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Theophylline extended-release tablets in Japan. Theophylline, also known as 1,3-dimethylxanthine, is a drug that inhibits phosphodiesterase and blocks adenosine receptors. [1] It is used to treat chronic obstructive pulmonary disease (COPD) and asthma. [2] Its pharmacology is similar to other methylxanthine drugs (e.g., theobromine and caffeine ...
Xanthine (/ ˈ z æ n θ iː n / or / ˈ z æ n θ aɪ n /, from Ancient Greek ξανθός xanthós ' yellow ' for its yellowish-white appearance; archaically xanthic acid; systematic name 3,7-dihydropurine-2,6-dione) is a purine base found in most human body tissues and fluids, as well as in other organisms. [2]
Phosphodiesterase-5. A phosphodiesterase inhibitor is a drug that blocks one or more of the five subtypes of the enzyme phosphodiesterase (PDE), thereby preventing the inactivation of the intracellular second messengers, cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) by the respective PDE subtype(s).
Paraxanthine, also known as 1,7-dimethylxanthine, is a metabolite of theophylline and theobromine, two well-known stimulants found in coffee, tea, and chocolate mainly in the form of caffeine. It is a member of the xanthine family of alkaloids, which includes theophylline, theobromine and caffeine.
8-Cyclopentyl-1,3-dimethylxanthine (8-Cyclopentyltheophylline, 8-CPT, CPX) is a drug which acts as a potent and selective antagonist for the adenosine receptors, with some selectivity for the A 1 receptor subtype, as well as a non-selective phosphodiesterase inhibitor.
8-Phenyltheophylline (8-phenyl-1,3-dimethylxanthine, 8-PT) is a drug derived from the xanthine family which acts as a potent and selective antagonist for the adenosine receptors A 1 and A 2A, but unlike other xanthine derivatives has virtually no activity as a phosphodiesterase inhibitor.
Most studies used analogues of the nucleotide substrates or derivatives of natural product inhibitors such as xanthine (e.g. theophylline) and papaverine. [ 6 ] [ 7 ] The active site of PDE3 can be considered as a summary of ideas about receptor topography resulting from the first generation inhibitors.
Methylxanthines are chemical compounds which are derivatives of xanthine with one or more methyl groups, including: One methyl group: 1-Methylxanthine; 3-Methylxanthine; 7-Methylxanthine; Two methyl groups: Theophylline (1,3-dimethylxanthine) Paraxanthine (1,7-dimethylxanthine) Theobromine (3,7-dimethylxanthine) Three methyl groups:
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