Abstract
The purine nucleoside adenosine has been shown to act as a neuromodulator in many areas of the mammalian brain. One of the main actions of adenosine in the central nervous system is the modulation of the release of a variety of neurotransmitters. Adenosine acts as a general depressant in the brain. In contrast, adenosine receptor antagonists show somnolytic and stimulant properties. Although purinergic psychopharmaceuticals are rare, the nonselective adenosine receptor antagonist caffeine may currently be considered the most frequently used nonprescription drug (Fredholm, 1995). Caffeine is of therapeutical benefit in states of migraine headache and headache of nonvascular origin. It is used as an adjuvant in analgesic medications, for the treatment of idiopathic apnea in premature neonates, and for seizure prolongation during courses of electroconvulsive therapy for the treatment of depression (Sawynok, 1995).
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References
Bourne, H. R. and Stryer, L. (1992) The target sets the tempo. Nature (Lond ) 358, 541–543
Bridges, A. J., Moos, W. H., Szotek, D. L, Trivedi, B. K., Bristol, J. A., Heffner, T. G., Bruns, R. F, and Downs, D A (1987) N6-(2,2-Diethyl)adenosine, a novel adenosine receptor agonist with antipsy-chotic-like activity. J Med.Chem 30, 1709–1711.
Bruns, R. F., Fergus, J H., Badger, E. W., Bristol, J. A., Santay, L A., Hartman, J. D., Hays, S. J, and Huang, C. C (1987) Binding of the Al-selective adenosine antagonist 8-cyclopentyl-l,3-dipropylxanthine to rat brain membranes. Naunyn-Schmiedeberg’s Arch Pharmacol 335, 59–63
Carter, A J., O’Connor, W. T., Carter, M. J., and Ungerstedt, U. (1995) Caffeine enhances acetylcholine release m the hippocampus in vivo by a selective interaction with adenosine Al receptors. J. Pharmacol Exp. Ther 273, 637–642
Cooper, D. M. F., Londos, C, and Rodbell, M. (1980) Adenosine receptor-mediated inhibition of rat cerebral cortical adenylate cyclase by a GTP-dependent process. Mol Pharmacol, 18, 598–601.
Daly, J. W., Butts-Lamb, P., and Padgett, W. (1983) Subclasses of adenosine receptors in the central nervous system-Interaction with caffeine and related methylxanthines. Cell Mol Neurobiol 3, 69–80
Dolphin, A. C. and Archer, E. R. (1983) An adenosine agonist inhibits and a cyclic AMP analogue enhances the release of glutamate but not GABA from slices of rat dentate gyrus Neurosci Lett 43, 49–54
Dragunow, M., Goddard, G. V., and Laverty, R. (1985) Is adenosine an endogenous anticonvulsant? Epilepsia 26, 480–487.
Drejer, J., Frandsen, A., Honoré, T., and Schousboe, A. (1987) Adenosine inhibits glutamate stimulated [3H]D-aspartate release from cerebellar granule cells. Neurochem. Int 11, 77–81
Dunwiddie, V and Fredholm, B B (1985) Adenosine modulation of synaptic responses in rat hippocampus: Possible role of inhibition or activation of adenylate cyclase. Adv Cyclic Nucleotide Protein Phosphorylation Res 19, 259–272
Dux, E., Fastboom, J, Ungerstedt, U, Rudolphi, K., and Fredholm, B. B (1990) Protective effect of adenosine and a novel xanthine derivative propentofylline on the cell damage after bilateral carotid occlusion. Brain Res 516, 248–256.
Ehlert, F. J (1985) The relationship between muscarinic receptor occupancy and adenylate cyclase inhibition in the rabbit myocardium Mol. Pharmacol. 28, 410–421.
Fastboom, J. and Fredholm, B. B (1990) Regional differences in the effect of guanine nucleotides on agonist and antagonist binding to adenosine Al-receptors in rat brain, as revealed by autoradiography. Neuroscience 34, 759–769.
Fastboom, J., Pazos, A., Probst, A., and Palacios, J M. (1987) Adenosine A 1 receptors in the human brain: A quantitative autoradiographic study. Neuroscience 22, 827–839
Ferré, S., Snaprud, P, and Fuxe, K (1993) Opposing actions of an adenosine A2 receptor agonist and a GTP analogue on the regulation of dopamine D2 receptors in rat neostriatal membranes. Eur. J Pharmacol (Mol. Pharmacol Section) 244, 311–315.
Ferré, S., von Euler, G, Johansson, B., Fredholm, B., and Fuxe, K (1991) Stimulation of high-affinity adenosine A2 receptors decreases the affinity of dopamine D2 receptors in rat striatal membranes. Proc. Natl. Acad. Sci. USA 88, 7238–7241.
Ferré, S., Fuxe, K., von Euler, G, Johansson, B., and Fredholm, B. B. (1992) Adenosine-dopamme interactions in the brain. Neuroscience 51, 501–512.
Fink, J. S, Weaver, D R., Rivkees, S. A., Peterfreund, S A., Pollack, A. E, Adler, E. M, and Reppert, S. M. (1992) Molecular cloning of the rat A2 adenosine receptor: selective co-expression with D2 dopamine receptors in rat striatum. Mol. Brain Res. 14, 186–195
Fredholm, B. B (1995) Adenosine, adenosine receptors and the actions of caffeine. Pharmacol Toxicol. 76, 93–101.
Fredholm, B. B. and Lindgren, E. (1987) Effects of N-ethylmaleimide and forskolin on noradrenaline release from rat hippocampal slices Evidence that prejunctional adenosine and α-receptors are linked to N-proteins but not to adenylate cyclase. Acta Physiol. Scand. 130, 95–105.
Fredholm, B B., Lindgren, E, and Lindstrom, K. (1985) Treatment with N-ethylmaleimide selectively reduces adenosine receptor-mediated decreases in cyclic AMP accumulation in rat hippocampal slices. Br J. Pharmacol. 86, 509–513.
Freissmuth, M, Schutz, W., and Linder, M E (1991a) Interactions of the bovine brain A1-adenosine receptor with recombinant G protein α-subunits. Selectivity for rG1α-3 J. Biol. Chem. 266, 17,778–17,783.
Freissmuth, M., Selzer, E., and Schutz, W. (1991b) Interactions of purified bovine bram A1 adenosine receptors with G proteins. Reciprocal modulation of agonist and antagonist binding. Biochem J. 275, 651–656.
Gallo-Rodriguez, C, Ji, X.-D., Melman, N., Siegman, B D, Sanders, L. H, Orlina, J, Fischer, B., Pu, Q., Olah, M. E., van Galen, P. J. M., Stiles, G. L, and Jacobson, K. A. (1994) Structure-activity relationships of N6-benzyladenosrne-5′-uronamides as A3-selective adenosine agonists. J. Med. Chem. 37, 636–646.
Georgiev, V, Johansson, B, and Fredholm, B B (1993) Long-term caffeine treatment leads to a decreased susceptibility to NMDA-induced clonic seizures in mice without changes in adenosine A1 receptor number. Brain Res. 612, 271–277
Gierschik, P, Moghtader, R, Straub, C, Dieterich, K., and Jakobs, K. H. (1991) Signal amplification m HL-60 granulocytes. Eur. J. Biochem 197, 725–732.
Gilman, A. G. (1987) G proteins: transducers of receptor-generated signals Annu Rev Biochem 56, 615–649
Goldsmith, P., Rossiter, K., Carter, A., Simonds, W., Unson, C G., Vinitsky, R, and Spiegel, A. M. (1988) Identification of the GTP-binding protein encoded by G13 complementary DNA J Biol Chem. 263, 6476–6479
Goodman, R R, Cooper, M. J., Gavish, M., and Snyder, S H (1982) Guanine nucleotide and cation regulation of the binding of [3H]cyclohexyladenosine and [3H]diethylphenylxanthine to adenosine A1 receptors in brain membranes Mol. Pharmacol 21, 329–335
Hagberg, H, Andersson, P., Lacarewicz, J., Jacobson, I, Butcher, S., and Sandberg, M. (1987) Extracellular adenosme, inosine, hypoxanthine, and xanthine in relation to tissue nucleotides and purines in rat striatum during transient ischemia J Neurochem 49, 227–231
Harms, H. H., Warden, G., and Mulder, A H (1979) Effects of adenosine on depolarization-induced release of various radiolabeled neurotransmitters from slices of rat corpus striatum. Neuropharmacology 18, 577–580
Haussleithner, V, Freissmuth, M, and Schutz, W (1985) Adenosine-receptor-mediated stimulation of low-Km GTPase in guinea pig cerebral cortex Biochem. J. 232, 501–504
Hawkins, M., Pan, W, Stefanovich, P, and Radulovacki, M. (1988) Desensitation of adenosme A2 receptors in the striatum of the rat following chronic treatment with diazepam. Neuropharmacology 27, 1131–1140.
Heffner, T. G., Wiley, J N, Williams, A E, Bruns, R F., Coughenour, L L, and Downs, D. A. (1987) Comparison of the behavioral effects of adenosine agonists and dopamine antagonists in mice Psychopharmacology 98, 31–37
Heurteaux, C, Lauritzen, I., Widmann, C. and Lazdunski, M (1995) Essential role of adenosine, adenosine A1 receptors, and ATP-sensitive K+ channels in cerebral ischemic preconditioning Proc Natl. Acad Sci. USA 92, 4666–4670.
Higashijima, T., Ferguson, K. M., Sternweis, P C, Smigel, M. D, and Gilman, A G (1987) Effects of Mg2+ and the βγ-subunit complex on the interactions of guanine nucleotides with G proteins. J. Biol Chem 262, 762–766
Hilf, G. and Jakobs, K H (1992) Agonist-independent inhibition of G protein activation by muscarinic acetylcholine receptor antagonists in cardiac membranes Eur J. Pharmacol 225, 245–252.
Hilf, G., Gierschik, P, and Jakobs, K H. (1989) Muscarinic acetylcholine receptor-stimulated binding of guanosine-5′-O-(3-thiotriphosphate) to guanine-nucleotide-binding proteins in cardiac membranes. Eur J Biochem 186, 725–731
Hollins, C and Stone, T. W. (1980) Adenosme inhibits γ-amino-butyric acid release from slices of rat cerebral cortex. Br J Pharmacol. 69, 107–112
Jacobson, K. A., Nikodijevic, O., Shi, D, Gallo-Rodriguez, C, Olah, M. E, Stiles, G. L, and Daly, J. W (1993) A role for central A3-adenosine receptors. Mediation of behavioral depressant effects. FEBS Lett 336, 57–60.
Jarvis, M F and Williams, M. (1989) Direct autoradiographic localization of adenosine A2 receptors in the rat brain using the A2-selective agonist, [3H]CGS 21680. Eur. J. Pharmacol. 168, 243–246.
Jarvis, M. F., Jackson, R. H., and Williams, M. (1989a) Autoradiographic characterization of the high-affinity adenosine A2 receptors in the rat brain Brain Res 484, 111–118.
Jarvis, M. F., Schulz, R., Hutchison, A J, Do, U. H., Sills, M. A., and Williams, M. (1989b) [3H]CGS 21680, a selective A2 adenosine recep-tor agonist directly labels A2 receptors in rat brain. J. Pharmacol Exp Ther. 251, 888–893
Ji, X.-D, Stiles, G L, and Jacobson, K. A. (1991) [3H]XAC (xanthine amine congener) is a radioligand for A2-adenosine receptors in rabbit striatum. Neurochem. Int. 18, 207–213.
Ji, X.-D., Stiles, G. L., van Galen, P. J M, and Jacobson, K. A. (1992) Characterization of human striatal A2-adenosine receptors using radioligand binding and photoaffinity labeling. J. Recept. Res. 12, 149–169.
Jockers, R., Linder, M E., Hohenegger, M., Nanoff, C, Bertin, B., Strosberg, A. D., Marullo, S., and Freissmuth, M. (1994) Species difference in the G protein selectivity of the human and bovine A1-adenosme receptor J. Biol. Chem. 269, 32,077–32,084
Johansson, B, Parkinson, F E, and Fredholm, B. B. (1992) Effects of mono-and divalent ions on the binding of the adenosine analogue CGS 21680 to adenosine A2 receptors in rat striatum. Biochem. Pharmacol 44, 2365–2370.
Jonzon, B and Fredholm, B B. (1984) Adenosine receptor mediated inhibition of noradrenaline release from slices of the rat hippocampus. Life Sci. 35, 1971–1979.
Kendall, D A and Hill, S J (1988) Adenosine inhibition of histamine-stim-ulated inositol phospholipid hydrolysis in mouse cerebral cortex. J. Neurochem 50, 497–502.
Kent, R S, de Lean, A, and Lefkowitz, R. J. (1980) A quantitative analysis of beta-adrenergic receptor interactions: Resolution of high and low affinity states of the receptor by computer modeling of ligand binding data Mol Pharmacol 17, 14–23.
Klotz, K.-N., Lohse, M. J., Schwabe, U, Cristalli, G., Vittori, S., and Grxfantini, M(1989) 2-Chloro-N6-[3H]cyclopentyladenosine (3H]CCPA)— a high affinity agonist radioligand for A1 adenosine receptors. Naunyn-Schmiedeberg’s Arch. Pharmacol. 340, 679–683.
Klotz, K-N, Keil, R., Zimmer, F. J., and Schwabe, U (1990) Guanine nucleotide effects on 8-cyclopentyl-l,3-[3H]dipropylxanthine binding to membrane-bound and solubilized A1 adenosine receptors of rat brain J Neurochem 54, 1988–1994.
Lahti, R. A., Figur, L. M., Piercey, M. F., Ruppel, P. L., and Evans, D. L. (1992) Intrinsic activity determinations at the dopamine D2 guanine nucleotide-bindmg protein-coupled receptor: utilization of receptor state binding affinities Mol Pharmacol 42, 432–438.
Laugwitz, K-L., Spicher, K., Schultz, G, and Offermanns, S. (1994) Identification of receptor-activated G proteins: Selective lmmunoprecipitation of photolabeled G protein α subunits Methods Enzymol 237, 283–294.
Lohse, M. J., Lenschow, V., and Schwabe, U (1984) Two affinity states of R1 adenosine receptors in brain membranes. Mol Pharmacol 26, 1–9.
Lohse, M J., Klotz, K.-N., Jakobs, K. H, and Schwabe, U. (1985) Barbiturates are selective antagonists at A1 adenosine receptors J Neurochem. 45, 1761–1770.
Lohse, M. J, Klotz, K-N., Lindenborn-Fotmos, J, Reddington, M., Schwabe, U., and Olsson, R. A. (1987a) 8-Cyclopentyl-l,3-dipropylxanthine (DPCPX)—a selective high affinity antagonist radioligand for A1 adenosine receptors. Naunyn-Schmiedeberg’s Arch. Pharmacol 336, 204–210
Lohse, M. J., Brenner, A S, and Jackisch, R. (1987b) Pentobarbital antagonizes the A1 receptor-mediated inhibition of hippocampal neurotransmitter release. J Neurochem. 49, 189–194.
Lohse, M. J, Boser, S., Klotz, K.-N., and Schwabe, U (1987c) Affinities of barbiturates for the GABA-receptor complex and A1 adenosine receptors, a possible explanation of their excitatory effects. Naunyn-Schmiedeberg’s Arch Pharmacol 336, 211–217.
Lorenzen, A., Fuss, M, Vogt., H, and Schwabe, U. (1993) Measurement of guanine nucleotide binding protein activation by A1 adenosine receptor agonists in bovine brain membranes, stimulation of guanosine-5′-O-(3-[35S]thio)triphosphate binding Mol Pharmacol. 44, 115–123
Luthin, D. R., Olsson, R A, Thompson, R D., Sawmiller, D R, and Linden, J. (1995a) Characterization of two affinity states of adenosine A2a receptors with a new radioligand, 2-[2-(4-amino-3-[125I]iodophenyl)-ethylamino]adenosine. Mol. Pharmacol. 47, 307–313
Luthin, D R, Lee, K. S, Okonkwo, D., Zhang, P J, and Linden, J (1995b) Photoaffinity labeling with 2-[2-(4-azido-3-[I-125]iodophenyl)ethylamino]adenosine of A2a adenosine receptors in rat brain. J. Neurochem. 65, 2072–2079
Marala, R B. and Mustafa, S J. (1993) Direct evidence for the coupling of A2-adenosine receptor to stimulatory guanine nucleotide-binding-protein in bovme brain striatum. J. Pharmacol Exp Ther. 266, 294–300
Marangos, P. J, Weiss, S R. B, Montgomery P., Patel, J, Narang, P. K., Cappabianca, A. M., and Post, R M. (1985) Chronic carbamazepine treatment increases brain adenosine receptors Epilepsia 26, 493–498.
Marangos, P. J., Montgomery, P., Weiss, S. R. B., Patel, J., and Post, R M. (1987) Persistent upregulation of brain adenosine receptors in response to chronic carbamazepine treatment. Clin Neurophartnacol. 10, 443–448
Martin, R L., Lloyd, H. G. E, and Cowan, A. I (1994) The early events of oxygen and glucose deprivation, setting the scene for neuronal death? Trends Neurosci 17, 251–257.
Michaelis, M. L., Michaelis, E. K., and Myers, S. L. (1979) Adenosine modulation of synaptosomal dopamine release. Life Sci 24, 2083–2092
Morgan, P. F and Stone, T. W. (1986) Inhibition by benzodiazepines and beta-carbolines of brief (5 seconds) synaptosomal accumulation of [3H]-adenosine. Biochem. Pharmacol. 35, 1760–1762.
Munshi, R. and Linden, J. (1989) Co-purification of A1 adenosine receptors and guanine nucleotide-binding proteins from bovine brain. J. Biol. Chem 264, 14,853–14,589.
Munshi, R, Pang, I.-H., Sternweis, P., and Linden, J. (1991) Aj Adenosine receptors of bovine brain couple to guanine nucleotide-binding proteins G11 G12, and G0. J. Biol Chem. 266, 22,285–22,289
Nakahata, N., Abe, M. T, Matsuoka, I., Ono, T., and Nakanishi, H. (1991) Adenosine inhibits histamine-induced phosphoinositide hydrolysis mediated via pertussis toxin-sensitive G protein in human astrocytoma cells. J. Neurochem. 57, 963–969
Nonaka, H, Mori, A., Ichimura, M., Shmdou, T., Yanagawa, K., Shimada, J, and Kase, H (1994) Binding of [3H]KF17387S, a selective adenosine A2 receptor antagonist, to rat brain membranes. Mol. Pharmacol 46, 817–822.
Offermanns, S., Schultz, G., and Rosenthal, W. (1991) Identification of receptor-activated G proteins with photoreactive GTP analog, [α-32P]GTP azidoanihde. Methods Enzymol. 195, 286–301.
Olah, M E., Gallo-Rodriguez, C, Jacobson, K A., and Stiles, G. L (1994) 125I-4-Ammobenzyl-5′-N-methylcarboxamidoadenosine, a high affinity radioligand for the rat A3 adenosine receptor. Mol Pharmacol 45, 978–982.
O’Regan, M. H and Phillis, J W. (1988) Potentiation of adenosine-evoked depression of rat cerebral cortical neurons by triazolam. Brain Res 445, 376–379.
Palmer, T M., Gettys, T W., and Stiles, G. L. (1995) Differential interaction with and regulation of multiple G proteins by the rat A3 adenosine receptor. J. Biol Chem. 270, 16,895–16,902.
Parkinson, F. E. and Fredholm, B. B. (1990) Autoradiographic evidence for G protein coupled A2-receptors in rat neostriatum using [3H]-CGS 21680 as a ligand. Naunyn-Schmiedeberg’s Arch Pharmacol 342, 85–89.
Pedata, F., Antonelli, T., Lambertini, L., Beam, L., and Pepeu, G. (1983) Effect of adenosine, adenosine triphosphate, adenosine deaminase, dipyridamole, and aminophylline on acetylcholine release from electrically-stimulated brain slices Neuropharmacology 22, 609–614.
Phillis, J. W. and Stair, R. E. (1987) Ro 15-1788 both antagonizes and potentiates adenosine-evoked depression of cerebral cortical neurons Eur J. Pharmacol 136, 151–156
Phillis, J. W., Wu, P. H, and Bender, A. S. (1981) Inhibition of adenosine uptake into rat brain synaptosomes by the benzodiazepines. Gen. Pharmacol 12, 67–70.
Prater, M. R., Taylor, H., Munshi, R., and Linden, J (1992) Indirect effect of guanine nucleotides on antagonist bindmg to A1 adenosine receptors: occupation of cryptic binding sites by endogenous vesicular adenosine. Mol. Pharmacol. 42, 765–772.
Prémont, J., Perez, M., Tassin, J-P., Thierry, A-M., Hervé, D., and Bockaert, J. (1979) Adenosine-sensitive adenylate cyclase in rat brain homogenates: kinetic characteristics, specificity, topographical, subcellular and cellular distribution Mol. Pharmacol. 16, 790–804.
Proctor, W. R and Dunwiddie, T. V. (1987) Pre-and postsynaptic actions of adenosine in the in vitro rat hippocampus Brain Res. 426, 187–190
Ramkumar, V, Bumgarner, J. R., Jacobson, K A, and Stiles, G L. (1988) Multiple components of the A1 adenosine receptor-adenylate cyclase system are regulated m rat cerebral cortex by chronic caffeine ingestion. J. Clin. Invest. 82, 242–247
Ramkumar, V., Stiles, G. L., Beaven, M. A., and Ali, H. (1993) The A3 adenosine receptor is the unique adenosine receptor which facilitates release of allergic mediators in mast cells J. Biol Chem 268, 16,887–16,890.
Rudolphi, K. A., Keil, M, Fastboom, J, and Fredholm, B. B. (1989) Ischaemic damage in gerbil hippocampus is reduced following upregulation of adenosine (A1) receptors by caffeine treatment Neurosa Lett. 103, 275–280.
Rudolphi, K. A., Schubert, P., Parkinson, F. A, and Fredholm, B. B. (1992) Neuroprotective role of adenosine m cerebral ischemia Trends Pharmacol Sci 13, 439–445
Salvatore, C A, Jacobson, M. A., Taylor, H. E, Linden, J, and Johnson, R G. (1993) Molecular cloning and characterization of the human A3 adenosme receptor. Proc Natl Acad. Sci. USA 90, 10,365–10,369.
Sawynok, J (1995) Pharmacological rationale for the clinical use of caffeine Drugs 49, 37–50
Schiffmann, S. N, Jacobs, O, and Vanderhaeghen, J-J (1991) Striatal restricted adenosine A2 receptor (RDC8) is expressed by enkephalin but not by substance P neurons an in situ hybridization study. J Neurochem 57, 1062–1067.
Schingnitz, G, Küfner-Muhl, U, Ensinger, H, Lehr, E, and Kuhn, F J. (1991) Selective Aj-antagomsts for treatment of cognitive deficits. Nucleosides Nucleotides 10, 1067–1076.
Schnecko, A., Witte, K., Bohl, J., Ohm, T., and Lemmer, B. (1994) Adenylyl cyclase activity in Alzheimer’s disease brain: stimulatory and inhibitory and signal transduction pathways are differentially affected Brain Res. 644, 291–296.
Scholz, K. P and Miller, R J (1991) Analysis of adenosine actions on Ca2+ currents and synaptic transmission in cultured rat hippocampal pyramidal neurones. J. Physiol. (Lond.) 435, 373–393
Scholz, K. P. and Miller, R. J. (1992) Inhibition of quantal transmitter release in the absence of calcium influx by a G protein-linked adenosine receptor at rat hippocampal synapses. Neuron 8, 1139–1150.
Scott, R. H. and Dolphin, A. C. (1987) Inhibition of calcium currents by an adenosine analogue 2-chloroadenosine, in Topics and Perspectives in Adenosine Research (Gerlach, E., and Becker, B. E, eds.), Springer-Verlag, Berlin, pp 549–558
Skolnick, P., Paul, S. M, and Marangos, P. J. (1980) Purines as endogenous ligands of the benzodiazepine receptor. Fed. Proc. 39, 3050–3055.
Stehle, J H., Rivkees, S A., Lee, J. J., Weaver, D. R., Deeds, J. D., and Reppert, S. M. (1992) Molecular cloning and expression of the cDNA for a novel A2-adenosme receptor subtype Mol Endocrinol. 6, 384–393
Stiles, G L. (1988) A1 Adenosine receptor-G protein coupling in bovine brain membranes-effects of guanine nucleotides, salt, and solubilization. J. Neumchem 51, 1592–1598.
Sweeney, M. I. and Dolphin, A C. (1995) Adenosine A1 agonists and the Ca2+ channel agonist Bay K 8644 produce a synergistic stimulation of the GTPase activity of G0 in rat frontal cortical membranes. J Neumchem. 64, 2034–2042.
Tian, W.-T, Duzic, E, Lanier, S. M, and Deth, R C. (1994) Determinants of α2 adrenergic receptor activation of G proteins: evidence for a precoupled receptor/G protein state. Mol Pharmacol. 45, 524–531.
Traynor, J. R and Nahorski, S. R (1995) Modulation by μ-opioid agonists of guanosine-5′-O-(3-[35S]thio)triphosphate binding to membranes from human neuroblastoma SH-SY5Y cells Mol. Pharmacol. 47, 848–854
Trussell, L O and Jackson, M B. (1985) Adenosme-activated potassium conductance in cultured striatal neurons. Proc. Natl. Acad Sci USA 82, 4857–4861.
Trussell, J. O. and Jackson, M. B. (1987) Dependence of an adenosine-activated potassium current on a GTP-binding protein in mammalian central neurons. J Neurosci. 7, 3306–3316
Van Calker, D., Muller, M, and Hamprecht, B. (1978) Adenosine inhibits the accumulation of cyclic AMP in cultured brain cells Nature (Lond.) 276, 839–841
Van Calker,, Muller, M, and Hamprecht, B. (1979) Adenosine regulates via two different types of receptors, the accumulation of cyclic AMP in cultured bram cells. J Neurochem. 33, 999–1005.
Van Calker, D, Steber, R, Klotz, K-N., and Greil, W. (1991) Carbamazepine distinguishes between adenosine receptors that mediate different second messenger responses. Eur. J Pharmacol. (Mol. Pharm Section) 206, 285–290.
Van der Wenden, E. M, Hartog-Witte, H. R., Roelen, H. C. P. F., von Frijtag Drabbe Kunzel, J K., Pirovano, I M., Mathôt, R A A., Danhof, M, van Aerschot, A, Lidaks, M. J, Ijzerman, A P, and Soudijn, W (1995a) 8-Substituted adenosine and theophylline 7-riboside analogues as potential partial agonists for the adenosine A1 receptor. Eur. J. Pharmacol (Mol Pharm Section) 290, 189–199
Van der Wenden, E. M, von Frijtag, Drabbe Kunzel, J K., Mathôt, R A A., Danhof, M., Ijzerman, A. P, Soudijn, W (1995b) Ribose-modified adenosine analogues as potential partial agonists for the adenosine receptor. J. Med. Chem 38, 4000–4006
Van der Ploeg, I, Parkinson, F E., and Fredholm, B B (1992) Effect of pertussis toxin on radioligand binding to rat brain adenosine A1 receptors. J Neurochem. 58, 1221–1229
Von Lubitz, D K., Lin, R. C, Popik, P., Carter, M F., and Jacobson, K A. (ai]1994) Adenosine A3 receptor and cerebral ischemia Eur J. Pharmacol. 263, 59–67
Von Lubitz, D K., Carter, M F., Deutsch, S. I., Lin, R. C, Mastropaolo, J, Meshulam, Y., and Jacobson, K A. (1995) The effects of adenosine A3 receptor stimulation on seizures in mice. Eur. J Pharmacol 275, 23–29
Waelbroeck, M., Robberecht, P, Chatelain, P, and Christophe, J. (1982) Rat cardiac muscarinic receptors I Effects of guanine nucleotides on high-and low-affinity binding sites Mol. Pharmacol. 21, 581–588.
Weir, R. L., Anderson, S. M, and Daly, J W (1990) Inhibition of N6-[3H]cyclohexyladenosine binding by carbamazepine. Epilepsia 31, 503–512
Wieland, T., Kreiss, J., Gierschik, P., and Jakobs, K H. (1992) Role of GDP in formyl-peptide-receptor-induced activation of guanine-nucleotide-binding proteins in membranes of HL 60 cells. Eur. J Biochem 205, 1201–1206
Yeung, S-M H. and Green, R D (1983) Agonist and antagonist affinities for inhibitory adenosine receptors are reciprocally affected by 5′-guanylylimidodiphosphate or N-ethylmaleimide. J Biol Chem 258, 2334–2339
Zhou, Q.-Y., Li, C, Olah, M. E., Johnson, R. A., Stiles, G. L., and Civelli, O (1992) Molecular cloning and characterization of an adenosine receptor-the A3 adenosine receptor Proc Natl. Acad Sci. USA 89, 7432–7436
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Lorenzen, A. (1997). Determination of Adenosine Receptor-G Protein Coupling. In: Mishra, R.K., Baker, G.B., Boulton, A.A. (eds) G Protein Methods and Protocols. Neuromethods, vol 31. Humana Press. https://doi.org/10.1385/0-89603-490-9:327
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