Transmembrane segment five serines of the D4 dopamine receptor uniquely influence the interactions of dopamine, norepinephrine, and Ro10-4548

Journal of Pharmacology and Experimental Therapeutics

Volumn 333, Issue 3, 2010, Pages 682-695

  Cummings, David F ^a   Ericksen, Spencer S ^b   Goetz, Angela ^c   Schetz, John A ^a,d,e,f  

^a UNIVERSITY OF NORTH TEXAS HEALTH SCIENCE CENTER   (United States)

^b WEILL CORNELL MEDICAL COLLEGE   (United States)

^c UNIVERSITY OF ERLANGEN NUREMBERG   (Germany)

^d Texas College of Medicine   (United States)

^e UNT Health Sciences Center   (United States)

^f UNIVERSITY OF TEXAS AT ARLINGTON   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

[RAC 2' 2 HYDROXY 3 4 (4 HYDROXY 2 METHOXYPHENYL) 1 PIPERAZINYL PROPOXY ACETANILIDE]; ALANINE; CYCLIC AMP; DOPAMINE; DOPAMINE 4 RECEPTOR; DOPAMINE RECEPTOR BLOCKING AGENT; NORADRENALIN; QUINPIROLE; SERINE; SERINE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; CONTROLLED STUDY; HYDROGEN BOND; MOLECULAR DOCKING; NONHUMAN; POINT MUTATION; PRIORITY JOURNAL; RAT; RECEPTOR AFFINITY; SIGNAL TRANSDUCTION;

ACETANILIDES; ANIMALS; CELL MEMBRANE; CHO CELLS; CRICETINAE; CRICETULUS; CYCLIC AMP; DOPAMINE; DOPAMINE AGONISTS; DOPAMINE ANTAGONISTS; HUMANS; HYDROGEN BONDING; MODELS, MOLECULAR; MOLECULAR CONFORMATION; MUTATION; NOREPINEPHRINE; PIPERAZINES; PROTEIN BINDING; RADIOLIGAND ASSAY; RATS; RECEPTORS, DOPAMINE D4; SERINE; SIGNAL TRANSDUCTION; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 77952371606     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.109.164962     Document Type: Article

References (40)

1. 2-adrenergic receptors control the equilibrium between active and inactive receptor states. Mol Pharmacol 57:198-210.
2. Cheng Y and Prusoff WH (1973) Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction. Biochem Pharmacol 22:3099-3108.
3. Cohen AI, Todd RD, Harmon S, and O'Malley KL (1992) Photoreceptors of mouse retinas possess D4 receptors coupled to adenylate cyclase. Proc Natl Acad Sci USA 89:12093-12097. (Pubitemid 23004791)
4. Collins GT, Truccone A, Haji-Abdi F, Newman AH, Grundt P, Rice KC, Husbands SM, Greedy BM, Enguehard-Gueiffier C, Gueiffier A, et al. (2009) Proerectile effects of dopamine D2-like agonists are mediated by the D3 receptor in rats and mice. J Pharmacol Exp Ther 329:210-217.
5. Cowart M, Latshaw SP, Bhatia P, Daanen JF, Rohde J, Nelson SL, Patel M, Kolasa T, Nakane M, Uchic ME, et al. (2004) Discovery of 2-(4-pyridin-2- ylpiperazin-1-ylmethyl)-1H-benzimidazole (ABT-724), a dopaminergic agent with a novel mode of action for the potential treatment of erectile dysfunction. J Med Chem 47:3853-3864. (Pubitemid 38900350)
6. Cox BA, Henningsen RA, Spanoyannis A, Neve RL, and Neve KA (1992) Contributions of conserved serine residues to the interactions of ligands with dopamine D2 receptors. J Neurochem 59:627-635.
7. Cummings DF, Ericksen SS, and Schetz JA (2009) Three amino acids in the D2 dopamine receptor regulate selective ligand function and affinity. J Neurochem 110:45-57.
8. 2-adrenergic receptor. Mol Pharmacol 66:356-363.
9. Depoortère R, Bardin L, Rodrigues M, Abrial E, Aliaga M, and Newman-Tancredi A (2009) Penile erection and yawning induced by dopamine D2-like receptor agonists in rats: influence of strain and contribution of dopamine D2, but not D3 and D4 receptors. Behav Pharmacol 20:303-311.
10. Deupi X, Olivella M, Sanz A, Dölker N, Campillo M, and Pardo L (2010) Influence of the g-conformation of Ser and Thr on the structure of transmembrane helices. J Struct Biol 169:116-123.
11. Ericksen SS, Cummings DF, Weinstein H, and Schetz JA (2009) Ligand selectivity of D2 dopamine receptors is modulated by changes in local dynamics produced by sodium binding. J Pharmacol Exp Ther 328:40-54.
12. Floresca CZ and Schetz JA (2004) Dopamine receptor microdomains involved in molecular recognition and the regulation of drug affinity and function. J Recept Signal Transduct Res 24:207-239.
13. Johansson S, Halleland H, Halmøy A, Jacobsen KK, Landaas ET, Dramsdahl M, Fasmer OB, Bergsholm P, Lundervold AJ, Gillberg C, et al. (2008) Genetic analyses of dopamine-related genes in adult ADHD patients suggest an association with the DRD5-microsatellite repeat, but not with DRD4 or SLC6A3 VNTRs. Am J Med Genet B Neuropsychiatr Genet 147B:1470-1475.
14. Kortagere S, Gmeiner P, Weinstein H, and Schetz JA (2004) Certain 1,4-disubstituted aromatic piperidines and piperazines with extreme selectivity for the dopamine D4 receptor interact with a common receptor microdomain. Mol Pharmacol 66:1491-1499. (Pubitemid 39564775)
15. LaHoste GJ, Swanson JM, Wigal SB, Glabe C, Wigal T, King N, and Kennedy JL (1996) Dopamine D4 receptor gene polymorphism is associated with attention-deficit hyperactivity disorder. Mol Psychiatry 1:121-144. (Pubitemid 126442401)
16. Lanau F, Zenner MT, Civelli O, and Hartman DS (1997) Epinephrine and norepinephrine act as potent agonists at the recombinant human dopamine D4 receptor. J Neurochem 68:804-812. (Pubitemid 27044746)
17. 2 adrenergic receptor. Mol Pharmacol 65:1181-1190.
18. + channel modulation in transfected cells. Int J Neuropsychopharmacol 11:293-307.
19. Nir I, Harrison JM, Haque R, Low MJ, Grandy DK, Rubinstein M, and Iuvone PM (2002) Dysfunctional light-evoked regulation of cAMP in photoreceptors and abnormal retinal adaptation in mice lacking dopamine D4 receptors. J Neurosci 22:2063-2073. (Pubitemid 35386507)
20. Nyrönen T, Pihlavisto M, Peltonen JM, Hoffrén AM, Varis M, Salminen T, Wurster S, Marjamäki A, Kanerva L, Katainen E, et al. (2001) Molecular mechanism for agonist-promoted α(2A)-adrenoceptor activation by norepinephrine and epinephrine. Mol Pharmacol 59:1343-1354. (Pubitemid 32381614)
21. Patel S, Chapman KL, Marston D, Hutson PH, and Ragan CI (2003) Pharmacological and functional characterization of dopamine D4 receptors in the rat retina. Neuropharmacology 44:1038-1046. (Pubitemid 36570428)
22. Peltonen JM, Nyrönen T, Wurster S, Pihlavisto M, Hoffrén AM, Marjamäki A, Xhaard H, Kanerva L, Savola JM, Johnson MS, et al. (2003) Molecular mechanisms of ligand-receptor interactions in transmembrane domain V of the α2A-adrenoceptor. Br J Pharmacol 140:347-358. (Pubitemid 37249195)
23. Pollock NJ, Manelli AM, Hutchins CW, Steffey ME, MacKenzie RG, and Frail DE (1992) Serine mutations in transmembrane V of the dopamine D1 receptor affect ligand interactions and receptor activation. J Biol Chem 267:17780-17786.
24. Powell SB, Paulus MP, Hartman DS, Godel T, and Geyer MA (2003) RO-10-5824 is a selective dopamine D4 receptor agonist that increases novel object exploration in C57 mice. Neuropharmacology 44:473-481. (Pubitemid 36293979)
25. Sartania N and Strange PG (1999) Role of conserved serine residues in the interaction of agonists with D3 dopamine receptors. J Neurochem 72:2621-2624. (Pubitemid 29242216)
26. Schetz JA (2009) Dopamine receptors: introduction, IUPHAR database. Available from: http://www.iuphar-db.org/DATABASE/FamilyIntroductionForward? familyID=20.
27. Schetz JA, Benjamin PS, and Sibley DR (2000) Nonconserved residues in the second transmembrane-spanning domain of the D(4) dopamine receptor are molecular determinants of D(4)-selective pharmacology. Mol Pharmacol 57:144-152.
28. Schetz JA and Sibley DR (2001) The binding-site crevice of the D4 dopamine receptor is coupled to three distinct sites of allosteric modulation. J Pharmacol Exp Ther 296:359-363.
29. Schetz JA and Sibley D (2007) Dopaminergic neurotransmission, in Handbook of Contemporary Neuropharmacology (Sibley D, Hanin I, Kuhar MJ, and Skolnick P eds) pp 221-256, John Wiley & Sons, Inc, Hoboken, NJ.
30. Seifert R, Wenzel-Seifert K, Gether U, and Kobilka BK (2001) Functional differences between full and partial agonists: evidence for ligand-specific receptor conformations. J Pharmacol Exp Ther 297:1218-1226. (Pubitemid 32472524)
31. Shaw P, Gornick M, Lerch J, Addington A, Seal J, Greenstein D, Sharp W, Evans A, Giedd JN, Castellanos FX, et al. (2007) Polymorphisms of the dopamine D4 receptor, clinical outcome, and cortical structure in attention-deficit/ hyperactivity disorder. Arch Gen Psychiatry 64:921-931. (Pubitemid 47230616)
32. Simpson MM, Ballesteros JA, Chiappa V, Chen J, Suehiro M, Hartman DS, Godel T, Snyder LA, Sakmar TP, and Javitch JA (1999) Dopamine D4/D2 receptor selectivity is determined by a divergent aromatic microdomain contained within the second, third, and seventh membrane-spanning segments. Mol Pharmacol 56:1116-1126.
33. Strader CD, Candelore MR, Hill WS, Dixon RA, and Sigal IS (1989b) A single amino acid substitution in the β-adrenergic receptor promotes partial agonist activity from antagonists. J Biol Chem 264:16470-16477.
34. Strange PG (1996) The energetics of ligand binding at catecholamine receptors. Trends Pharmacol Sci 17:238-244. (Pubitemid 26233104)
35. 2 adrenoceptor binding site with catechol reveals differences in binding and activation by agonists and partial agonists. J Biol Chem 280:22165-22171.
36. 2 adrenoceptor. Kinetic evidence for intermediate conformational states. J Biol Chem 279:686-691.
37. Wiens BL, Nelson CS, and Neve KA (1998) Contribution of serine residues to constitutive and agonist-induced signaling via the D2S dopamine receptor: evidence for multiple, agonist-specific active conformations. Mol Pharmacol 54:435-444.
38. Wilcox RE, Huang WH, Brusniak MY, Wilcox DM, Pearlman RS, Teeter MM, DuRand CJ, Wiens BL, and Neve KA (2000) CoMFA-based prediction of agonist affinities at recombinant wild type versus serine to alanine point mutated D2 dopamine receptors. J Med Chem 43:3005-3019.
39. Woodward R, Coley C, Daniell S, Naylor LH, and Strange PG (1996) Investigation of the role of conserved serine residues in the long form of the rat D2 dopamine receptor using site-directed mutagenesis. J Neurochem 66:394-402. (Pubitemid 26010805)
40. Zuurmond HM, Hessling J, Blüml K, Lohse M, and Ijzerman AP (1999) Study of interaction between agonists and asn293 in helix VI of human β(2)-adrenergic receptor. Mol Pharmacol 56:909-916.