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Abstract

Adenosine receptors are members of the superfamily of receptors having seven trans-membrane domains and coupled to guanyl nucleotide-binding protein (G proteins). The A1, A2a, A2d, and A3 adenosine receptors have been cloned from several species, including in each case rat, dog, mouse, and human. The A1 and A3 receptors couple via G proteins to adenylate cyclase (inhibition), phospholipase C (activation), and, in the case of A1receptors, to potassium channels (activation) and calcium channels (inhibition). The A2a and A2b receptors couple via G proteins to adenylate cyclase (activation). A putative A4 receptor has not been cloned and will not be included in the present overview.

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References

  1. Jacobson KA, van Galen PJM, Williams M (1992) Adenosine receptors: Pharmacology, structure-activity relationships, and therapeutic potential. J Med Chem 35:407–422.

    Article  PubMed  CAS  Google Scholar 

  2. van Galen PJM, Stiles GL, Michaels G, Jacobson KA (1992) Adenosine A1 and A2 receptors: Structure-function relationships. Med Res Rev 12:423–471.

    Article  PubMed  Google Scholar 

  3. Jacobson KA, Daly JW (1991) Purine functionalized congeners as molecular probes for adenosine receptors. Nucleosides Nucleotides 10:1029–1038.

    Article  CAS  Google Scholar 

  4. Jacobson KA, Nikodijević O, Ji X-D, Berkich DA, Eveleth D, Dean PL, Hiramatsu K-I, Kassell NF, van Galen PJM, Lee KS, Bartus RT, Daly JW, Lalloue KF, Maillard M (1992)Synthesis and biological activity of N6-(psulfophenyl)alkyl and N6-sulfoalkyl derivatives of adenosine: Water-soluble and peripherally selective adenosine agonists. J Med Chem 35: 4143–4149.

    Article  PubMed  CAS  Google Scholar 

  5. Patel A, Craig RH, Daluge SM, Linden J (1988) 125I-BW-A844U, an antagonist radio-ligand with high affinity and selectivity for adenosine A1 receptors and 125I-azido-BWA844U, a photoaffinity label. Mol Pharmacol 33:585–591.

    PubMed  CAS  Google Scholar 

  6. Suzuki F, Shimada J, Nonaka H, Ishii A, Shiozaki S, Ichikawa S, Ono E (1992) 7,8-Dihydro-8-ethyl-2-(3-noradamantyl)-4-propyl-1H-imidazo[2,1-i]purin-5(4H)-one: A potent and water-soluble adenosine A1 antagonist. J Med Chem 35:3578–3581.

    Article  PubMed  CAS  Google Scholar 

  7. Suzuki F, Shimada J, Shiozaki S, Ichikawa S, Ishii A, Nakamura J, Nonaka H, Kobayashi H, Fuse E (1993) Adenosine A1 antagonists. 3. Structure-activity relationships on amelioration against scopolamine or N6-((R)-phenylisopropyl)-adenosine-induced cognitive dis-turbance. J Med Chem 36:2508–2518.

    Article  PubMed  CAS  Google Scholar 

  8. Cristalli G, Eleuteri A, Vittori S, Velpini R, Lohse MJ, Klotz K-L (1992) 2-Alkynyl derivatives of adenosine and adenosine-5’-Nethyluronamide as selective agonists at A125 adenosine receptors. J Med Chem 35:2363–2368.

    Article  PubMed  CAS  Google Scholar 

  9. Homma H, Watanabe Y, Abiru T, Murayama T, Nomura Y, Matsuda A (1992) Nucleosides and nucleotides 112. 2-(1-hexyn-l-yl)adenosine5’-uronamides: A new entry of selective A2 adenosine receptor agonists with potent antihypertensive activity. J Med Chem 35: 2881–2890.

    Article  PubMed  CAS  Google Scholar 

  10. Nikodijević O, Daly JW, Jacobson KA (1990) Characterization of the locomotor depression produced by an A2-selective adenosine agonist. FEBS Lett 261:67–70.

    Article  PubMed  Google Scholar 

  11. Bridges AJ, Bruns RF, Ortwine DF, Priebe SR, Szotek DL, Trivedi BK (1988)N6-[2-(3,5dimethoxy-phenyl)-2-(2-methylphenyl)ethyl] adenosine and its uronamide derivatives. Novel adenosine agonists with both high affinity and high selectivity for the adenosine A2 receptor. J Med Chem 31:1282–1285.

    Article  PubMed  CAS  Google Scholar 

  12. Shimada J, Suzuki F, Nonaka H, Ishii A, Ichikawa S (1992) (E)-1,3-dialkyl-7-methyl-8(3,4,5-trimethoxystyryl) xanthines: Potent and selective adenosine A2 antagonists. J Med Chem 35:2342–2345.

    Article  PubMed  CAS  Google Scholar 

  13. Jacobson KA, Gallo-Rodriquez C, Melman N,Fisher B, Maillard M, van Bergen A, van Galen PJM, Karton Y (1993) Structure-activity relationships of 8-styrylxanthines as A2-selective adenosine antagonists. J Med Chem 36:1333–1342.

    Article  PubMed  CAS  Google Scholar 

  14. Ukena D, Jacobson KA, Kirk KL, Daly JW (1986) A [3H]amine congener of 1,3-dipropyl8-phenylxanthine: A new radioligand for A2 adenosine receptors of human platelets. FEBS 199:269–274.

    Article  CAS  Google Scholar 

  15. Ji X-D, Stiles GL, Jacobson KA (1991) [3H]XAC (xanthine amine congener) is a radio-ligand for A2-adenosine receptors in rabbit striatum. Neurochem Int 18:207–213.

    Article  PubMed  CAS  Google Scholar 

  16. Bruns RF, Fergus JH, Badger EW, Bristol JA, Santay LA, Hays JJ (1987) PD 115, 199: An antagonist ligand for adenosine A2 receptors. Naunyn Schmiedebergs Arch. Pharmacol 335: 64–69.

    CAS  Google Scholar 

  17. Jarvis MF, Williams M, Do UH, Sills MA (1991) Characterization of the binding of a novel nonxanthine adenosine antagonist radioligand, [3H]CGS 15943, to multiple affinity states of the adenosine A1 receptor in the rat cortex. Mol Pharmacol 39:49–54.

    PubMed  CAS  Google Scholar 

  18. Nikodijevic O, Sarges R, Daly JW, Jacobson KA (1991) Behavioral effects of A1 and A2-selective adenosine agonists and antagonists: Evidence for synergism and antagonism. J Pharmacol Exp Ther 259:286–294.

    PubMed  CAS  Google Scholar 

  19. Bruns RF (1980) Adenosine receptor activation in human fibroblasts: Nucleoside agonists and antagonists. Can J Physiol Pharmacol 58:673–691.

    Article  PubMed  CAS  Google Scholar 

  20. Bruns RF (1981) Adenosine antagonism by purines, pteridines and benzopteridines in human fibroblasts. Biochem Pharmacol 30:325–333.

    Article  PubMed  CAS  Google Scholar 

  21. Brackett LE, Daly JW (1994) Functional characterization of the A2b adenosine receptor in NIH 3T3 fibroblasts Biochem Pharmacol 47: 801–814.

    Article  PubMed  CAS  Google Scholar 

  22. Bruns RF, Lu GH, Pugsley TA (1986) Characterization of the A2 adenosine receptor labeled by [3H]NECA in rat striatal membranes. Mol Pharmacol 29:331–346.

    PubMed  CAS  Google Scholar 

  23. Zhou Q-Y, Li C, Olah ME, Johnson RA, Stiles GL, Civelli O (1992) Molecular cloning and characterization of an adenosine receptor: The A3 adenosine receptor. Proc Natl Acad Sci USA 89:7432–7436.

    Article  PubMed  CAS  Google Scholar 

  24. Linden J, Taylor HE, Robeva AS, Tucker AL, Stehle JH, Rivkees SA, Fink JS, Reppert SM (1993) Molecular cloning and functional expression of a sheep A3 adenosine receptor with widespread tissue distribution. Mol Pharmacol 44:524–532.

    PubMed  CAS  Google Scholar 

  25. Salvatore CA, Jacobson MA, Taylor HE, Linden J, Johnson RG (1993) Molecular cloning and characterization of the human A3 adenosine receptor. Proc Natl Acad Sci USA 90:10365–10369.

    Article  PubMed  CAS  Google Scholar 

  26. Gallo-Rodriguez C, Ji X, Melman N, Siegman BD, Sanders LH, Orlina J, Fischer B, Pu Q, Olah ME, van Galen PJM, Stiles GL, Jacobson KA (1994) Structure-activity relationships of N6-benzyladenosine-5’-uronamides as A3- selective adenosine agonists. J Med Chem 37: 636–646.

    Article  PubMed  CAS  Google Scholar 

  27. Ji X-D, von Lubitz D, Olah ME, Stiles GL, Jacobson KA (1994) Species differences in ligand affinity at central A3-adenosine receptors Drug Dev Res, 33:51–59.

    Article  CAS  Google Scholar 

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Daly, J.W., Jacobson, K.A. (1995). Adenosine Receptors:Selective Agonists and Antagonists. In: Belardinelli, L., Pelleg, A. (eds) Adenosine and Adenine Nucleotides: From Molecular Biology to Integrative Physiology. Springer, Boston, MA. https://doi.org/10.1007/978-1-4615-2011-5_19

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  • DOI: https://doi.org/10.1007/978-1-4615-2011-5_19

  • Publisher Name: Springer, Boston, MA

  • Print ISBN: 978-1-4613-5831-2

  • Online ISBN: 978-1-4615-2011-5

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