Xanthine derivatives

Xanthine derivatives
Accession Number
DBCAT001034  (DBCAT000503, DBCAT001028, DBCAT001220, DBCAT002203, DBCAT002692, DBCAT003295)

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.

ATC Classification
DrugDrug Description
OxtriphyllineA bronchodilator used for the treatment of asthma, bronchitis, COPD, and emphysema.
DoxofyllineA methylxanthine derivative used in chronic obstructive pulmonary disease, asthma, and bronchospasms.
BamifyllineA methylxanthine derivative indicated in the treatment of bronchial asthma and other conditions with bronchospasm.
AcefyllineNot Annotated
BufyllineNot Annotated
FenethyllineNot Available
ProxyphyllineNot Annotated
BromotheophyllineBromotheophylline is used as a diuretic and also, in combination with DB00316, it is used for the relief of temporary water weight gain, bloating, swelling and full feeling associated with...
PentoxifyllineA methylxanthine derivative used to treat intermittent claudication caused by chronic occlusive arterial disease of the limbs.
8-azaguanine8-azaguanine is one of the early purine analogs showing antineoplastic activity. It functions as an antimetabolite and is easily incorporated into ribonucleic acids.
7,9-DimethylguanineNot Available
XanthineA drug used to manage uncomplicated liver dysfunction in combination with orotic acid.
7-DeazaguanineNot Available
GuanineNot Available
9-MethylguanineNot Available
PeldesinePeldesine is a potent inhibitor of human CCRF-CEM T-cell proliferation. It has undergone phase I trials for the treatment of Human Immunodeficiency Virus (HIV) infections.
HypoxanthineHypoxanthine is a purine and a reaction intermediate in the metabolism of adenosine and in the formation of nucleic acids by the salvage pathway.
9-DeazaguanineNot Available
ValomaciclovirInvestigated for use/treatment in herpes zoster infections and viral infection.
3-isobutyl-1-methyl-7H-xanthineNot Available
Uric acidAt present (August 2013), there is no approved indication for uric acid. The potential therapeutic use for uric acid is as an adjunct in acute ischemic stroke.
6-O-benzylguanine6-O-benzylguanine has been used in trials studying the treatment of HIV Infection, Adult Gliosarcoma, Adult Glioblastoma, Stage I Adult Hodgkin Lymphoma, and Stage II Adult Hodgkin Lymphoma, among others.
LisofyllineLisofylline has been investigated for the treatment of Type 1 Diabetes Mellitus.
LobucavirLobucavir has been used in trials studying the treatment of HIV Infections and Cytomegalovirus Infections.
CafedrineCafedrine is under investigation in clinical trial NCT01311414 (Effect of Cafedrine/Theodrenaline and Urapidil on Cerebral Oxygenation).
TheodrenalineTheodrenaline is under investigation in clinical trial NCT01311414 (Effect of Cafedrine/Theodrenaline and Urapidil on Cerebral Oxygenation).
EtamiphyllineNot Annotated
PentifyllineNot Annotated
FurafyllineFurafylline is a derivative of methylxanthine derivative. It was developed on the context of asthma as a long-acting alternative for theophylline.
Theobrominetheobromine is used as a vasodilator, a diuretic, and heart stimulant. And similar to caffeine, it may be useful in management of fatigue and orthostatic hypotension.
PropentofyllineInvestigated for use/treatment in alzheimer's disease.
CaffeineA stimulant present in tea, coffee, cola beverages, analgesic drugs, and agents used to increase alertness. It is also used in to prevent and treat pulmonary complications of premature birth.
8-chlorotheophyllineWhen used in combination with DB01075 as the antiemetic DB00985, 8-chlorotheophylline is indicated for the prevention and treatment of nausea, vomiting, or vertigo of motion sickness.
TheophyllineA xanthine used to manage the symptoms of asthma, COPD, and other lung conditions caused by reversible airflow obstruction.
DyphyllineA theophylline derivative used to treat asthma, bronchospasm, and COPD.
AminophyllineA bronchodilator consisting of theophylline that is used for the treatment of bronchospasm due to asthma, emphysema and chronic bronchitis.
MercaptopurineAn antineoplastic agent used to treat acute lymphocytic leukemia.
PCS-499PCS-499 is under investigation in clinical trial NCT01487109 (A Phase 2 Study to Evaluate the Safety and Efficacy of CTP-499 in Type 2 Diabetic Nephropathy Patients).
5'-S-methyl-5'-thioadenosineNot Available
7-cyano-7-deazaguanineNot Available
Besifovir dipivoxilInvestigated for use/treatment in hepatitis (viral, B).
Valomaciclovir stearateValomaciclovir stearate is under investigation in clinical trial NCT00831103 (A Phase 2b Trial of EPB-348 for the Treatment of Herpes Zoster).
BesifovirNot Annotated
Drugs & Drug Targets
OxtriphyllinecGMP-inhibited 3',5'-cyclic phosphodiesterase Atarget
OxtriphyllinecAMP-specific 3',5'-cyclic phosphodiesterase 4Atarget
OxtriphyllineAdenosine receptor A2atarget
OxtriphyllineAdenosine receptor A1target
OxtriphyllineCytochrome P450 1A2enzyme
OxtriphyllineSolute carrier family 22 member 7transporter
OxtriphyllineHistone deacetylase 2target
DoxofyllinePhosphodiesterase 2A, cGMP-stimulatedtarget
DoxofyllineAdenosine receptor A2atarget
DoxofyllineBeta-2 adrenergic receptortarget
DoxofyllineCytochrome P450 1A2enzyme
BamifyllineCytochrome P450 1A2enzyme
AcefyllineCytochrome P450 1A2enzyme
BufyllineCytochrome P450 1A2enzyme
FenethyllineCytochrome P450 1A2enzyme
ProxyphyllineCytochrome P450 1A2enzyme
BromotheophyllineCytochrome P450 1A2enzyme
PentoxifyllineAdenosine receptor A1target
PentoxifyllineAdenosine receptor A2atarget
PentoxifyllineCytochrome P450 1A2enzyme
PentoxifyllinePhosphodiesterase enzymestarget
8-azaguaninePurine nucleoside phosphorylasetarget
8-azaguanineCytochrome P450 1A2enzyme
7,9-DimethylguanineCap-specific mRNA (nucleoside-2'-O-)-methyltransferasetarget
XanthinePurine nucleoside phosphorylase 2target
XanthineXanthine phosphoribosyltransferasetarget
XanthineCytochrome P450 1A2enzyme
GuaninePurine nucleoside phosphorylasetarget
GuaninePurine nucleoside phosphorylase 2target
GuanineXanthine phosphoribosyltransferasetarget
GuanineGTP cyclohydrolase 1target
GuaninePurine nucleoside phosphorylasetarget
9-MethylguanineDihydroneopterin aldolasetarget
9-MethylguanineCytochrome P450 1A2enzyme
PeldesinePurine nucleoside phosphorylasetarget
HypoxanthinePurine nucleoside phosphorylasetarget
HypoxanthineCytochrome P450 1A2enzyme
9-DeazaguanineHypoxanthine-guanine phosphoribosyltransferasetarget
9-DeazaguanineCytochrome P450 1A2enzyme
3-isobutyl-1-methyl-7H-xanthinecGMP-specific 3',5'-cyclic phosphodiesterasetarget
3-isobutyl-1-methyl-7H-xanthinecGMP-inhibited 3',5'-cyclic phosphodiesterase Btarget
3-isobutyl-1-methyl-7H-xanthineHigh affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7Atarget
3-isobutyl-1-methyl-7H-xanthinecAMP-specific 3',5'-cyclic phosphodiesterase 4Dtarget
3-isobutyl-1-methyl-7H-xanthineHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9Atarget
3-isobutyl-1-methyl-7H-xanthineHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8Atarget
3-isobutyl-1-methyl-7H-xanthinecGMP-dependent 3',5'-cyclic phosphodiesterasetarget
3-isobutyl-1-methyl-7H-xanthineRetinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gammatarget
Uric acidSolute carrier family 22 member 6transporter
Uric acidSolute carrier family 22 member 8transporter
Uric acidGlycogen phosphorylase, liver formtarget
Uric acidSolute carrier family 2, facilitated glucose transporter member 9transporter
6-O-benzylguanineCytochrome P450 3A4enzyme
LisofyllineCytochrome P450 1A2enzyme
EtamiphyllineCytochrome P450 1A2enzyme
PentifyllineCytochrome P450 1A2enzyme
FurafyllineCytochrome P450 1A2enzyme
TheobromineCytochrome P450 1A2enzyme
TheobromineCytochrome P450 2E1enzyme
TheobromineAdenosine receptor A1target
TheobromineAdenosine receptor A2atarget
TheobrominecAMP-specific 3',5'-cyclic phosphodiesterase 4Btarget
PropentofyllinecAMP-specific 3',5'-cyclic phosphodiesterase 4Atarget
PropentofyllineCytochrome P450 1A2enzyme
CaffeineAdenosine receptor A1target
CaffeinecAMP-specific 3',5'-cyclic phosphodiesterase 4Btarget
CaffeineAdenosine receptor A2atarget
CaffeineCytochrome P450 1A2enzyme
CaffeineRyanodine receptor 1target
CaffeineCytochrome P450 3A4enzyme
CaffeineCytochrome P450 2E1enzyme
CaffeineCytochrome P450 2C8enzyme
CaffeineCytochrome P450 2C9enzyme
CaffeineCytochrome P450 1A1enzyme
CaffeineCytochrome P450 1B1enzyme
CaffeineCytochrome P450 2D6enzyme
CaffeineCyclic nucleotide phosphodiesterasetarget
CaffeineDNA-dependent protein kinase catalytic subunittarget
CaffeinePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformtarget
CaffeinePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformtarget
CaffeinePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformtarget
CaffeineInositol 1,4,5-trisphosphate receptortarget
CaffeineSerine-protein kinase ATMtarget
CaffeineATP-binding cassette sub-family G member 2transporter
CaffeineAdenosine receptor A2btarget
CaffeineAdenosine receptor A3target
CaffeinePhosphodiesterase enzymestarget
8-chlorotheophyllineAdenosine receptor A2atarget
8-chlorotheophyllineCytochrome P450 1A2enzyme
TheophyllinecGMP-inhibited 3',5'-cyclic phosphodiesterase Atarget
TheophyllinecAMP-specific 3',5'-cyclic phosphodiesterase 4Btarget
TheophyllineAdenosine receptor A2btarget
TheophyllinecAMP-specific 3',5'-cyclic phosphodiesterase 4Atarget
TheophyllinecGMP-specific 3',5'-cyclic phosphodiesterasetarget
TheophyllineAdenosine receptor A1target
TheophyllineAdenosine receptor A2atarget
TheophyllineCytochrome P450 1A2enzyme
TheophyllineAdenosine deaminaseenzyme
TheophyllineCytochrome P450 2E1enzyme
TheophyllineCytochrome P450 3A4enzyme
TheophyllineSolute carrier family 22 member 7transporter
TheophyllineCytochrome P450 1A1enzyme
TheophyllineCytochrome P450 1B1enzyme
TheophyllineCytochrome P450 2D6enzyme
TheophyllineHistone deacetylase 2target
TheophyllineMinor histocompatibility antigen H13target
TheophyllineNodal modulator 1target
TheophyllinePoly [ADP-ribose] polymerase 1target
TheophyllineProtein RIC-3target
TheophyllineTubulin monoglycylase TTLL3target
DyphyllinecAMP-specific 3',5'-cyclic phosphodiesterase 4Btarget
DyphyllinecAMP-specific 3',5'-cyclic phosphodiesterase 4Atarget
DyphyllinecAMP-specific 3',5'-cyclic phosphodiesterase 4Ctarget
DyphyllinecAMP-specific 3',5'-cyclic phosphodiesterase 4Dtarget
DyphyllineAdenosine receptor A1target
DyphyllineAdenosine receptor A2atarget
AminophyllinecGMP-inhibited 3',5'-cyclic phosphodiesterase Atarget
AminophyllineAdenosine receptor A3target
AminophyllineAdenosine receptor A1target
AminophyllineCytochrome P450 1A2enzyme
AminophyllineCytochrome P450 2E1enzyme
AminophyllineCytochrome P450 3A4enzyme
AminophyllineHistone deacetylase 2target
MercaptopurineThiopurine S-methyltransferaseenzyme
MercaptopurineXanthine dehydrogenase/oxidaseenzyme
MercaptopurineHypoxanthine-guanine phosphoribosyltransferasetarget
MercaptopurineSolute carrier family 22 member 8transporter
MercaptopurineMultidrug resistance-associated protein 4transporter
MercaptopurineMultidrug resistance-associated protein 5transporter
MercaptopurineSodium/nucleoside cotransporter 2transporter
MercaptopurineSolute carrier family 28 member 3transporter
MercaptopurineEquilibrative nucleoside transporter 1transporter
MercaptopurineEquilibrative nucleoside transporter 2transporter
MercaptopurineAldehyde oxidaseenzyme
MercaptopurineInosine-5'-monophosphate dehydrogenasetarget
5'-S-methyl-5'-thioadenosineModification methylase RsrItarget
5'-S-methyl-5'-thioadenosineS-methyl-5'-thioadenosine phosphorylasetarget
7-cyano-7-deazaguanineQueuine tRNA-ribosyltransferasetarget
Besifovir dipivoxilDNA polymerasetarget