Definition and research guide
This page combines a MeSH definition, publication statistics and selected research abstracts. It is a starting point for reading the literature, not a medical textbook or a systematic evidence review.
Content available: 4 complete abstracts (765 words), 10 references. Full article text is not stored or reproduced here; follow the PMID, DOI or PMC links to read the original sources and their access terms.
Definition
A methyl xanthine derivative from tea with diuretic, smooth muscle relaxant, bronchial dilation, cardiac and central nervous system stimulant activities. Theophylline inhibits the 3',5'-cyclic nucleotide phosphodiesterase that degrades cyclic amp thus potentiates the actions of agents that act through adenylyl cyclases and cyclic AMP.
Definition: NLM Medical Subject Headings (MeSH) scope note (Public domain (U.S. National Library of Medicine); attribution requested). View the MeSH record.
Also known as: 3,7-Dihydro-1,3-dimethyl-1H-purine-2,6-dione; 1,3-Dimethylxanthine; 1,3 Dimethylxanthine; Glycine Theophyllinate; Theophyllinate, Glycine; Nuelin S.A.; Nuelin; Synophylate.
Where it fits in the MeSH classification
- Broader topics
- Xanthines
- Narrower topics
- 1-Methyl-3-isobutylxanthine; Aminophylline; Dimenhydrinate; Dyphylline; Xanthinol Niacinate
Related concepts
- Cyclic Nucleotide Phosphodiesterase
- Cyclic Amp
- Adenylyl Cyclases
Research landscape
PubMed indexes 28,819 records tagged with the MeSH heading “Theophylline” (counts retrieved 2026-10-31). 650 of them (2.3%) were published from 2020 onward, and the busiest period so far is through 1999 with 23,067 records.
Reviews account for 1,433 records (5.0%) and meta-analyses for 79. Randomized controlled trials number 1,260 (4.4%) as a share of all records on the topic.
Show the data
| Period | Records |
|---|---|
| through 1999 | 23,067 |
| 2000-2009 | 3,293 |
| 2010-2019 | 1,809 |
| 2020 onward | 650 |
Publication-type chart data
| Type | Records | Share |
|---|---|---|
| Reviews | 1,433 | 5.0% |
| Meta-analyses | 79 | 0.3% |
| Randomized controlled trials | 1,260 | 4.4% |
Method: PubMed query "Theophylline"[MeSH Terms] with publication-type and date filters, retrieved 2026-10-31.
Reading the evidence in drugs and chemicals
Studies of a chemical or drug can answer very different questions: what it is and how it behaves in cells and animals, how the body handles it, and whether it changes outcomes in people. Laboratory and animal findings often do not carry over to patients, and observational studies of exposures are confounded by who uses a substance and why. Nothing on this page is a recommendation to use, avoid, start or stop any substance or medicine; talk to a qualified clinician or pharmacist about your own situation. Check the dose, the species, the comparison group and whether a patient-relevant outcome was measured.
Evidence from open-access studies
These open-access studies come from PubMed’s best-match results for this heading (papers whose main topic it is), ranked here by citation count, with one recent addition. Each abstract is reproduced in full under its recorded open licence so that you can read the authors’ own words. They illustrate the literature; they are not a systematic summary of it. Citation counts measure attention, not reliability or clinical benefit.
Roles of db-cAMP, IBMX and RA in aspects of neural differentiation of cord blood derived mesenchymal-like stem cells [1]
Abstract reading summary — source excerpts
- Opening excerpt
- Mesenchymal stem cells (MSCs) have multilineage differentiation potential which includes cell lineages of the central nervous system; hence MSCs might be useful in the treatment of neurodegenerative diseases such as Parkinson's disease.
- Closing excerpt
- We also demonstrate a possible inhibitory role of the protein kinase A signaling pathway in the phosphorylation of specific TH isoforms.
- Interpretation limits
- Verbatim excerpts from the authors’ abstract; the closing excerpt may describe a finding, limitation or recommendation. Design, population, effect size and uncertainty have not been independently extracted or appraised. Read the complete abstract and linked paper before interpreting the findings.
Read complete abstract (171 words)
Mesenchymal stem cells (MSCs) have multilineage differentiation potential which includes cell lineages of the central nervous system; hence MSCs might be useful in the treatment of neurodegenerative diseases such as Parkinson's disease. Although mesenchymal stem cells have been shown to differentiate into the neural lineage, there is still little knowledge about the underlying mechanisms of differentiation particularly towards specialized neurons such as dopaminergic neurons. Here, we show that MSCs derived from human umbilical cord blood (MSC(hUCBs)) are capable of expressing tyrosine hydroxylase (TH) and Nurr1, markers typically associated with DA neurons. We also found differential phosphorylation of TH isoforms indicating the presence of post-translational mechanisms possibly activating and modifying TH in MSC(hUCB). Furthermore, functional dissection of components in the differentiation medium revealed that dibutyryl-cAMP (db-cAMP), 3-isobutyl-1-methylxanthine (IBMX) and retinoic acid (RA) are involved in the regulation of Nurr1 and Neurofilament-L expression as well as in the differential phosphorylation of TH. We also demonstrate a possible inhibitory role of the protein kinase A signaling pathway in the phosphorylation of specific TH isoforms.
Abstract reproduced from the open-access article under the recorded cc by licence; © the authors. PMID 20195526 · DOI · PMC2827567
Transporter protein and drug-conjugated gold nanoparticles capable of bypassing the blood-brain barrier [2]
Abstract reading summary — source excerpts
- Opening excerpt
- Drug delivery to the central nervous system (CNS) is challenging due to the inability of many drugs to cross the blood-brain barrier (BBB).
- Closing excerpt
- This study not only demonstrates a promising strategy to deliver drugs to the CNS bypassing the BBB but also contributes a potential nanotherapy for the treatment of respiratory muscle paralysis resulted from cervical SCI.
- Interpretation limits
- Verbatim excerpts from the authors’ abstract; the closing excerpt may describe a finding, limitation or recommendation. Design, population, effect size and uncertainty have not been independently extracted or appraised. Read the complete abstract and linked paper before interpreting the findings.
Read complete abstract (163 words)
Drug delivery to the central nervous system (CNS) is challenging due to the inability of many drugs to cross the blood-brain barrier (BBB). Here, we show that wheat germ agglutinin horse radish peroxidase (WGA-HRP) chemically conjugated to gold nanoparticles (AuNPs) can be transported to the spinal cord and brainstem following intramuscular injection into the diaphragm of rats. We synthesized and determined the size and chemical composition of a three-part nanoconjugate consisting of WGA-HRP, AuNPs, and drugs for the treatment of diaphragm paralysis associated with high cervical spinal cord injury (SCI). Upon injection into the diaphragm muscle of rats, we show that the nanoconjugate is capable of delivering the drug at a much lower dose than the unconjugated drug injected systemically to effectively induce respiratory recovery in rats following SCI. This study not only demonstrates a promising strategy to deliver drugs to the CNS bypassing the BBB but also contributes a potential nanotherapy for the treatment of respiratory muscle paralysis resulted from cervical SCI.
Abstract reproduced from the open-access article under the recorded cc by licence; © the authors. PMID 27180729 · DOI · PMC4867579
Theophylline controllable RNAi-based genetic switches regulate expression of lncRNA TINCR and malignant phenotypes in bladder cancer cells [3]
Abstract reading summary — source excerpts
- Opening excerpt
- TINCR is a well-known lncRNA which acts as a master regulator in somatic differentiation development.
- Closing excerpt
- These findings suggest that lncRNA-TINCR could promote bladder cancer development and progression and artificial control of its expression through inducible RNAi may represent a new kind of therapeutic strategy for treating human bladder cancer.
- Interpretation limits
- Verbatim excerpts from the authors’ abstract; the closing excerpt may describe a finding, limitation or recommendation. Design, population, effect size and uncertainty have not been independently extracted or appraised. Read the complete abstract and linked paper before interpreting the findings.
Read complete abstract (157 words)
TINCR is a well-known lncRNA which acts as a master regulator in somatic differentiation development. However, it is still unclear whether TINCR is also involved in caner occurrence and progression. In this study, we observed that TINCR was up-regulated in bladder cancer tissues and cells and contributed to oncogenesis and cancer progression. Silencing TINCR expression inhibited cell proliferation and promoted apoptosis in vitro, indicating that TINCR may be the potential therapeutic target for treating bladder urothelial carcinoma. Thus we used the synthetic biology approach to create theophylline controllable RNAi-based genetic switches which silenced TINCR in a dosage-dependent manner. Both RNAi-OFF and ON switches can be used to quantitatively control the expression of TINCR in bladder cancer to suppress the progression of bladder cancer. These findings suggest that lncRNA-TINCR could promote bladder cancer development and progression and artificial control of its expression through inducible RNAi may represent a new kind of therapeutic strategy for treating human bladder cancer.
Abstract reproduced from the open-access article under the recorded cc by licence; © the authors. PMID 27586866 · DOI · PMC5009373
A randomised feasibility tolerability study of aminophylline for the prevention of preterm labour [4]
Abstract reading summary — source excerpts
- Opening excerpt
- BackgroundProgesterone is known to maintain uterine quiescence as pregnancy advances.
- Closing excerpt
- cond=NCT03152942%26;draw=2%26;rank=1 .
- Interpretation limits
- Verbatim excerpts from the authors’ abstract; the closing excerpt may describe a finding, limitation or recommendation. Design, population, effect size and uncertainty have not been independently extracted or appraised. Read the complete abstract and linked paper before interpreting the findings.
Read complete abstract (274 words)
BackgroundProgesterone is known to maintain uterine quiescence as pregnancy advances. Recently, its efficacy in preventing preterm birth has been questioned prompting a search for an alternative treatment option. Cyclic AMP has been shown invitro to act in synergy with progesterone to maintain uterine quiescence.MethodsWe undertook an open label randomised feasibility study to test the hypothesis that the addition of aminophylline to the standard of care (SoC) is acceptable and can be tolerated in pregnant women at high risk of spontaneous preterm labour (sPTL). Women at high risk of sPTL, who met the inclusion criteria were invited to participate and randomised to receive the SoC (progesterone alone, n = 33) or treatment with the SoC and aminophylline (n = 37). The main outcome measure was to assess the how many women at high-risk of sPTL tolerated and continued to take aminophylline. Data were analysed using Graphpad Prism 8.0c (Graphpad Software, San Diego, CA, USA).ResultsWe found that of the addition of aminophylline was well tolerated in 30 of the 33 (91%) of women who continued in the combined arm, without any additional adverse maternal or fetal outcomes. 58% of eligible women agreed to participate in the study. The compliance rate was high at 99.42% +-0.82%. 67% of the women completed the post study questionnaire and all stated their willingness to take aminophylline if it were offered routinely for the prevention of sPTL.ConclusionsThe addition of aminophylline to the SoC is acceptable to women at high-risk of sPTL confirming that a randomised trial of aminophylline to reduce preterm delivery in women at high-risk of PTL is feasible.Trial registrationClinical trial gov NCT03152942. Date of full registration: 15/5/2017. https://clinicaltrials.gov/ct2/show/NCT03152942?cond=NCT03152942%26;draw=2%26;rank=1 .
Abstract reproduced from the open-access article under the recorded cc by licence; © the authors. PMID 40148792 · DOI · PMC11948830
Key reviews and meta-analyses
The most cited review-type papers among PubMed’s best-match results for this heading, listed with bibliographic details only. Follow the links for the full text and access terms.
- Research article Theophylline. A "state of the art" review [5]
- Research article Methylxanthines in apnea of prematurity [6]
- Research article Theophylline in asthma [7]
- Research article Dimenhydrinate for prophylaxis of postoperative nausea and vomiting: a meta-analysis of randomized controlled trials [8]
- Research article Pharmacokinetic drug interactions with theophylline [9]
- Research article Theophylline for prevention of contrast-induced nephropathy: a systematic review and meta-analysis [10]
References
- Tio M, Tan KH, Lee W, Wang TT, Udolph G. Roles of db-cAMP, IBMX and RA in aspects of neural differentiation of cord blood derived mesenchymal-like stem cells. . 2010. PMID 20195526 · DOI · PMC2827567
- Zhang Y, Walker JB, Minic Z, Liu F, Goshgarian H, Mao G. Transporter protein and drug-conjugated gold nanoparticles capable of bypassing the blood-brain barrier. . 2016. PMID 27180729 · DOI · PMC4867579
- Chen Z, Liu Y, He A, Li J, Chen M, Zhan Y, et al.. Theophylline controllable RNAi-based genetic switches regulate expression of lncRNA TINCR and malignant phenotypes in bladder cancer cells. . 2016. PMID 27586866 · DOI · PMC5009373
- Singh N, Shah NM, Sooranna G, Bourke M, Yulia A, Battersby C, et al.. A randomised feasibility tolerability study of aminophylline for the prevention of preterm labour. . 2025. PMID 40148792 · DOI · PMC11948830
- Hendeles L, Weinberger M. Theophylline. A "state of the art" review. Pharmacotherapy. 1983. PMID 6344032 · DOI
- Aranda JV, Turmen T. Methylxanthines in apnea of prematurity. Clin Perinatol. 1979. PMID 383366 · DOI
- Weinberger M, Hendeles L. Theophylline in asthma. N Engl J Med. 1996. PMID 8614425 · DOI
- Kranke P, Morin AM, Roewer N, Eberhart LH. Dimenhydrinate for prophylaxis of postoperative nausea and vomiting: a meta-analysis of randomized controlled trials. Acta Anaesthesiol Scand. 2002. PMID 11939912 · DOI
- Jonkman JH, Upton RA. Pharmacokinetic drug interactions with theophylline. Clin Pharmacokinet. 1984. PMID 6147220 · DOI
- Bagshaw SM, Ghali WA. Theophylline for prevention of contrast-induced nephropathy: a systematic review and meta-analysis. Arch Intern Med. 2005. PMID 15911721 · DOI
About this article
- Sources
- NLM Medical Subject Headings (definition, synonyms); NCBI PubMed (counts, identifiers); Europe PMC (open-access abstracts and citation counts).
- Verification
- Every reference was resolved against PubMed on 2026-10-31; title, year and DOI matched.
- Review state
- automated source verified; no human expert review has been recorded yet.
- Version
- 1, last updated 2026-10-31.
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Evidence strength
EvidenceHelix's computed view of the study designs behind this topic: how common meta-analyses, randomized trials and reviews are, how recent the literature is, and a plain-language reading. It describes the design mix of the literature. It is not a quality appraisal of any study, and it is not medical advice.