The world's first wiki where authorship really matters (Nature Genetics, 2008). Due credit and reputation for authors. Imagine a global collaborative knowledge base for original thoughts. Search thousands of articles and collaborate with scientists around the globe.

wikigene or wiki gene protein drug chemical gene disease author authorship tracking collaborative publishing evolutionary knowledge reputation system wiki2.0 global collaboration genes proteins drugs chemicals diseases compound
Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)



Gene Review

Adora1  -  adenosine A1 receptor

Mus musculus

Synonyms: A1-AR, A1AR, A1R, AA1R, AI848715, ...
Welcome! If you are familiar with the subject of this article, you can contribute to this open access knowledge base by deleting incorrect information, restructuring or completely rewriting any text. Read more.

Disease relevance of Adora1


Psychiatry related information on Adora1


High impact information on Adora1


Chemical compound and disease context of Adora1


Biological context of Adora1


Anatomical context of Adora1


Associations of Adora1 with chemical compounds

  • A1R activation with 2-chloro-N6-cyclopentyladenosine (CCPA) resulted in a 27% reduction in contractile response to the beta-adrenergic agonist isoproterenol (ISO) [24].
  • Pre-treatment with a selective A1AR agonist (50 nM CHA) failed to modify coronary dysfunction, whereas A1AR antagonism (200 nM DPCPX) worsened the effects of I/R (2-chloroadenosine pEC50=6.9+/-0.1) [25].
  • Thus, the inducible A1-AR transgenic mouse model provides novel insights into the role of adenosine signaling in heart failure and illustrates the potentially deleterious consequences of selective versus nonselective activation of adenosine-signaling pathways in the heart [2].
  • To evaluate the temporal relationship between AR signaling and cardiac remodeling, we studied the effects of controlled overexpression of the A1-AR using a cardiac-specific and tetracycline-transactivating factor-regulated promoter [2].
  • The stimulatory response to R-PIA was attenuated following blockade of ARs by 0.5 mM theophylline and 10 microM BW-A1433, but not by blockade of the A1AR with 100 nM xanthine amine congener [26].

Regulatory relationships of Adora1


Other interactions of Adora1

  • This study investigated the A1R and A2AR function in beta-adrenergic-stimulated, isolated wild-type and A2AR knockout murine hearts [24].
  • Despite the approximate doubling of distal fluid and Cl delivery, AQP1/A1AR-/- mice have a normal salt excretion, normal arterial blood pressure, and only a small increase in plasma renin concentration [18].
  • Allopurinol attenuated both the increase in A1AR expression and NF-kappaB activation produced by osmotic diuretics, indicating a role of adenosine metabolites in these processes [19].
  • In Ltk cells stably expressing A1 adenosine receptors and D1A dopamine receptors, pre-treatment of cells with R(-)-PIA, a full A1 receptor agonist, did not significantly inhibit the acute increase in cAMP levels induced by D1 receptor agonists, but blocked desensitization of D1A receptors [28].
  • This indicates that A1 receptor activation non-competitively inhibits effector mechanisms activated by beta-adrenoceptors (e.g. adenylate cyclase) and/or A1 receptors activate unrelated but opposing mechanisms [29].

Analytical, diagnostic and therapeutic context of Adora1

  • In anesthetized wild-type (A1AR+/+) and A1AR-deficient mice (A1AR-/-), glomerular filtration rate (GFR) and renal blood flow (RBF) were determined before and after reducing renal perfusion pressure through a suprarenal aortic clamp [30].
  • These findings were corroborated by Northern blot analysis which revealed A1-receptor mRNA to be exclusively expressed in the mature adipocytes, whereas A2-receptor mRNA gradually declined during the differentiation process except in 16-day post-confluent cells [31].
  • Male homozygous A1R KO mice, wild-type (WT) mice, and heterozygotes (HET) from a mixed 129/C57BL background were implanted during anesthesia with electrodes for electroencephalography (EEG) and electromyography (EMG) [32].
  • In vivo micropuncture experiments were performed under anesthesia in A1AR-deficient and wild-type littermate mice to study the effects of chronic absence of A1AR on fluid and Na(+) reabsorption along the nephron, as well as the functional consequences at the single-nephron level of the lack TGF [33].
  • In vivo, the induction of arterial hypertension by either acute (single subcutaneous injection) or chronic (osmotic minipump for 72 hours) application of phenylephrine significantly reduced plasma renin concentration (PRC) in wild-type mice to approximately 40% of control, whereas it did not significantly affect PRC in A1AR(-/-) mice [34].


  1. Effects of adenosine deaminase and A1 receptor deficiency in normoxic and ischaemic mouse hearts. Willems, L., Reichelt, M.E., Molina, J.G., Sun, C.X., Chunn, J.L., Ashton, K.J., Schnermann, J., Blackburn, M.R., Headrick, J.P. Cardiovasc. Res. (2006) [Pubmed]
  2. Regulated overexpression of the A1-adenosine receptor in mice results in adverse but reversible changes in cardiac morphology and function. Funakoshi, H., Chan, T.O., Good, J.C., Libonati, J.R., Piuhola, J., Chen, X., MacDonnell, S.M., Lee, L.L., Herrmann, D.E., Zhang, J., Martini, J., Palmer, T.M., Sanbe, A., Robbins, J., Houser, S.R., Koch, W.J., Feldman, A.M. Circulation (2006) [Pubmed]
  3. Effects of aging and ischemia on adenosine receptor transcription in mouse myocardium. Ashton, K.J., Nilsson, U., Willems, L., Holmgren, K., Headrick, J.P. Biochem. Biophys. Res. Commun. (2003) [Pubmed]
  4. Hyperalgesia, anxiety, and decreased hypoxic neuroprotection in mice lacking the adenosine A1 receptor. Johansson, B., Halldner, L., Dunwiddie, T.V., Masino, S.A., Poelchen, W., Giménez-Llort, L., Escorihuela, R.M., Fernández-Teruel, A., Wiesenfeld-Hallin, Z., Xu, X.J., Hårdemark, A., Betsholtz, C., Herlenius, E., Fredholm, B.B. Proc. Natl. Acad. Sci. U.S.A. (2001) [Pubmed]
  5. Adenosine A2A, but not A1, receptors mediate the arousal effect of caffeine. Huang, Z.L., Qu, W.M., Eguchi, N., Chen, J.F., Schwarzschild, M.A., Fredholm, B.B., Urade, Y., Hayaishi, O. Nat. Neurosci. (2005) [Pubmed]
  6. Cocaine-induced hyperactivity is more influenced by adenosine receptor agonists than amphetamine-induced hyperactivity. Poleszak, E., Malec, D. Polish journal of pharmacology. (2002) [Pubmed]
  7. Effects of N6-cyclohexyl adenosine (CHA) on isolation-induced aggression in male mice. Navarro, J.F., Romero, C., Maldonado, E. Methods and findings in experimental and clinical pharmacology. (2000) [Pubmed]
  8. Pharmacological characterization of FR194921, a new potent, selective, and orally active antagonist for central adenosine A1 receptors. Maemoto, T., Tada, M., Mihara, T., Ueyama, N., Matsuoka, H., Harada, K., Yamaji, T., Shirakawa, K., Kuroda, S., Akahane, A., Iwashita, A., Matsuoka, N., Mutoh, S. J. Pharmacol. Sci. (2004) [Pubmed]
  9. 2-Chloro-N6-cyclopentyladenosine enhances the anticonvulsant action of carbamazepine in the mouse maximal electroshock-induced seizure model. Łuszczki, J.J., Kozicka, M., Swiader, M.J., Czuczwar, S.J. Pharmacological reports : PR. (2005) [Pubmed]
  10. Physiological role for P2X1 receptors in renal microvascular autoregulatory behavior. Inscho, E.W., Cook, A.K., Imig, J.D., Vial, C., Evans, R.J. J. Clin. Invest. (2003) [Pubmed]
  11. The antiinflammatory mechanism of methotrexate. Increased adenosine release at inflamed sites diminishes leukocyte accumulation in an in vivo model of inflammation. Cronstein, B.N., Naime, D., Ostad, E. J. Clin. Invest. (1993) [Pubmed]
  12. Mediation of tubuloglomerular feedback by adenosine: evidence from mice lacking adenosine 1 receptors. Sun, D., Samuelson, L.C., Yang, T., Huang, Y., Paliege, A., Saunders, T., Briggs, J., Schnermann, J. Proc. Natl. Acad. Sci. U.S.A. (2001) [Pubmed]
  13. A1 adenosine receptor knockout mice exhibit increased renal injury following ischemia and reperfusion. Lee, H.T., Xu, H., Nasr, S.H., Schnermann, J., Emala, C.W. Am. J. Physiol. Renal Physiol. (2004) [Pubmed]
  14. Transgenic A1 adenosine receptor overexpression increases myocardial resistance to ischemia. Matherne, G.P., Linden, J., Byford, A.M., Gauthier, N.S., Headrick, J.P. Proc. Natl. Acad. Sci. U.S.A. (1997) [Pubmed]
  15. A1 receptor antagonist 8-cyclopentyl-1,3-dipropylxanthine selectively activates chloride efflux from human epithelial and mouse fibroblast cell lines expressing the cystic fibrosis transmembrane regulator delta F508 mutation. Guay-Broder, C., Jacobson, K.A., Barnoy, S., Cabantchik, Z.I., Guggino, W.B., Zeitlin, P.L., Turner, R.J., Vergara, L., Eidelman, O., Pollard, H.B. Biochemistry (1995) [Pubmed]
  16. A1 adenosine receptor knockout mice are protected against acute radiocontrast nephropathy in vivo. Lee, H.T., Jan, M., Bae, S.C., Joo, J.D., Goubaeva, F.R., Yang, J., Kim, M. Am. J. Physiol. Renal Physiol. (2006) [Pubmed]
  17. Adenosine A1 receptors are crucial in keeping an epileptic focus localized. Fedele, D.E., Li, T., Lan, J.Q., Fredholm, B.B., Boison, D. Exp. Neurol. (2006) [Pubmed]
  18. Compensation of proximal tubule malabsorption in AQP1-deficient mice without TGF-mediated reduction of GFR. Hashimoto, S., Huang, Y., Mizel, D., Briggs, J., Schnermann, J. Acta Physiol. Scand. (2004) [Pubmed]
  19. Osmotic diuretics induce adenosine A1 receptor expression and protect renal proximal tubular epithelial cells against cisplatin-mediated apoptosis. Pingle, S.C., Mishra, S., Marcuzzi, A., Bhat, S.G., Sekino, Y., Rybak, L.P., Ramkumar, V. J. Biol. Chem. (2004) [Pubmed]
  20. Increased nociceptive response in mice lacking the adenosine A1 receptor. Wu, W.P., Hao, J.X., Halldner, L., Lövdahl, C., DeLander, G.E., Wiesenfeld-Hallin, Z., Fredholm, B.B., Xu, X.J. Pain (2005) [Pubmed]
  21. Luminal adenosine stimulates chloride secretion through A1 receptor in mouse jejunum. Ghanem, E., Lövdahl, C., Daré, E., Ledent, C., Fredholm, B.B., Boeynaems, J.M., Van Driessche, W., Beauwens, R. Am. J. Physiol. Gastrointest. Liver Physiol. (2005) [Pubmed]
  22. Cardiac overexpression of A1-adenosine receptor protects intact mice against myocardial infarction. Yang, Z., Cerniway, R.J., Byford, A.M., Berr, S.S., French, B.A., Matherne, G.P. Am. J. Physiol. Heart Circ. Physiol. (2002) [Pubmed]
  23. Altered sinus nodal and atrioventricular nodal function in freely moving mice overexpressing the A1 adenosine receptor. Kirchhof, P., Fabritz, L., Fortmuller, L., Matherne, G.P., Lankford, A., Baba, H.A., Schmitz, W., Breithardt, G., Neumann, J., Boknik, P. Am. J. Physiol. Heart Circ. Physiol. (2003) [Pubmed]
  24. Contractile effects of adenosine A1 and A2A receptors in isolated murine hearts. Tikh, E.I., Fenton, R.A., Dobson, J.G. Am. J. Physiol. Heart Circ. Physiol. (2006) [Pubmed]
  25. Adenosine receptor-mediated coronary vascular protection in post-ischemic mouse heart. Zatta, A.J., Matherne, G.P., Headrick, J.P. Life Sci. (2006) [Pubmed]
  26. Adenosine acts as an endogenous modulator of IL-2-dependent proliferation of cytotoxic T lymphocytes. Antonysamy, M.A., Moticka, E.J., Ramkumar, V. J. Immunol. (1995) [Pubmed]
  27. Intrastriatal adenosine A1 receptor antisense oligodeoxynucleotide blocks ethanol-induced motor incoordination. Phan, T.A., Gray, A.M., Nyce, J.W. Eur. J. Pharmacol. (1997) [Pubmed]
  28. Autocrine activation of adenosine A1 receptors blocks D1A but not D1B dopamine receptor desensitization. Le Crom, S., Prou, D., Vernier, P. J. Neurochem. (2002) [Pubmed]
  29. Chronotropic and vasodilatory responses to adenosine and isoproterenol in mouse heart: effects of adenosine A1 receptor overexpression. Headrick, J.P., Gauthier, N.S., Morrison, R.R., Matherne, G.P. Clin. Exp. Pharmacol. Physiol. (2000) [Pubmed]
  30. Reduced autoregulatory effectiveness in adenosine 1 receptor-deficient mice. Hashimoto, S., Huang, Y., Briggs, J., Schnermann, J. Am. J. Physiol. Renal Physiol. (2006) [Pubmed]
  31. Changes in adenosine A1- and A2-receptor expression during adipose cell differentiation. Børglum, J.D., Vassaux, G., Richelsen, B., Gaillard, D., Darimont, C., Ailhaud, G., Négrel, R. Mol. Cell. Endocrinol. (1996) [Pubmed]
  32. Sleep and its homeostatic regulation in mice lacking the adenosine A1 receptor. Stenberg, D., Litonius, E., Halldner, L., Johansson, B., Fredholm, B.B., Porkka-Heiskanen, T. Journal of sleep research. (2003) [Pubmed]
  33. Functional consequences at the single-nephron level of the lack of adenosine A1 receptors and tubuloglomerular feedback in mice. Vallon, V., Richter, K., Huang, D.Y., Rieg, T., Schnermann, J. Pflugers Arch. (2004) [Pubmed]
  34. Blood pressure-dependent inhibition of Renin secretion requires A1 adenosine receptors. Schweda, F., Segerer, F., Castrop, H., Schnermann, J., Kurtz, A. Hypertension (2005) [Pubmed]
WikiGenes - Universities