Drug intelligence / Profile preview

theobromine

Development stage
Phase 3
Modality
Small Molecules
Administration
Oral
01

Overview

Theobromine is a naturally occurring xanthine alkaloid and the principal methylxanthine found in cacao beans (Theobroma cacao) and chocolate products. It is structurally related to caffeine and theophylline. Theobromine acts primarily as an antagonist at adenosine receptor A1 and adenosine receptor A2a, leading to increased neurotransmitter release and mild stimulation of cardiac muscle, vasodilation, bronchodilation, and diuresis[1][4][5][6]. Its phosphodiesterase inhibitory activity is weaker than that of caffeine. The compound has little central nervous system stimulant effect compared to caffeine but exerts notable effects on smooth muscle relaxation (especially vascular), heart stimulation, and increased urine output[1][4]. Historically used as a diuretic and for treating angina pectoris or hypertension; it is now rarely used pharmaceutically except in some countries such as South Korea[4]. Theobromine may also inhibit poly(ADP-ribose) polymerase-1 (PARP-1), which could contribute to anti-inflammatory effects[6].

Other names
xantheose3,7-dimethylxanthine
02

Targets

ADORA2A (Adenosine A₂A Receptor)PARP1 (Poly (adp-ribose) polymerase 1)PDE (Phosphodiesterase family)ADORA1 (Adenosine receptor A1 subtype)

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