Adenosine receptors as therapeutic targets

Nature Reviews Drug Discovery

Volumn 5, Issue 3, 2006, Pages 247-264

  Jacobson, Kenneth A ^a   Gao, Zhan Guo ^a  

^a NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 (2 HYDROXYETHYL) 1 [3 (2 PHENYLPYRAZOLO[1,5 A]PYRIDIN 3 YL)ACRYLOYL]PIPERIDINE; 2 [4 (2 CARBOXYETHYL)PHENETHYLAMINO]ADENOSINE 5' (N ETHYLCARBOXAMIDE); 4 [2 [7 AMINO 2 (2 FURYL) 1,2,4 TRIAZOLO[2,3 A][1,3,5]TRIAZIN 5 YLAMINO]ETHYL]PHENOL; 4 [7 [[1 [(3 CHLORO 2 THIENYL)METHYL]PROPYL]AMINO] 3H IMIDAZO[4,5 B]PYRIDIN 3 YL] N ETHYL 2,3 DIHYDROXYCYCLOPENTANECARBOXAMIDE; 5 AMINO 2 (2 FURYL) 7 (2 PHENYLETHYL)PYRAZOLO[4,3 E][1,2,4]TRIAZOLO[1,5 C]PYRIMIDINE; 6 N (2 HYDROXYCYCLOPENTYL)ADENOSINE; 6 N [2 (3,5 DIMETHOXYPHENYL) 2 (2 METHYLPHENYL)ETHYL]ADENOSINE; 6 N CYCLOHEXYL 2' O METHYLADENOSINE; 8 (2 NOR 1 ADAMANTYL) 1,3 DIPROPYLXANTHINE; 9 METHYL 6 N (2 NORBORNYL)ADENINE; ADENOSINE; ADENOSINE 5' (N ETHYLCARBOXAMIDE); ADENOSINE RECEPTOR; ADENOSINE RECEPTOR BLOCKING AGENT; ADENOSINE RECEPTOR STIMULATING AGENT; ADENYLATE CYCLASE; BINODENOSON; CV 3146; CVT 2759; GR 56072; ISTRADEFYLLINE; MITOGEN ACTIVATED PROTEIN KINASE; MRS 1292; N (4 CYANOPHENYL) 2 [4 (2,3,6,7 TETRAHYDRO 2,6 DIOXO 1,3 DIPROPYL 1H PURIN 8 YL)PHENOXY]ACETAMIDE; NAXIFYLLINE; NNC 210136; OT 7999; PSB 11; REGADENOSON; RG 14202; SELODENOSON; TECADENOSON; UNCLASSIFIED DRUG;

BINDING AFFINITY; CLINICAL TRIAL; CORONARY ARTERY CONSTRICTION; DRUG RECEPTOR BINDING; DRUG STRUCTURE; DRUG TARGETING; ENZYME ACTIVITY; GLAUCOMA; HEADACHE; HEART ATRIUM FIBRILLATION; HEART MUSCLE ISCHEMIA; HUMAN; HYPOTENSION; MOLECULAR MECHANICS; NEPHROTOXICITY; NONHUMAN; PARKINSON DISEASE; PAROXYSMAL SUPRAVENTRICULAR TACHYCARDIA; PRIORITY JOURNAL; REGULATORY MECHANISM; RENAL DIABETES; REVIEW; STRUCTURE ACTIVITY RELATION;

ANIMALS; DISEASE; DRUG THERAPY; HUMANS; LIGANDS; MOLECULAR STRUCTURE; RECEPTORS, PURINERGIC P1; SIGNAL TRANSDUCTION; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 33644770260     PISSN: 14741776     EISSN: 14741784     Source Type: Journal    
DOI: 10.1038/nrd1983     Document Type: Review

References (209)

1. Fredholm, B. B., IJzerman, A. P., Jacobson, K. A., Klotz, K. N. & Linden, J. International Union of Pharmacology. XXV. Nomenclature and classification of adenosine receptors. Pharmacol. Rev. 53, 527-552 (2001).
2. Linden, J. Adenosine in tissue protection and tissue regeneration. Mol. Pharmacol. 67, 1385-1387 (2005).
3. McGaraughty, S., Cowart, M., Jarvis, M. F. & Berman, R. F. Anticonvulsant and antinociceptive actions of novel adenosine kinase inhibitors. Curr. Top. Med. Chem. 5, 43-58 (2005).
4. Zimmermann, H. Extracellular metabolism of ATP and other nucleotides. Naunyn Schmiedebergs Arch. Pharmacol. 362, 299-309 (2000).
5. Pascual, O. et al. Astrocytic purinergic signalling coordinates synaptic networks. Science 310, 113-116 (2005).
6. Parkinson, F. E., Xiong, W. & Zamzow, C. R. Astrocytes and neurons: different roles in regulating adenosine levels. Neurol. Res. 27, 153-160 (2005).
7. Gao, Z. G., Kim, S. K., IJzerman, A. P. & Jacobson, K.A. Allosteric modulation of the adenosine family of receptors. Mini Rev. Med. Chem. 5, 545-553 (2005).
8. van Calker, D., Muller, M. & Hamprecht, B. Adenosine regulates via two different types of receptors, the accumulation of cyclic AMP in cultured brain cells. J. Neurochem. 33, 999-1005 (1979).
9. Londos, C., Cooper, D. M. & Wolff, J. Subclasses of external adenosine receptors. Proc. Natl Acad. Sci. USA 77, 2551-2554 (1980).
10. Tawfik, H. E., Schnermann, J., Oldenburg, P. J. & Mustafa, S. J. Role of A1 adenosine receptors in the regulation of vascular tone. Am. J. Physiol. Heart Circ. Physiol. 288, H1411-H1416 (2005).
11. Rogel, A., Bromberg, Y., Sperling, O. & Zoref-Shani, E. Phospholipase C is involved in the adenosine-activated signal transduction pathway conferring protection against iodoacetic acid-induced injury in primary rat neuronal cultures. Neurosci. Lett. 373, 218-221 (2005).
12. Belardinelli, L., Shryock, J. C., Song, Y., Wang, D. & Srinivas, M. Ionic basis of the electrophysiological actions of adenosine on cardiomyocytes. FASEB J. 9, 359-365 (1995).
13. Reid, E. A. et al. In vivo adenosine receptor preconditioning reduces myocardial infarct size via subcellular ERK signalling. Am. J. Physiol. Heart Circ. Physiol. 288, H2253-H2259 (2005).
14. olf in rat striatum. Mol. Pharmacol. 58, 771-777 (2000).
15. 2A receptors triggers both phospholipase C and adenylate cyclase pathways in rat tail artery. Cardiovasc. Res. 63, 739-746 (2004).
16. 16 couple a wide variety of receptors to phospholipase C. J. Biol. Chem. 270, 15175-15180 (1995).
17. Daly, J. W., Butts-Lamb, P. & Padgett, W. Subclasses of adenosine receptors in the central nervous system: Interaction with caffeine and related methylxanthines. Cell. Mol. Neurobiol. 3, 69-80 (1983).
18. 2B adenosine receptor in NIH 3T3 fibroblasts. Biochem. Pharmacol. 47, 801-814 (1994).
19. 2B-receptor-mediated cyclic AMP accumulation in primary rat astrocytes. Br. J. Pharmacol. 111, 191-198 (1994).
20. 2B receptors evoke interleukin-8 secretion in human mast cells. An enprofylline-sensitive mechanism with implications for asthma. J. Clin. Invest. 96, 1979-1986 (1995).
21. 2 receptors stimulate mitogen-activated protein kinase in human embryonic kidney-293 cells. Cross-talk between cyclic AMP and protein kinase C pathways. J. Biol. Chem. 274, 5972-5980 (1999).
22. q in human embryonic kidney 293 cells and HMC-1 mast cells. Mol. Pharmacol. 56, 705-713 (1999).
23. 2B adenosine receptor mediates human chorionic vasoconstriction and signals through the arachidonic acid cascade. Am. J. Physiol. Heart Circ. Physiol. 288, H2439-H2449 (2005).
24. 3 adenosine receptor. Proc. Natl Acad. Sci. USA 89, 7432-7436 (1992).
25. 3 receptors in rat brain. Mol. Pharmacol. 48, 1038-1045 (1995).
26. 3 receptors in regulation of cardiomyocyte homeostasis after mitochondrial respiratory chain injury. Am. J. Physiol. Heart Circ. Physiol. 288, H2792-H2801 (2005).
27. 3 adenosine receptors in CHO cells. Biochem. Pharmacol. 64, 61-65 (2002).
28. 3 adenosine receptor in monocyte-derived dendritic cells and recombinant cells. Mol. Pharmacol. 63, 342-350 (2003).
29. 3 adenosine receptor in cultured newborn rat cardiac myocytes. Cell Calcium 36, 387-396 (2004).
30. ATP channel activation. Cardiovasc. Res. 40, 138-145 (1998).
31. Mozzicato, S., Joshi, B. V., Jacobson, K. A. & Liang, B. T. Role of direct RhoA-phospholipase D1 interaction in mediating adenosine-induced protection from cardiac ischemia. FASEB J. 18, 406-408 (2004).
32. Fishman, P. et al. Evidence for involvement of Wnt signalling pathway in IB-MECA mediated suppression of melanoma cells. Oncogene 21, 4060-4064 (2002).
33. 3 receptor expressed in Chinese hamster ovary cells to the extracellular signal-regulated kinase 1/2. Mol. Pharmacol. 62, 1137-1146 (2002).
34. Schulte, G. & Fredholm, B. B. Signalling from adenosine receptors to mitogen-activated protein kinases. Cell Signal. 15, 813-827 (2003).
35. 3 adenosine receptor activation inhibits cell proliferation via phosphatidylinositol 3-kinase (PI3K)/AKT-dependent inhibition of the extracellular signal-regulated kinase (ERK)1/2 phosphorylation in A375 human melanoma cells. J. Biol. Chem. 280, 19516-19526 (2005).
36. Olah, M. E. & Stiles, G. L. The role of receptor structure in determining adenosine receptor activity. Pharmacol. Ther. 85, 55-75 (2000).
37. Yan, L., Burbiel, J. C., Maass, A. & Müller, C. E. Adenosine receptor agonists: From basic medicinal chemistry to clinical development. Expert Opin. Emerging Drugs 8, 537-576 (2003).
38. 2A agonist and antagonist. J. Med. Chem. 46, 4847-4859 (2003).
39. 3 adenosine receptor agonists. J. Med. Chem. 48,1745-1758 (2005).
40. Moro, S., Gao, Z. G., Jacobson, K. A. & Spalluto, G. Progress in pursuit of therapeutic adenosine receptor antagonists. Med. Res. Rev. 26, 131-159 (2006).
41. 3 adenosine receptor antagonists. J. Med. Chem. 48, 5698-5704 (2005).
42. 3 adenosine receptor activation: Nucleoside ligands at the agonist/antagonist boundary. J. Med. Chem. 45, 4471-4484 (2002).
43. 3 adenosine receptors, Biochem. Pharmacol. 65, 1675-1684 (2003).
44. 1 adenosine receptors. J. Pharmacol. Exp. Ther. 276, 490-499 (1996).
45. 2A receptor agonists. J. Med. Chem. 44, 531-539 (2001).
46. 2 receptor. J. Med. Chem. 31, 1282-1285 (1988).
47. 2A adenosine receptor. Mol. Pharmacol. 48, 970-974 (1996).
48. 2A adenosine receptor antagonists. J. Med. Chem. 41, 2126-2133 (1998).
49. 2B adenosine receptors. Drug Des. Discov. 16, 217-226 (1999).
50. 2A receptor selective antagonist KW6002: Research and development toward a novel nondopaminergic therapy for Parkinson's disease. Neurology 61, S97-S100 (2003).
51. 2B adenosine receptors. Curr. Top. Med. Chem. 3, 427-443 (2003).
52. 2B receptor with an improved selectivity profile compared to the reference agonist N-ethylcarboxamidoadenosine. J. Med. Chem. 47, 3707-3709 (2004).
53. 2B adenosine receptors. Biochem. Pharmacol. 61, 657-663 (2001).
54. 3H]MRE 2029-F20. Mol. Pharmacol. 67, 2137-2147 (2005).
55. 2B receptors. Biochem. Pharmacol. 68, 305-312 (2004).
56. 3 adenosine receptors: Novel ligands and paradoxical effects. Trends Pharmacol. Sci. 19, 184-191 (1998).
57. 3 adenosine receptor. Mol. Pharmacol. 45, 978-982 (1994).
58. 3 adenosine receptor. J. Med. Chem. 46, 3775-3777 (2003).
59. 3 receptors: Pharmacological properties, species differences and receptor functions. Trends Pharmacol. Sci. 15, 298-306 (1994).
60. 3 adenosine-receptor antagonist MRS 1292 inhibits adenosine-triggered human nonpigmented ciliary epithelial cell fluid release and reduces mouse intraocular pressure. Curr. Eye Res. 30, 747-754 (2005).
61. 3 adenosine receptors. Bioorg. Med. Chem. Lett. 12, 501-503 (2002).
62. 3 adenosine receptor antagonists. J. Med. Chem.48, 4910-4918 (2005).
63. 1 adenosine receptor agonists from a molecular perspective and their potential use as chronic ventricular rate control agents during atrial fibrillation (AF). Curr. Top. Med. Chem. 4, 839-854 (2004).
64. 1 adenosine receptor agonist, antagonizes catecholamine-induced lipolysis without cardiovascular effects in awake rats. J. Pharmacol. Exp. Ther. 305, 225-231 (2003).
65. Bayes, M., Rabasseda, X. & Prous, J. R. Gateways to clinical trials. Methods Find. Exp. Clin. Pharmacol. 25, 831-855 (2003).
66. Ellenbogen, K. A. et al. Trial to evaluate the management of paroxysmal supraventricular tachycardia during an electrophysiology study with tecadenoson. Circulation 111, 3202-3208 (2005).
67. 1 receptor agonist. Drug Dev. Res. 34, 276-288 (1995).
68. 6-(3-iodobenzyl) adenosine-5′-N-methyluronamide protects against myocardial stunning and infarction without hemodynamic changes in conscious rabbits. Circ. Res. 80, 800-809 (1997).
69. 2A subtype receptor agonists. Br. J. Pharmacol. 144, 642-650 (2005).
70. 1 receptors are necessary for protection of the murine heart by remote, delayed adaptation to ischaemia. Acta Physiol. Scand. 182, 133-143 (2004).
71. 1 adenosine receptor overexpression increases myocardial resistance to ischemia. Proc. Natl Acad. Sci. USA 94, 6541-6546 (1997).
72. 1 adenosine receptors. J. Mol. Cell. Cardiol. 30, 187-193 (1998).
73. 1-adenosine receptor protects intact mice against myocardial infarction. Am. J. Physiol. Heart Circ. Physiol. 282, H949-H955 (2002).
74. 1-adenosine receptors. Am. J. Physiol. Heart Circ. Physiol. 279, H1690-H1697 (2000).
75. 3 adenosine receptors improves tolerance to ischemia-reperfusion injury in mouse myocardium. Am. J. Physiol. Heart Circ. Physiol. 281, H1751-H1758 (2001).
76. 6-cyclopentyladenosine (CPA) decisive for its therapeutic efficacy in sarin poisoning. Arch. Toxicol. 78, 34-39 (2004).
77. 1 adenosine receptor limits myocardial ischemic tolerance. Circ. Res. 96, 363-367 (2005).
78. 3 receptors reduce ischemic myocardial injury. Am. J. Physiol. Heart Circ. Physiol. 285, H2780-H2787 (2003).
79. 3 adenosine receptors decreases heart rate, preserves energetics, and protects ischemic hearts. Am. J. Physiol. Heart Circ. Physiol. 283, H1562-H1568 (2002).
80. 3 adenosine receptor. Circ. Res. 91, 165-172 (2002).
81. 3 adenosine receptor confers resistance to myocardial ischemic injury and does not prevent early preconditioning. J. Mol. Cell Cardiol. 33, 825-830 (2001).
82. 3 adenosine receptor activation and gene knock-out in ischemic-reperfused mouse heart. Cardiovasc. Res. 53, 147-155 (2002).
83. 2A-adenosine receptor activation is due primarily to its actions on lymphocytes. Circulation 111, 2190-2197 (2005).
84. Gerlai, R. Gene-targeting studies of mammalian behavior: Is it the mutation or the background genotype? Trends Neurosci. 19, 177-181 (1996).
85. 3 receptor activation. Eur. J. Pharmacol. 441, 165-172 (2002).
86. 3 receptors mediates preconditioning of isolated cardiac myocytes. Eur. J. Pharmacol. 320, 241-248 (1997).
87. 3 adenosine receptor protects against doxorubicin-induced cardiotoxicity. J. Mol. Cell. Cardiol. 33, 1249-1261 (2001).
88. 2A receptors: Functional and biochemical aspects. Circulation 102, 285-289 (2000).
89. 2A agonist for pharmacologic stress single-photon emission computed tomography myocardial perfusion imaging. J. Am. Coll. Cardiol. 46, 2069-2075 (2005).
90. Barrett, R. J., Lamson, M. J., Johnson, J. & Smith, W. B. Pharmacokinetics and safety of binodenoson after intravenous dose escalation in healthy volunteers. J. Nucl. Cardiol. 12, 166-171 (2005).
91. 1 subtype. J. Pharmacol. Exp. Ther. 267, 1100-1104 (1993).
92. Szentmiklosi, A. J. et al. Adenosine receptors mediate both contractile and relaxant effects of adenosine in main pulmonary artery of guinea pigs. Naunyn. Schmiedebergs Arch. Pharmacol. 351, 417-425 (1995).
93. 2B receptors. J. Exp. Med. 198, 783-796 (2003).
94. 2B receptors mediate antimitogenesis in vascular smooth muscle cells. Hypertension 35, 267-272 (2000).
95. 2B receptors in cardiac fibroblasts. Am. J. Physiol. Heart Circ. Physiol. 287, H2478-H2486 (2004).
96. 2B activation. J. Surg. Res. 84, 57-63 (1999).
97. 2B angiogenic phenotype. Hypertension 44, 649-654 (2004).
98. 3 receptors on mast cells. J. Clin. Invest. 105, 361-367 (2000).
99. 3 adenosine receptor in determining tissue levels of cAMP and blood pressure: Studies in knock-out mice. Biochim. Biophys. Acta 1500, 280-290 (2000).
100. 3 receptors augments adenosine-induced coronary flow in isolated mouse heart. Am. J. Physiol. Heart Circ. Physiol. 282, H2183-H2189 (2002).
101. 3 adenosine receptor deficiency does not influence atherogenesis. J. Cell Biochem. 92, 1034-1043 (2004).
102. 1 receptors in the discriminative-stimulus effects of caffeine in rats. Psychopharmacology (Berl.) 179, 576-586 (2005).
103. 2A receptor. Nature 388, 674-678 (1997).
104. Fredholm, B. B., Chen, J. F., Masino, S. A. & Vaugeois, J. M. Actions of adenosine at its receptors in the CNS: Insights from knockouts and drugs. Annu. Rev. Pharmacol. Toxicol. 45, 385-412 (2005).
105. 1, receptors mediate the arousal effect of caffeine. Nature Neurosci. 8, 858-859 (2005).
106. 2A receptor in sleep promotion. Eur. J. Pharmacol. 351, 155-162 (1998).
107. 1 receptors. J. Pharmacol. Sci. 96, 42-52 (2004).
108. Sawynok, J. Adenosine receptor activation and nociception. Eur. J. Pharmacol. 347, 1-11 (1998).
109. 1 receptor. Proc. Natl. Acad. Sci. USA 98, 9407-9412 (2001).
110. 1 receptor. Pain 113, 395-404 (2005).
111. Gordh, T., Karlsten, R. & Kristensen, J. Intervention with spinal NMDA, adenosine, and NO systems for pain modulation. Ann. Med. 27, 229-234 (1995).
112. 1 receptor agonist GR79236 on trigeminal nociception with blink reflex recordings in healthy human subjects. Cephalalgia 23, 287-292 (2003).
113. Zambrowicz, B. P., Turner, C. A. & Sands, A. T. Predicting drug efficacy: Knockouts model pipeline drugs of the pharmaceutical industry. Curr. Opin. Pharmacol. 3, 563-570 (2003).
114. Li, X., Conklin, D., Pan, H. L. & Eisenach, J. C. Allosteric adenosine receptor modulation reduces hypersensitivity following peripheral inflammation by a central mechanism. J. Pharmacol. Exp. Ther. 305, 950-955 (2003).
115. Ferre, S., von Euler, G., Johansson, B., Fredholm, B. B. & Fuxe, K. 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 (1991).
116. 2 receptors. J. Biol. Chem. 277, 18091-18097 (2002).
117. 2A receptors. Prog. Neurobiol. 59, 355-396 (1999).
118. 2A receptor antagonist. J. Neurosci. 20, 5848-5852 (2000).
119. 2A receptor antagonists in Parkinson's disease. Pharmacol. Ther. 105, 267-310 (2005).
120. Ross, G. W. et al. Association of coffee and caffeine intake with the risk of Parkinson disease. JAMA 283, 2674-2679 (2000).
121. Ascherio, A. et al. Prospective study of caffeine consumption and risk of Parkinson's disease in men and women. Ann. Neurol. 50, 56-63 (2001).
122. 2A receptor antagonist treatment of Parkinson's disease. Neurology 61, 293-296 (2003).
123. 2A receptor antagonist istradefylline in advanced PD. Neurology 61, 297-303 (2003).
124. 2A receptor antagonists for the treatment of Parkinson's disease. Neurology 61, S101-S106 (2003).
125. 2A antagonists. Bioorg. Med. Chem. Lett. 15, 1333-1336 (2005).
126. 2A receptor antagonists. J. Med. Chem. 47, 6218-6229 (2004).
127. 2A adenosine receptor deficiency attenuates brain injury induced by transient focal ischemia in mice. J. Neurosci. 19, 9192-9200 (1999).
128. 2A receptors by SCH 58261 results in neuroprotective effects in cerebral ischaemia in rats. Neuroreport 9, 3955-3959 (1998).
129. 2A antagonists. J. Neurosci. 23, 5361-5369 (2003).
130. 2A receptors in bone marrow cells reveals their significant contribution to the development of ischemic brain injury. Nature Med. 10, 1081-1087 (2004).
131. 2A knockout mice. Stroke 34, 739-744 (2003).
132. 2A receptor activation reduces proinflammatory events and decreases cell death following intracerebral hemorrhage. Ann. Neurol. 49, 727-735 (2001).
133. 2A receptor expression on motor neurons. Ann. Thorac. Surg. 74, 846-849 (2002).
134. von Lubitz, D. K. J. E. et al. Postischemic administration of adenosine amine congener (ADAC): Analysis of recovery in gerbils. Eur. J. Pharmacol. 316, 171-179 (1996).
135. 1 agonists with diminished hypotensive effects. J. Med. Chem. 42, 3463-3477 (1999).
136. 1 receptor gene does not alter neuronal damage following ischaemia in vivo or in vitro. Eur. J. Neurosci. 20, 1197-1204 (2004).
137. 1 adenosine receptors mediate hypoxia-induced ventriculomegaly. Proc. Natl Acad. Sci. USA 100, 11718-11722 (2003).
138. Stevens, B., Porta, S., Haak, L. L., Gallo, V. & Fields, R. D. Adenosine: A neuron-glial transmitter promoting myelination in the CNS in response to action potentials. Neuron 36, 855-868 (2002).
139. 3 adenosine receptor with widespread tissue distribution. Mol. Pharmacol. 44, 524-532 (1993).
140. Dixon, A. K., Gubitz, A. K., Sirinathsinghji, D. J., Richardson, P. J. & Freeman, T. C. Tissue distribution of adenosine receptor mRNAs in the rat. Br. J. Pharmacol. 118, 1461-1468 (1996).
141. 3 adenosine receptors in smooth, cardiac, and skeletal muscle is lethal to embryos. Microvasc. Res. 63, 61-69 (2002).
142. 3-adenosine receptors. Mediation of behavioral depressant effects. FEBS Lett. 336, 57-60 (1993).
143. 3 receptor stimulation and cerebral ischemia. Eur. J. Pharmacol. 263, 59-67 (1994).
144. Porkka-Heiskanen, T. et al. Adenosine: A mediator of the sleep-inducing effects of prolonged wakefulness. Science 276, 1265-1268 (1997).
145. Porkka-Heiskanen, T., Alanko, L., Kalinchuk, A. & Stenberg, D. Adenosine and sleep. Sleep Med. Rev. 6, 321-332 (2002).
146. 1 receptor. J. Sleep Res. 12, 283-290 (2003).
147. 2A receptor-deficient mice. Neurology 61, S94-S96 (2003).
148. Basheer, R., Strecker, R. E., Thakkar, M. M. & McCarley, R. W. Adenosine and sleep-wake regulation. Prog. Neurobiol. 73, 379-396 (2004).
149. 2 receptor-stimulated PKA signalling and regulate ethanol consumption. Cell 109, 733-743 (2002).
150. Mailliard, W. S. & Diamond, I. Recent advances in the neurobiology of alcoholism: The role of adenosine. Pharmacol. Ther. 101, 39-46 (2004).
151. 1 adenosine receptor density caused by glioma invasion. J. Nucl. Med. 46, 450-454 (2005).
152. 11C]SCH442416. Eur. J. Nucl. Med. Mol. Imaging 32, 405-413 (2005).
153. 2A receptor or its chronic blockade decrease ethanol withdrawal-induced seizures in mice. Neuropharmacology 40, 424-432 (2001).
154. 3 receptors. Am. J. Physiol. Renal Physiol. 278, F380-F387 (2000).
155. 1 receptor expression and protect renal proximal tubular epithelial cells against cisplatin-mediated apoptosis. J. Biol. Chem. 279, 43157-43167 (2004).
156. 1 receptor-deficient mice. Am. J. Physiol. Regul. Integr. Comp. Physiol. 281, R1362-R1367 (2001).
157. 1 receptors. Proc. Natl Acad. Sci. USA 98, 9983-9988 (2001).
158. 1 adenosine receptor knockout mice exhibit increased renal injury following ischemia and reperfusion. Am. J. Physiol. Renal Physiol. 286, F298-F306 (2004).
159. 1 receptor antagonist. J. Am. Soc. Nephrol. 10, 714-720 (1999).
160. 1 adenosine receptor antagonist, protects against the decline in renal function observed with diuretic therapy. Circulation 105, 1348-1353 (2002).
161. 1 adenosine receptor antagonists on infarct size and multiple cycle ischemic preconditioning in anesthetized dogs. J. Pharmacol. Exp. Ther. 308, 846-856 (2004).
162. 2A adenosine receptors on bone marrow-derived cells. J. Clin. Invest. 112, 883-891 (2003).
163. 2A adenosine receptor-mediated inhibition of renal injury and neutrophil adhesion. Am. J. Physiol. Renal Physiol. 279, F809-F818 (2000).
164. Zannikos, P. N. et al. Pharmacokinetics and safety of single intravenous infusions of the adenosine agonist, AMP 579, in patients with end-stage renal insufficiency. J. Clin. Pharmacol. 40, 745-751 (2000).
165. Vitzthum, H., Weiss, B., Bachleitner, W., Kramer, B. K. & Kurtz, A. Gene expression of adenosine receptors along the nephron. Kidney Int. 65, 1180-1190 (2004).
166. 2B adenosine receptor coupled to cyclic AMP generation in human embryonic kidney (HEK 293) cells. Br. J. Pharmacol. 122, 546-550 (1997).
167. 2B receptors. Hypertension 46, 628-634 (2005).
168. 3 adenosine receptor knockout mice are protected against ischemia- and myoglobinuria-induced renal failure. Am. J. Physiol. Renal Physiol. 284, F267-F273 (2003).
169. 1 adenosine receptor in adenosine-dependent pulmonary injury. J. Clin. Invest. 115, 35-43 (2005).
170. 2B receptor as a novel therapeutic target in asthma. Br. J. Pharmacol. 145, 1009-1015 (2005).
171. 3 adenosine receptor gene in mice and its effect on stimulated inflammatory cells. J. Biol. Chem. 275, 4429-4434 (2000).
172. Feoktistov, I. & Biaggioni, I. Role of adenosine in asthma. Drug Dev. Res. 39, 333-336 (1996).
173. 2B-mediated process involving Th2 cytokines IL-4 and IL-13 with implications for asthma. J. Immunol. 172, 7726-7733 (2004).
174. 2B receptor. Mol. Pharmacol. 52, 846-860 (1997).
175. 3 receptor antagonist with therapeutic potential. Bioorg. Med. Chem. Lett. 15, 3081-3085 (2005).
176. 2A receptor agonist, on allergic airways inflammation in the rat. Eur. J. Pharmacol. 438, 183-188 (2002).
177. 2A receptor agonists as inhibitors of cellular activation. Expert Opin. Ther. Pat. 10, 723-728 (2000).
178. 3 adenosine receptor provides lung protection against ischemia-reperfusion injury associated with reduction in apoptosis. Am. J. Transplant. 4, 1941-1948 (2004).
179. 2A receptors. Annu. Rev. Immunol. 22, 657-682 (2004).
180. 2A receptors directly inhibits IL-2 secretion in vitro and IL-2 driven expansion in vivo. Blood 105, 4707-4714 (2005).
181. 2A adenosine receptor induction inhibits IFN- production in murine CD4+ T cells. J. Immunol. 174, 1073-1080 (2005).
182. Ohta, A. & Sitkovsky, M. Role of G-protein-coupled adenosine receptors in downregulation of inflammation and protection from tissue damage. Nature 414, 916-920 (2001).
183. Kirkpatrick, P. Putting the brake on inflammation. Nature Rev. Drug Disc. 1, 99 (2002).
184. 3 receptors are required for inhibition of inflammation by methotrexate and its analog MX-68. Arthritis Rheum. 48, 240-247 (2003).
185. 2A adenosine receptors during reperfusion: Inhibition of chemokine induction. Am. J. Physiol. Gastrointest. Liver Physiol. 286, G285-G293 (2004).
186. 2A adenosine receptor activation improves survival in mouse models of endotoxemia and sepsis. J. Infect. Dis. 189, 1897-1904 (2004).
187. 2A adenosine receptor attenuates intestinal inflammation in animal models of inflammatory bowel disease. Gastroenterology 129, 26-33 (2005).
188. 2A adenosine receptor activation reduces skin pressure ulcer formation and inflammation. Am. J. Physiol. Heart Circ. Physiol. 281, H67-H74 (2001).
189. 2 (Gαs-linked) receptors. J. Exp. Med. 186, 1615-1620 (1997).
190. 3 adenosine receptor is the unique adenosine receptor which facilitates release of allergic mediators in mast cells. J. Biol. Chem. 268, 16887-16890 (1993).
191. Haskó, G. & Cronstein, B. N. Adenosine: An endogenous regulator of innate immunity. Trends Immunol. 25, 33-39 (2004).
192. 3 adenosine receptor agonists in murine autoimmune arthritis models. J. Rheumatol. 32, 469-476 (2005).
193. 1 adenosine receptor in adipose tissue protects mice from obesity-related insulin resistance. Diabetes Obes. Metab. 3, 360-366 (2001).
194. 2B receptor. J. Med. Chem. 44, 170-179 (2001).
195. 3 receptor agonists. Biochem. Biophys. Res. Commun. 219, 904-910 (1996).
196. Kim, S. G. et al. p53-Independent induction of Fas and apoptosis in leukemic cells by an adenosine derivative, Cl-IB-MECA. Biochem. Pharmacol. 63, 871-880 (2002).
197. 3 adenosine receptor activation triggers phosphorylation of protein kinase B and protects rat basophilic leukemia 2H3 mast cells from apoptosis. Mol. Pharmacol. 59, 76-82 (2001).
198. Neary, J. T., McCarthy, M., Kang, Y. & Zuniga, S. Mitogenic signalling from P1 and P2 purinergic receptors to mitogen-activated protein kinase in human fetal astrocyte cultures. Neurosci. Lett. 242, 159-162 (1998).
199. Merighi, S. et al. Adenosine receptors as mediators of both cell proliferation and cell death of cultured human melanoma cells. J. Invest. Dermatol. 119, 923-933 (2002).
200. 3 adenosine receptor as a target for cancer therapy. Anticancer Drugs 13, 437-443 (2002).
201. 3 adenosine receptor is highly expressed in tumor versus normal cells: Potential target for tumor growth inhibition. Clin. Cancer Res. 10, 4472-4479 (2004).
202. Lu, J., Pierron, A. & Ravid, K. An adenosine analogue, IB-MECA, down-regulates estrogen receptor alpha and suppresses human breast cancer cell proliferation. Cancer Res. 63, 6413-6423 (2003).
203. 3 adenosine receptors reduces mouse intraocular pressure. Invest. Ophthalmol. Vis. Sci. 43, 3021-3026 (2002).
204. 3 receptor ligands: New potential therapy for the treatment of glaucoma. Bioorg. Med. Chem. Lett. 14, 3775-3779 (2004).
205. 3 receptor with selectively enhanced affinity for amine-modified nucleosides, J. Med. Chem. 44, 4125-4136 (2001).
206. 2A adenosine receptor and its agonists. Chem. Biol. 12, 237-247 (2005).
207. Klotz, K. N. et al. Comparative pharmacology of human adenosine receptor subtypes - characterization of stably transfected receptors in CHO cells. Naunyn Schmiedebergs Arch. Pharmacol. 357, 1-9 (1998).
208. 2A receptor. Bioorg. Med. Chem. Lett. 12, 2935-2939 (2002).
209. 3 adenosine receptor (neoceptor) using tailored nucleoside agonists. J. Med. Chem. (in the press).