Theacrine, also known as 1,3,7,9-tetramethyluric acid, is a
purine alkaloid found in
Cupuaçu (Theobroma grandiflorum) and in a Chinese tea known as kucha (
Chinese: 苦茶;
pinyin: kǔ chá;
lit. 'bitter tea') (Camellia assamica var. Kucha).[1][2] It shows
anti-inflammatory and
analgesic effects and appears to affect
adenosine signalling in a manner similar to
caffeine.[2][3] In kucha leaves, theacrine is synthesized from caffeine in what is thought to be a three-step
pathway.[2] Theacrine and
caffeine are structurally similar.
Pharmacology
Pharmacodynamics
The exact mechanism of action of theacrine is uncertain, as no
binding affinities have been published. However, animal research involving selective
A1 and
A2Aadenosine agonists found theacrine pretreatment attenuated the expected motor depression induced by adenosine agonism, indicating that theacrine is likely an adenosine antagonist.[2]
Administration of selective
dopamine D1 and D2
antagonists demonstrate that, similarly to caffeine,[4] theacrine's actions are in part mediated by
dopamine receptors.[2] This should not be taken as evidence that theacrine directly interacts with and/or augments dopamine receptors distinct from caffeine, as some marketers have misleadingly claimed.
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 the
tachyphylaxis typical of neuroactive agents like caffeine and other stimulants.[6]
In animal studies, theacrine has an
LD50 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.