Low, but not high, dose caffeine is a readily available probe for adenosine actions

Bertil B Fredholm; Jiangning Yang; Yingqing Wang

doi:10.1016/j.mam.2016.11.011

Low, but not high, dose caffeine is a readily available probe for adenosine actions

Mol Aspects Med. 2017 Jun:55:20-25. doi: 10.1016/j.mam.2016.11.011. Epub 2016 Nov 30.

Authors

Bertil B Fredholm¹, Jiangning Yang², Yingqing Wang³

Affiliations

¹ Department of Physiology and Pharmacology, Karolinska Institutet, S-171 77, Stockholm, Sweden. Electronic address: Bertil.Fredholm@ki.se.
² Department of Physiology and Pharmacology, Karolinska Institutet, S-171 77, Stockholm, Sweden; Division of Cardiology, Department of Medicine, Karolinska Institutet, Stockholm, Sweden.
³ Department of Physiology and Pharmacology, Karolinska Institutet, S-171 77, Stockholm, Sweden; Division of Antitumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China.

PMID: 27915051
DOI: 10.1016/j.mam.2016.11.011

Abstract

Caffeine is very widely used and knowledge of its mode of action can be used to gain an understanding of basal physiological regulation. This review makes the point that caffeine is - in low doses - an antagonist of adenosine acting at A₁, A_2A and A_2B receptors. We use published and unpublished data to make the point that high dose effects of caffeine are not only qualitatively different but have a different underlying mechanism. Therefore one must be careful in only using epidemiological or experimental data where rather low doses of caffeine are used to draw conclusions about the physiology and pathophysiology of adenosine.

Keywords: Adenosine; Caffeine; Heart rate; Locomotion; Theophylline.

Publication types

Review

MeSH terms

Adenosine / metabolism*
Caffeine / metabolism*
Caffeine / therapeutic use
Dose-Response Relationship, Drug*
Humans

Substances

Caffeine
Adenosine