPH and hypertension doxazocin4 in BPH and hypertension denotes selective antagonists to the receptor. Subtypes There are 3 α1-AR subtypes: alpha-1A, -1B and -1D, all of which signal through the Gq/11 family of G-proteins and different subtypes show different patterns of activation. See also Other adrenergic receptors Alpha-2 adrenergic receptor Beta-1 adrenergic receptor Beta-2 adrenergic receptor Beta-3 adrenergic receptor References ^ 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 h i Rang, H. P. 2003. Pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4. Page 163 ^ 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 Fitzpatrick, David; Purves, Dale; Augustine, George 2004. Table 20:2, Neuroscience, Third ion, Sunderland, Mass: Sinauer. ISBN 0-87893-725-0. ^ Chou EC, Capello SA, Levin RM, Longhurst PA 2003. Excitatory α1-adrenergic receptors predominate over inhibitory β-receptors in rabbit dorsal detrusor. J. Urol. 170 6 Pt 1: 2503-7. doi:10.1097/01.ju.0000094184.97133.69. PMID 14634460. ^ Morton JS, Daly CJ, Jackson VM, McGrath JC 2007. Alpha1A-adrenoceptors mediate contractions to phenylephrine in rabbit penile arteries. Br. J. Pharmacol. 150 1: 112-20. doi:10.1038/sj.bjp.0706956. PMID 17115072. ^ a b Walter F., PhD. Boron. Medical Physiology: A Cellular And Molecular Approaoch. Elsevier/Saunders. ISBN 1-4160-2328-3. Page 787 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-1_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 This page was last modified on 24 August 2008, at 03:15
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