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Adenosine Receptor Subtypes: Characterization and Therapeutic Regulation
Abstract
Adenosine receptors (ARs) are members of the G protein-coupled receptor family and mediate the multiple physiological effects of adenosine. Currently, four AR subtypes have been cloned: A1AR, A2aAR, A2bAR, and A3AR. All subtypes are distinctly distributed throughout the body and AR agonists and antagonists have potential therapeutic utility. Knowledge of AR amino acid structure has been utilized in mutagenesis studies to identify specific receptor regions that interact with distinct classes of ligands. Cloning of ARs has also permitted receptor regulatory processes such as desensitization to be studied in greater detail, in particular, the molecular mechanisms underlying this event. Cloning of the human A1AR has revealed that alternate splicing generates distinct receptor transcripts. The existence of a particular transcript in a tissue or cell apparently regulates the level of A1AR expression in the tissue. This review focuses on these aspects of AR structure and function and their therapeutic regulation.
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Cited by
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Nurminen, M.-L., Niittynen, L., Korpela, R., & Vapaatalo, H. (1999) · European Journal of Clinical Nutrition · doi:10.1038/sj.ejcn.1600899 · Cited by 351
Gallopin, T., Luppi, P.-H., Cauli, B., Urade, Y., Rossier, J., Hayaishi, O., Lambolez, B., & Fort, P. (2005) · Neuroscience · doi:10.1016/j.neuroscience.2005.05.045 · Cited by 229
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Headrick, J. P., Hack, B., & Ashton, K. J. (2003) · American Journal of Physiology-Heart and Circulatory Physiology · doi:10.1152/ajpheart.00407.2003 · Cited by 171
Samari, H. R., & Seglen, P. O. (1998) · Journal of Biological Chemistry · doi:10.1074/jbc.273.37.23758 · Cited by 125
Metadata
- Authors
- Olah, M. E., & Stiles, G. L.
- Venue
- Annual Review of Pharmacology and Toxicology
- Publisher
- Annual Reviews
- Published
- 1995-04
- Volume
- 35
- Issue
- 1
- Pages
- 581-606
- ISSN
- 0362-1642 (ISSN-L)
- 1545-4304
- OpenAlex
- W2173637498
- Cited by
- 540
- References
- 0
- FWCI
- 16.16
- Type
- journal article
- Language
- en
- Open access
- closed
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- Olah, M. E., & Stiles, G. L. (1995). Adenosine Receptor Subtypes: Characterization and Therapeutic Regulation. Annual Review of Pharmacology and Toxicology. https://doi.org/10.1146/annurev.pa.35.040195.003053
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