Adenosine A1 receptors in human brain and transfected CHO cells: Inhibition of [3H]CPFPX binding by adenosine and caffeine

Neuroscience Letters

Volumn 487, Issue 3, 2011, Pages 415-420

  Elmenhorst, David ^a   Garibotto, Valentina ^a,d   Prescher, Andreas ^b   Bauer, Andreas ^a,c  

^a FORSCHUNGSZENTRUM JÜLICH   (Germany)

^b RWTH AACHEN UNIVERSITY   (Germany)

^c Department of Orthopedic Surgery   (Germany)

^d GENEVA UNIVERSITY HOSPITALS   (Switzerland)

Author keywords

Adenosine; Brain; Caffeine; Competition; CPFPX; Human; Saturation binding

Indexed keywords

8 CYCLOPENTYL 3 (3 FLUOROPROPYL) 1 PROPYLXANTHINE F 18; 8 CYCLOPENTYL 3 (3 FLUOROPROPYL) 1 PROPYLXANTHINE H 3; ADENOSINE; ADENOSINE A1 RECEPTOR; CAFFEINE; GUANOSINE TRIPHOSPHATE; TRACER; UNCLASSIFIED DRUG;

AGED; ANIMAL CELL; ARTICLE; BRAIN HOMOGENATE; BRAIN TISSUE; CHO CELL; DISSOCIATION CONSTANT; GENETIC TRANSFECTION; GRAY MATTER; HUMAN; HUMAN TISSUE; HYPOXIA; IC 50; IN VIVO STUDY; NONHUMAN; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; QUANTITATIVE ANALYSIS; RECEPTOR DENSITY;

ADENOSINE; ANIMALS; BINDING, COMPETITIVE; BRAIN; CAFFEINE; CHO CELLS; CRICETINAE; CRICETULUS; HUMANS; POSITRON-EMISSION TOMOGRAPHY; RADIOPHARMACEUTICALS; RECEPTOR, ADENOSINE A1; TRANSFECTION; TRITIUM; XANTHINES;

EID: 78650521405     PISSN: 03043940     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.neulet.2010.10.068     Document Type: Article

References (31)

1. Arnaud M.J., Bracco I., Welsch C. Metabolism and distribution of labeled theophylline in the pregnant rat. Impairment of theophylline metabolism by pregnancy and absence of a blood-brain barrier in the fetus. Pediatr. Res. 1982, 16:167-171.
2. Ballarin M., Fredholm B.B., Ambrosio S., Mahy N. Extracellular levels of adenosine and its metabolites in the striatum of awake rats: inhibition of uptake and metabolism. Acta Physiol. Scand. 1991, 142:97-103.
3. Bauer A., Holschbach M.H., Meyer P.T., Boy C., Herzog H., Olsson R.A., Coenen H.H., Zilles K. In vivo imaging of adenosine A1 receptors in the human brain with [18F]CPFPX and positron emission tomography. Neuroimage 2003, 19:1760-1769.
4. Bonati M., Latini R., Galletti F., Young J.F., Tognoni G., Garattini S. Caffeine disposition after oral doses. Clin. Pharmacol. Ther. 1982, 32:98-106.
5. Bruns R.F., Lu G.H., Pugsley T.A. Characterization of the A2 adenosine receptor labeled by [3H]NECA in rat striatal membranes. Mol. Pharmacol. 1986, 29:331-346.
6. Brunye T.T., Mahoney C.R., Lieberman H.R., Taylor H.A. Caffeine modulates attention network function. Brain Cogn. 2009.
7. Chen Y., Parrish T.B. Caffeine dose effect on activation-induced BOLD and CBF responses. Neuroimage 2009, 46:577-583.
8. Cheng Y., Prusoff W.H. Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction. Biochem. Pharmacol. 1973, 22:3099-3108.
9. Cohen F.R., Lazareno S., Birdsall N.J. The effects of saponin on the binding and functional properties of the human adenosine A1 receptor. Br. J. Pharmacol. 1996, 117:1521-1529.
10. Daly J.W., Padgett W.L., Shamim M.T. Analogues of caffeine and theophylline: effect of structural alterations on affinity at adenosine receptors. J. Med. Chem. 1986, 29:1305-1308.
11. Daly J.W., Hide I., Bridson P.K. Imidazodiazepinediones: a new class of adenosine receptor antagonists. J. Med. Chem. 1990, 33:2818-2821.
12. Deckert J., Berger W., Kleopa K., Heckers S., Ransmayr G., Heinsen H., Beckmann H., Riederer P. Adenosine A1 receptors in human hippocampus: inhibition of [3H]8-cyclopentyl-1,3-dipropylxanthine binding by antagonist drugs. Neurosci. Lett. 1993, 150:191-194.
13. During M.J., Spencer D.D. Adenosine: a potential mediator of seizure arrest and postictal refractoriness. Ann. Neurol. 1992, 32:618-624.
14. Finlayson K., Maemoto T., Butcher S.P., Sharkey J., Olverman H.J. Comparison of effects of MgCl2 and Gpp(NH)p on antagonist and agonist radioligand binding to adenosine A1 receptors. Acta Pharmacol. Sin. 2003, 24:729-740.
15. Fredholm B.B. Purinoceptors in the nervous system. Pharmacol. Toxicol. 1995, 76:228-239.
16. Fredholm B.B., Chen J.F., Cunha R.A., Svenningsson P., Vaugeois J.M. Adenosine and brain function. Int. Rev. Neurobiol. 2005, 63:191-270.
17. Hagberg H., Andersson P., Lacarewicz J., Jacobson I., Butcher S., Sandberg M. Extracellular adenosine, inosine, hypoxanthine, and xanthine in relation to tissue nucleotides and purines in rat striatum during transient ischemia. J. Neurochem. 1987, 49:227-231.
18. Holschbach M.H., Olsson R.A., Bier D., Wutz W., Sihver W., Schuller M., Palm B., Coenen H.H. Synthesis and evaluation of no-carrier-added 8-cyclopentyl-3-(3-[(18)F]fluoropropyl)-1-propylxanthine ([(18)F]CPFPX): a potent and selective A(1)-adenosine receptor antagonist for in vivo imaging. J. Med. Chem. 2002, 45:5150-5156.
19. Klotz K.N., Hessling J., Hegler J., Owman C., Kull B., Fredholm B.B., Lohse M.J. Comparative pharmacology of human adenosine receptor subtypes-characterization of stably transfected receptors in CHO cells. Naunyn Schmiedebergs Arch. Pharmacol. 1998, 357:1-9.
20. Kostopoulos G., Drapeau C., Avoli M., Olivier A., Villemeure J.G. Endogenous adenosine can reduce epileptiform activity in the human epileptogenic cortex maintained in vitro. Neurosci. Lett. 1989, 106:119-124.
21. Kull B., Svenningsson P., Hall H., Fredholm B.B. GTP differentially affects antagonist radioligand binding to adenosine A(1) and A(2A) receptors in human brain. Neuropharmacology 2000, 39:2374-2380.
22. Liu X., Smith B.J., Chen C., Callegari E., Becker S.L., Chen X., Cianfrogna J., Doran A.C., Doran S.D., Gibbs J.P., Hosea N., Liu J., Nelson F.R., Szewc M.A., Van D.J. Evaluation of cerebrospinal fluid concentration and plasma free concentration as a surrogate measurement for brain free concentration. Drug Metab. Dispos. 2006, 34:1443-1447.
23. Magistretti P.J., Pellerin L. Metabolic coupling during activation. A cellular view. Adv. Exp. Med. Biol. 1997, 413:161-166.
24. Meyer P.T., Bier D., Holschbach M.H., Cremer M., Tellmann L., Bauer A. Image of the month. In vivo imaging of rat brain A1 adenosine receptor occupancy by caffeine. Eur. J. Nucl. Med Mol. Imaging 2003, 30:1440.
25. Muller C.E., Schumacher B., Brattstrom A., Abourashed E.A., Koetter U. Interactions of valerian extracts and a fixed valerian-hop extract combination with adenosine receptors. Life Sci. 2002, 71:1939-1949.
26. Sarges R., Howard H.R., Browne R.G., Lebel L.A., Seymour P.A., Koe B.K. 4-Amino[1,2,4]triazolo[4,3-a]quinoxalines. A novel class of potent adenosine receptor antagonists and potential rapid-onset antidepressants. J. Med. Chem. 1990, 33:2240-2254.
27. Schwabe U., Ukena D., Lohse M.J. Xanthine derivatives as antagonists at A1 and A2 adenosine receptors. Naunyn Schmiedebergs Arch. Pharmacol. 1985, 330:212-221.
28. Shryock J.C., Ozeck M.J., Belardinelli L. Inverse agonists and neutral antagonists of recombinant human A1 adenosine receptors stably expressed in Chinese hamster ovary cells. Mol. Pharmacol. 1998, 53:886-893.
29. Strecker R.E., Morairty S., Thakkar M.M., Porkka-Heiskanen T., Basheer R., Dauphin L.J., Rainnie D.G., Portas C.M., Greene R.W., McCarley R.W. Adenosinergic modulation of basal forebrain and preoptic/anterior hypothalamic neuronal activity in the control of behavioral state. Behav. Brain Res. 2000, 115:183-204.
30. Zeitzer J.M., Morales-Villagran A., Maidment N.T., Behnke E.J., Ackerson L.C., Lopez-Rodriguez F., Fried I., Engel J., Wilson C.L. Extracellular adenosine in the human brain during sleep and sleep deprivation: an in vivo microdialysis study. Sleep 2006, 29:455-461.
31. Zetterstrom T., Vernet L., Ungerstedt U., Tossman U., Jonzon B., Fredholm B.B. Purine levels in the intact rat brain. Studies with an implanted perfused hollow fibre. Neurosci. Lett. 1982, 29:111-115.