Partial agonism at the human α2A-autoreceptor: Role of binding duration

Naunyn-Schmiedeberg's Archives of Pharmacology

Volumn 378, Issue 1, 2008, Pages 17-26

  Hoeren, M ^a   Brawek, B ^a   Mantovani, M ^a   Loffler M ^a   Steffens, M ^a   Van Velthoven, V ^a   Feuerstein, T J ^a  

^a UNIVERSITY OF FREIBURG   (Germany)

Author keywords

2 Adrenoceptor; Activation interval; Binding duration; Efficacy; Partial agonism; Temperature

Indexed keywords

ALPHA 2 ADRENERGIC RECEPTOR STIMULATING AGENT; ALPHA 2A ADRENERGIC RECEPTOR; AUTORECEPTOR; BRIMONIDINE; CLONIDINE; GUANFACINE; NORADRENALIN; PARTIAL AGONIST; TRITIUM;

ADOLESCENT; ADULT; AGED; ARTICLE; BRAIN SLICE; BRAIN SYNAPTOSOME; CHILD; CONTROLLED STUDY; DRUG EFFICACY; DRUG RECEPTOR BINDING; ELECTROSTIMULATION; HUMAN; HUMAN TISSUE; NEOCORTEX; NORADRENALIN RELEASE; RECEPTOR AFFINITY; TEMPERATURE SENSITIVITY;

ADOLESCENT; ADRENERGIC ALPHA-AGONISTS; ADULT; AGED; AUTORECEPTORS; CHILD; CHILD, PRESCHOOL; CLONIDINE; FEMALE; GUANFACINE; HUMANS; INFANT; MALE; MIDDLE AGED; NEOCORTEX; PROTEIN BINDING; QUINOXALINES; RECEPTORS, ADRENERGIC, ALPHA-2; TEMPERATURE; TIME FACTORS; YOUNG ADULT;

EID: 45849096809     PISSN: 00281298     EISSN: None     Source Type: Journal    
DOI: 10.1007/s00210-008-0295-6     Document Type: Article

References (27)

1. 2-adrenergic selectivity and differing affinities for GTP. Life Sci 43:1805-1812
2. Bylund DB, Murrin LC (2000) Radioligand saturation binding experiments over large concentration ranges. Life Sci 67:2897-2911
3. Cash R, Raisman R, Ruberg M, Agid Y (1985) Adrenergic receptors in frontal cortex in human brain. Eur J Pharmacol 108:225-232
4. Dalpiaz A, Scatturin A, Varani K, Pecoraro R, Pavan B, Borea PA (2000) Binding thermodynamics and intrinsic activity of adenosine A1 receptor ligands. Life Sci 67:1517-1524
5. Feuerstein TJ, Limberger N (1999) Mathematical analysis of the control of neurotransmitter release by presynaptic receptors as a supplement to experimental data. Naunyn-Schmiedeberg's Arch Pharmacol 359:345-359
6. Feuerstein TJ, Dooley DJ, Seeger W (1990) Inhibition of norepinephrine and acetylcholine release from human neocortex by ω-Conotoxin GVIA. J Pharmacol Exp Ther 252:778-785
7. Feuerstein TJ, Huber B, Vetter J, Aranda H, Van Velthoven V, Limberger N (2000) Characterization of the α2-adrenoceptor subtype, which functions as α2-autoreceptor in human neocortex. J Pharmacol Exp Ther 294:356-362
8. 2 adrenergic receptor. J Biol Chem 276:24433-24436
9. Hein P, Rochais F, Hoffmann C, Dorsch S, Nikolaev VO, Engelhardt S, Berlot CH, Lohse MJ, Bunemann M (2006) Gs activation is time-limiting in initiating receptor-mediated signaling. J Biol Chem 281:33345-33351
10. Jasper JR, Insel PA (1992) Evolving concepts of partial agonism. The beta-adrenergic receptor as a paradigm. Biochem Pharmacol 43:119-130
11. Jin R, Banke TG, Mayer ML, Traynelis SF, Gouaux E (2003) Structural basis for partial agonist action at ionotropic glutamate receptors. Nat Neurosci 6:803-810
12. Kenakin T (2002) Drug efficacy at G protein-coupled receptors. Annu Rev Pharmacol Toxicol 42:349-379
13. Kenakin T (2004) Principles: receptor theory in pharmacology. Trends Pharmacol Sci 25:186-192
14. Kilpatrick GJ, el Tayar N, Van de Waterbeemd H, Jenner P, Testa B, Marsden CD (1986) The thermodynamics of agonist and antagonist binding to dopamine D-2 receptors. Mol Pharmacol 30:226-234
15. Koshland DE Jr., Nemethy G, Filmer D (1966) Comparison of experimental binding data and theoretical models in proteins containing subunits. Biochemistry 5:365-385
16. Lowry OH, Rosebrough NJ, Farr AL, Randall RJ (1951) Protein measurement with the Folin phenol reagent. J Biol Chem 193:265-275
17. Monod J, Wyman J, Changeux JP (1965) On the nature of allosteric transitions: a plausible model. J Mol Biol 12:88-118
18. i-protein heterotrimer. J Biol Chem 281:24506-24511
19. 3H]clonidine binding. Mol Pharmacol 35:345-354
20. Ross EM (1996) Pharmacodynamics. Mechanisms of drug action and the relationship between drug concentration and effect. In: Goodman, Gilman's The pharmacological basis of therapeutics, J.G. Hardman, L.E. Limbird (eds.), The McGraw-Hill Companies 9th edn. pp 29-41
21. Seifert R, Wenzel-Seifert K, Gether U, Kobilka BK (2001) Functional differences between full and partial agonists: evidence for ligand-specific receptor conformations. J Pharmacol Exp Ther 297:1218-1226
22. 2-adrenoceptor agonist exceed its activation interval at the autoreceptor? Int J Pharmacol 1:299-310
23. Stephenson RP (1956) A modification of receptor theory. Br J Pharmacol Chemother 11:379-393
24. Stickle D, Barber R (1989) Evidence for the role of epinephrine binding frequency in activation of adenylate cyclase. Mol Pharmacol 36:437-445
25. Vilardaga JP, Bunemann M, Krasel C, Castro M, Lohse MJ (2003) Measurement of the millisecond activation switch of G protein-coupled receptors in living cells. Nat Biotechnol 21:807-812
26. Vrbjar N, Kean KT, Szabo A, Senak L, Mendelsohn R, Keough KM (1992) Sarcoplasmic reticulum from rabbit and winter flounder: temperature-dependence of protein conformation and lipid motion. Biochim Biophys Acta 1107:1-11
27. Weiland GA, Minneman KP, Molinoff PB (1979) Fundamental difference between the molecular interactions of agonists and antagonists with the beta-adrenergic receptor. Nature 281:114-117