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14-September-2008 18:02:42 - receptor Dopamine Dopamine Dopamine receptors are a class of metabotropic G protein-coupled receptors that are prominent in the vertebrate central nervous system CNS. The neurotransmitter dopamine is the primary endogenous ligand for dopamine receptors. Dopamine receptors have key roles in many processes, including the control of motivation, learning, and fine motor movement, as well as modulation of neuroendocrine signaling. Abnormal dopamine receptor signaling and dopaminergic nerve function is implicated in several neuropsychiatric disorders.1 Thus, dopamine receptors are common neurologic drug targets; antipsychotics are often dopamine receptor antagonists while psychostimulants are typically indirect agonists of dopamine receptors. Contents 1 Dopamine receptor subtypes 1.1 D1-like family excitatory 1.2 D2-like family inhibitory 2 Role of dopamine receptors in the central nervous system 3 Non-CNS dopamine receptors 3.1 Cardio-pulmonary system 3.2 Renal system 4 Dopamine receptors in disease 4.1 Attention-deficit hyperactivity disorder 4.2 Recreational drug use and abuse 4.3 Schizophrenia 4.4 Genetic hypertension 5 See also 6 External links 7 References Dopamine receptor subtypes Dopamine receptor agonists + and antagonists -. Specificity is not always perfect. This table is not complete. D1-like D2-like citation needed D1 D5 D2 D3 D4 Apomorphine + + + + + Fenoldopam + + + ? + SKF 38393 + + + SKF 82958 + + Dihydrexidine + + Quinpirole + + Haloperidol - ? - - ? Flupentixol - ? - ? ? Fluphenazine - ? ? ? ? SCH 23390 - - Spiperone ? - ? ? Raclopride - - - Clozapine - - - - - There are five subtypes of dopamine receptors, D1, D2, D3, D4, and D5. The D1 and D5 receptors are members of the D1-like family of dopamine receptors, whereas the D2, D3 and D4 receptors are members of the D2-like family. There is also some evidence that suggests the existence of possible D6 and D7 dopamine receptors, but such receptors have not been conclusively identified.2 At a global level, D1 receptors have widespread expression throughout the brain. Furthermore, D1-2 receptor subtypes are found at 10-100 times the levels of the D2-5 subtypes.3 D1-like family excitatory Activation of D1-like family receptors is coupled to the G protein Gαs, which subsequently activates adenylyl cyclase, increasing the intracellular concentration of the second messenger cyclic adenosine monophosphate cAMP. Increased cAMP in neurons is typically excitatory and can induce an action potential by modulating the activity of ion channels. D1 DRD1 D5 DRD5 D2-like family inhibitory D2-like activation is coupled to the G protein Gαi, which directly inhibits the formation of cAMP by inhibiting the enzyme adenylate cyclase.4 D2 DRD2. There is a short version of D2 D2Sh and a long version of D2 D2Lh: The D2Sh are pre-synaptic situated, having modulatory functions called autoreceptor, they regulate the neurotransmission by feed-back mechanisms, i.e., synthesis, storage and release of dopamine into the synaptic cleft. The D2Lh may have the classic function of a post-synaptic receptor, i.e., keep going on the neurotransmission excitatory or inhibitory once blocked by a receptor antagonist or stimulated by the endogenous neurotransmitter itself or a synthetic full or partial agonist. D3 DRD3 Maximum expression of dopamine D3 receptors is noted in the islands of Calleja and nucleus accumbens.5 D4 DRD4. The D4 receptor has the following variants D4.2, D4.3a, D4.3b, D4.4a, D4.4b, D4.4c, D4.4d, D4.4e, D4.5a, D4.5b, D4.6a, D4.6b, D4.7a, D4.7b, D4.7c, D4.7d, D4.8, D4.10. These variants differ in a variable number tandem repeat domain present within the coding sequence of exon 3. Some of these alleles are associated with greater incidence of certain diseases. For example, the D4.7 alleles have an established association with attention-deficit hyperactivity disorder. Role of dopamine receptors in the central nervous system Dopamine receptors control neural signaling that modulates many important behaviors, such as spatial working memory.6. Although dopamine receptors are widely distributed in the brain, different areas have different receptor types densities, presumably reflecting different functional roles. Non-CNS dopamine receptors Cardio-pulmonary system In humans, the pulmonary artery expresses D1, D2, D4, and D5 and receptor subtypes, which may account for vasorelaxive effects of dopamine in the blood.7 In rats, D1-like receptors are present on the smooth muscle of the blood vessels in most major organs.8 D4 receptors have been identified in the atria of rat and human hearts.9 Dopamine increases myocardial contractility and cardiac output, without changing heart rate, by signaling through dopamine receptors.2 Renal system Dopamine receptors are present along the nephron in the kidney, with proximal tubule epithelial cells showing the highest density.8 In rats, D1-like receptors are present on the juxtaglomerular apparatus and on renal tubules, while D2-like receptors are present on the renal tubules, glomeruli, postganglionic sympathetic nerve terminals, and zona glomerulosa cells of the renal cortex.8 Dopamine signaling affects diuresis and natriuresis.2 Dopamine receptors in disease Dysfunction of dopaminergic neurotransmission in the CNS has been implicated in a variety of neuropsychiatric disorders, including Social Phobia,10 Tourette's syndrome,11 Parkinson's disease,12 schizophrenia,11 neuroleptic malignant syndrome13 Attention-deficit hyperactivity disorder ADHD,14 and drug and alcohol dependence.1115 Attention-deficit hyperactivity disorder Dopamine receptors have been recognized as important components in the etiology of ADHD for many years. Drugs used to treat ADHD, including methylphenidate and amphetamine, have significant effects on dopamine signaling in the brain. Studies of gene association have implicated several genes within dopamine signaling pathways; in particular, the D4.7 variant of D4 has been consistently shown to be more frequent in ADHD patients.16 ADHD patients with the 4.7 allele also tend to have better cognitive performance and long-term outcomes compared to ADHD patients without the 4.7 allele, suggesting that the allele is associated with a more benign form of ADHD.16 The D4.7 allele has suppressed gene expression compared to other variants.17 Recreational drug use and abuse Dopamine is the primary neurotransmitter involved in the reward pathways in the brain. Thus, drugs that increase dopamine signaling may produce euphoric effects. Many recreational drugs, such as cocaine and amphetamines, alter the functionality of the dopamine transporter DAT, the protein responsible for removing dopamine from the neural synapse. When DAT activity is blocked, the synapse floods with dopamine and increases dopaminergic signaling. When this occurs, particularly in the nucleus accumbens,18 increased D115 and D218 receptor signaling mediates the rewarding stimulus of drug intake.18 Reward pathway signaling can affect other regions of the brain as well, inducing long-term changes in regions such as the nucleus accumbens and frontal cortex; these changes can strengthen drug craving and alter cognitive pathways, with drug abuse potentially creating drug addiction and drug dependence. Schizophrenia Main article: Dopamine hypothesis of schizophrenia While there is evidence that the dopamine system is involved in schizophrenia, the theory that hyperactive dopaminergic signal transduction induces the disease is controversial. Psychostimulants, such as amphetamine and cocaine, induce dramatic changes in dopamine signaling; large doses and prolonged usage can induce symptoms that resemble schizophrenia. Additionally, many antipsychotic drugs target dopamine receptors, especially D2 receptors. Genetic hypertension Dopamine receptor mutations can cause genetic hypertension in humans.19 This can occur in animal models and humans with defective dopamine receptor activity, particularly D1.8 See also Category:Dopamine agonists Category:Dopamine antagonists External links IUPHAR GPCR Database - Dopamine Receptors Zimmerberg, B., Dopamine receptors: A representative family of metabotropic receptors, Multimedia Neuroscience Education Project 2002 References ^ Girault J, Greengard P 2004. The neurobiology of dopamine signaling. Arch Neurol 61 5: 641-4. doi:10.1001/archneur.61.5.641. PMID 15148138. ^ a b c Contreras F, Fouillioux C, Bolívar A, Simonovis N, Hernández-Hernández R, Armas-Hernandez M, Velasco M 2002. Dopamine, hypertension and obesity. J Hum Hypertens 16 Suppl 1: S13-7. doi:10.1038/sj.jhh.1001334. PMID 11986886. ^ Hurley MJ, Jenner P 2006. What has been learnt from study of dopamine receptors in Parkinson's disease?. Pharmacol Ther.. PMID 16458973. ^ Neves SR, Ram PT, Iyengar R May 2002. G protein pathways. Science journal 296 5573: 1636-9. doi:10.1126/science.1071550. PMID 12040175. ^ Suzuki M, Hurd YL, Sokoloff P, Schwartz JC, Sedvall G. D3 dopamine receptor mRNA is widely expressed in the human brain. Brain Res. 1998 Jan 1;7791-2:58-74. PMID 9473588 ^ Williams G, Castner S 2006. Under the curve: critical issues for elucidating D1 receptor function in working memory. Neuroscience 139 1: 263-76. doi:10.1016/j.neuroscience.2005.09.028. PMID 16310964. ^ Ricci A, Mignini F, Tomassoni D, Amenta F 2006. Dopamine receptor subtypes in the human pulmonary arterial tree. Auton Autacoid Pharmacol 26 4: 361-9. doi:10.1111/j.1474-8673.2006.00376.x. PMID 16968475. ^ a b c d Hussain T, Lokhandwala M 2003. Renal dopamine receptors and hypertension. Exp Biol Med Maywood 228 2: 134-42. PMID 12563019. ^ Ricci A, Bronzetti E, Fedele F, Ferrante F, Zaccheo D, Amenta F 1998. Pharmacological characterization and autoradiographic localization of a putative dopamine D4 receptor in the heart. J Auton Pharmacol 18 2: 115-21. doi:10.1046/j.1365-2680.1998.1820115.x. PMID 9730266. ^ Schneier FR, Liebowitz MR, Abi-Dargham A, Zea-Ponce Y, Lin SH, Laruelle M 2000. Low dopamine D2 receptor binding potential in social phobia. Am J Psychiatry 157 3: 457-459. doi:10.1176/appi.ajp.157.3.457. PMID 10698826. ^ a b c Kienast T, Heinz A 2006. Dopamine and the diseased brain. CNS Neurol Disord Drug Targets 5 1: 109-31. doi:10.2174/187152706784111560. PMID 16613557. ^ Fuxe K, Manger P, Genedani S, Agnati L 2006. The nigrostriatal DA pathway and Parkinson's disease. J Neural Transm Suppl 70: 71-83. doi:10.1007/978-3-211-45295-0_13. PMID 17017512. ^ Mihara K, Kondo T, Suzuki A, et al 2003. Relationship between functional dopamine D2 and D3 receptors gene polymorphisms and neuroleptic malignant syndrome. Am. J. Med. Genet. B Neuropsychiatr. Genet. 117 1: 57-60. doi:10.1002/ajmg.b.10025. PMID 12555236. ^ Faraone S, Khan S 2006. Candidate gene studies of attention-deficit/hyperactivity disorder. J Clin Psychiatry 67 Suppl 8: 13-20. PMID 16961425. ^ a b Hummel M, Unterwald E 2002. D1 dopamine receptor: a putative neurochemical and behavioral link to cocaine action. J Cell Physiol 191 1: 17-27. doi:10.1002/jcp.10078. PMID 11920678. ^ a b Gornick M, Addington A, Shaw P, Bobb A, Sharp W, Greenstein D, Arepalli S, Castellanos F, Rapoport J 2007. Association of the dopamine receptor D4 DRD4 gene 7-repeat allele with children with attention-deficit/hyperactivity disorder ADHD: An update. Am J Med Genet B Neuropsychiatr Genet 144 3: 379-82. doi:10.1002/ajmg.b.30460. PMID 17171657. ^ Schoots O, Van Tol H 2003. The human dopamine D4 receptor repeat sequences modulate expression. Pharmacogenomics J 3 6: 343-8. doi:10.1038/sj.tpj.6500208. PMID 14581929. ^ a b c Di Chiara G, Bassareo V, Fenu S, De Luca M, Spina L, Cadoni C, Acquas E, Carboni E, Valentini V, Lecca D 2004. Dopamine and drug addiction: the nucleus accumbens shell connection. Neuropharmacology 47 Suppl 1: 227-41. PMID 15464140. ^ Jose P, Eisner G, Felder R 2003. Regulation of blood pressure by dopamine receptors. Nephron Physiol 95 2: p19-27. doi:10.1159/000073676. PMID 14610323. 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/Dopamine_receptor Categories: G protein coupled receptorsHidden categories: All articles with statements | Articles with statements since April 2007 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 日本語 This page was last modified on 23 August 2008, at 19:56
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