Caffeine

Caffeine is a methylxanthine alkaloid naturally found in various plant parts that acts as an antagonist at central adenosine receptors at relevant physiological concentrations (IC₅₀ = ~30 μM).^1,2 It alters fatigue, mood, alertness, motor reaction time, vascular hemodynamics, and pain sensation.^2,3,4 Caffeine has also been implicated in carcinogenesis, although the concentrations used to affect cell cycling and apoptosis in the laboratory may not be commonly achieved in vivo.⁵

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1. Snyder, S.H., Katims, J.J., Annau, Z., et al. Adenosine receptors and behavioral actions of methylxanthines. Proc. Natl. Acad. Sci. USA 78(5), 3260-3264 (1981).

2. Fredholm, B.B., Bättig, K., Holmén, J., et al. Actions of caffeine in the brain with special reference to factors that contribute to its widespread use. Pharmacol. Rev. 51(1), 83-133 (1999).

3. Carrillo, J.A., and Benitez, J. Clinically significant pharmacokinetic interactions between dietary caffeine and medications. Clin. Pharmacokinet. 39(2), 127-153 (2000).

4. Pelligrino, D.A., Xu, H.L., and Vetri, F. Caffeine and the control of cerebral hemodynamics. J. Alzheimers Dis. 20(Suppl 1), S51-S62 (2010).

5. Bode, A.M., and Dong, Z. The enigmatic effects of caffeine in cell cycle and cancer. Cancer Lett. 247(1), 26-39 (2007).