Target intelligence / Profile preview

Methylxanthines

Molecular classification
Purine derivatives, Xanthine derivatives, Phosphodiesterase inhibitors, Adenosine receptor antagonists, Histone deacetylase activators, Calcium regulators, GABA receptor modulators
01

Overview

Methylxanthines are a class of chemical compounds derived from xanthine with one or more methyl groups attached to their structure. They are found naturally in various plants and have significant pharmacological properties, acting as phosphodiesterase inhibitors, adenosine receptor antagonists, and influencing calcium regulation and histone deacetylase activity. They are used therapeutically in respiratory conditions and as CNS stimulants but have a narrow therapeutic window and potential for toxicity.

Other names
1-Methylxanthine7-MethylxanthineTheophylline (1,3-dimethylxanthine)Paraxanthine (1,7-dimethylxanthine)Theobromine (3,7-dimethylxanthine)Caffeine (1,3,7-trimethylxanthine)
02

Mechanism of action

Methylxanthines exert their effects through multiple mechanisms including phosphodiesterase inhibition, adenosine receptor antagonism, histone deacetylase activation, calcium regulation, and GABA receptor modulation.

03

Biological functions

Phosphodiesterase inhibitionAdenosine receptor antagonismHistone deacetylase activationCalcium regulationGABA receptor modulationBronchodilationCNS stimulationDiuresisImmunomodulationAnti-inflammation
04

Disease associations

AsthmaChronic bronchitisEmphysemaChronic obstructive pulmonary disease (COPD)Airways obstructionPeripheral vascular disease
05

Safety considerations

Central nervous system stimulationCardiovascular effectsGastrointestinal disturbancesDiuretic effectsNarrow therapeutic window (especially theophylline)Toxicity at higher doses
06

Interacting drugs

Theophylline

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