The exact mechanism of action of theacrine is uncertain, as no binding affinities have been published. However, animal research involving selectiveA1 andA2Aadenosine agonists found theacrine pretreatment attenuated the expected motor depression induced by adenosine agonism, indicating that theacrine is likely an adenosine antagonist.[2]
Administration of selectivedopamine D1 and D2antagonists demonstrate that, similarly to caffeine,[4] the behavioural effects of theacrine are in part mediated bydopamine receptors.[2]
Theacrine has demonstrated clinical safety and non-habituating effects in healthy humans over eight weeks of daily use at up to 300 mg/day.[6] Moreover, there was no evidence of thetachyphylaxis typical of neuroactive agents like caffeine and other stimulants.[6]
In animal studies, theacrine has anLD50 of 810 mg/kg,[3][6] compared to 265 mg/kg for caffeine.[7]
^abcdeFeduccia AA, Wang Y, Simms JA, Yi HY, Li R, Bjeldanes L, Ye C, Bartlett SE (2012). "Locomotor activation by theacrine, a purine alkaloid structurally similar to caffeine: Involvement of adenosine and dopamine receptors".Pharmacology Biochemistry and Behavior.102 (2):241–248.doi:10.1016/j.pbb.2012.04.014.PMID22579816.S2CID31549989.
^abWang Y, Yang X, Zheng X, Li J, Ye C, Song X (2010). "Theacrine, a purine alkaloid with anti-inflammatory and analgesic activities".Fitoterapia.81 (6):627–631.doi:10.1016/j.fitote.2010.03.008.PMID20227468.
^Warszawski D, Gorodischer R, Kaplanski J (1978). "Comparative toxicity of caffeine and aminophylline (theophylline ethylenediamine) in young and adult rats".Biology of the Neonate.34 (1–2):68–71.doi:10.1159/000241107.PMID698326.
