rolofylline profile

rolofylline: selective antagonist for adenosine receptors; a cardiovascular agent [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	64627
CHEMBL ID	52333
CHEBI ID	177647
SCHEMBL ID	720438
SCHEMBL ID	13448940
SCHEMBL ID	18029490
MeSH ID	M0198780

Synonym
1,3-dipropyl-8-(3-tricyclo[3.3.1.03,7]nonanyl)-7h-purine-2,6-dione
CHEBI:177647
mk-7418
rolofylline
hmr-4902
kw-3902
1,3-dipropyl-8-(3-noradamantyl)xanthine
8-(hexahydro-2,5-methanopentalen-3a(1h)-yl)-3,7-dihydro-1,3-dipropyl-1h-purine-2,6-dione
kw 3902
CHEMBL52333 ,
L001406
D08989
rolofylline (usan)
136199-02-5
bdbm50003019
8-(hexahydro-2,5-methano-pentalen-3a-yl)-1,3-dipropyl-3,7-dihydro-purine-2,6-dione
kw3902
gtpl5604
SCHEMBL720438
SCHEMBL13448940
SCHEMBL18029490
AKOS024458012
8-(hexahydro-2,5-methanopentalen-3a(1h)-yl)-1,3-dipropyl-3,9-dihydro-1h-purine-2,6-dione
DTXSID50929292
Q7361410
BRD-A95683721-001-01-2
CS-0002980
HY-10965
MS-25589
A858196
E98670
AKOS040742571

Excerpt	Reference	Relevance
"Rolofylline is a potent, selective adenosine A1 receptor antagonist that was under development for the treatment of patients with acute decompensated heart failure and renal function impairment. "	( A single supratherapeutic dose of rolofylline does not prolong the QTcF interval in healthy volunteers. Dishy, V; Han, L; Johnson-Levonas, AO; Lai, E; Lazarus Shipitofsky, N; Lewis, W; Lutz, R; Radziszewski, W; Stroh, M; Wagner, J, )	1.85
"Rolofylline is a potent, selective adenosine A1 receptor antagonist that was under development for the treatment of patients with acute decompensated heart failure and renal function impairment. "	( The effects of multiple doses of rolofylline on the single-dose pharmacokinetics of midazolam in healthy subjects. Dishy, V; Dittrich, H; Hwang, E; Johnson-Levonas, AO; Lai, E; Lazarus-Shipitofsky, N; Lutz, R; Radziszewski, W; Stroh, M; Wagner, JA, )	1.86
"Rolofylline is a potent, selective adenosine A1 receptor antagonist that was under development for the treatment of patients with acute congestive heart failure and renal impairment. "	( Simultaneous pharmacokinetic model for rolofylline and both M1-trans and M1-cis metabolites. Hutmacher, MM; Lutz, R; Magara, H; Pang, J; Stone, J; Stroh, M, 2013)	2.1

Excerpt	Reference	Relevance
"Rolofylline treatment was associated with an increased seizure rate, an anticipated complication of A(1)-receptor antagonists. "	( The safety of an adenosine A(1)-receptor antagonist, rolofylline, in patients with acute heart failure and renal impairment: findings from PROTECT. Carson, PE; Cleland, JG; Cotter, G; Davison, BA; Delucca, P; Dittrich, H; Givertz, MM; Hauptman, PJ; Iragui, VJ; Lovett, DH; Mansoor, GA; Massie, BM; Metra, M; Miller, AB; Mohr, JP; O'Connor, CM; Piña, IL; Ponikowski, P; Salerno, CM; Teerlink, JR; Thomson, S; Varosy, PD; Voors, AA; Wolko, D; Zile, MR, 2012)	2.07

Excerpt	Reference	Relevance
" Adverse events (AEs) and serious AEs (SAEs) were recorded from baseline through 7 and 14 days, respectively, and clinical events were adjudicated through 60 days."	( The safety of an adenosine A(1)-receptor antagonist, rolofylline, in patients with acute heart failure and renal impairment: findings from PROTECT. Carson, PE; Cleland, JG; Cotter, G; Davison, BA; Delucca, P; Dittrich, H; Givertz, MM; Hauptman, PJ; Iragui, VJ; Lovett, DH; Mansoor, GA; Massie, BM; Metra, M; Miller, AB; Mohr, JP; O'Connor, CM; Piña, IL; Ponikowski, P; Salerno, CM; Teerlink, JR; Thomson, S; Varosy, PD; Voors, AA; Wolko, D; Zile, MR, 2012)	0.63

Excerpt	Reference	Relevance
" The aim of this investigation was to provide a pharmacokinetic (PK) model for rolofylline and metabolites following intravenous administration to healthy volunteers."	( Simultaneous pharmacokinetic model for rolofylline and both M1-trans and M1-cis metabolites. Hutmacher, MM; Lutz, R; Magara, H; Pang, J; Stone, J; Stroh, M, 2013)	0.89

Excerpt	Reference	Relevance
"01 mg/kg) as well as high oral bioavailability in rat, dog, and cynomolgus monkey."	( Potent and orally bioavailable 8-bicyclo[2.2.2]octylxanthines as adenosine A1 receptor antagonists. Conlon, PR; Dowling, JE; Fure, M; Jayaraj, A; Jin, X; Kiesman, WF; Kim, J; Linden, J; Lutterodt, F; Petter, RC; Smits, G; Sullivan, G; Zhao, J, 2006)	0.33

Excerpt	Relevance	Reference
" There was no significant difference in the pharmacokinetic parameters of KW-3902 (elimination half-life (T1/2), area under the plasma concentration-time curves (AUC0-infinity), total body clearance (CL), mean residence time (MRT) and volume of distribution at steady-state (Vdss) and M1 (Cmax, T1/2, AUC0-infinity and MRT) after injection of these three dosage forms."	( Role of the lipid emulsion on an injectable formulation of lipophilic KW-3902, a newly synthesized adenosine A1-receptor antagonist. Hosokawa, T; Iwata, K; Kato, Y; Mochizuki, H; Yamamoto, Y; Yamauchi, M, 2002)	0.31
" Moreover, the total amount of drug retained in the dispersion system depended on both K(f/b) and the dosing volume."	( Evaluation of the carrier potential for the lipid dispersion system with lipophilic compound. Hosokawa, T; Iwata, K; Kato, Y; Nakamura, A; Yamamoto, Y; Yamauchi, M, 2003)	0.32
" For the IV antiarrhythmic agents that act as ventricular rate control agents, a selective response can be accomplished by careful IV dosing paradigms."	( A1 adenosine receptor antagonists, agonists, and allosteric enhancers. Elzein, E; Kiesman, WF; Zablocki, J, 2009)	0.35
" New insight has been gained regarding volume management, including dosing strategies for intravenous loop diuretics and the role of ultrafiltration in patients with heart failure and renal dysfunction."	( Acute decompensated heart failure: update on new and emerging evidence and directions for future research. Albert, NM; Butler, J; Carson, PE; Collins, SP; Colvin-Adams, M; Dimarco, JP; Ezekowitz, JA; Fang, JC; Givertz, MM; Hernandez, AF; Hershberger, RE; Katz, SD; Krishnamani, R; Rogers, JG; Spertus, JA; Starling, RC; Stevenson, WG; Stough, WG; Sweitzer, NK; Tang, WH; Teerlink, JR; Walsh, MN; Westlake Canary, CA, 2013)	0.39
" The proposed metric-weight loss indexed to diuretic dose-better captures a dose-response relationship."	( Diuretic response in acute heart failure: clinical characteristics and prognostic significance. Bloomfield, DM; Cleland, JG; Cotter, G; Damman, K; Davison, B; Dittrich, HC; Fiuzat, M; Givertz, MM; Hillege, HL; Massie, BM; Metra, M; O'Connor, CM; Ponikowski, P; Teerlink, JR; Valente, MA; Van Veldhuisen, DJ; Voors, AA, 2014)	0.4

Class	Description
oxopurine
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Adenosine receptor A3	Homo sapiens (human)	Ki	4.3900	0.0000	0.9306	10.0000	AID1412906; AID1687722
Adenosine receptor A1	Rattus norvegicus (Norway rat)	Ki	0.0031	0.0001	1.2092	9.9700	AID1687717; AID32033; AID32168; AID32177; AID462305
Adenosine receptor A1	Bos taurus (cattle)	Ki	0.0002	0.0000	0.7131	6.0000	AID31984
Adenosine receptor A2a	Homo sapiens (human)	Ki	0.1968	0.0000	1.0609	9.7920	AID1412904; AID1687718; AID30502; AID30625; AID30790
Adenosine receptor A2b	Homo sapiens (human)	Ki	0.2666	0.0002	1.6352	10.0000	AID1412905; AID1687720; AID30502; AID30625; AID30790
Adenosine receptor A2b	Rattus norvegicus (Norway rat)	Ki	0.4450	0.0006	1.3536	10.0000	AID33563; AID33576
Adenosine receptor A1	Homo sapiens (human)	Ki	0.0006	0.0002	0.9316	10.0000	AID1412903; AID1687716; AID1871327; AID30772; AID462302
Adenosine receptor A2a	Rattus norvegicus (Norway rat)	Ki	0.3600	0.0002	1.4940	10.0000	AID1687719; AID33563; AID33576; AID462306
Adenosine receptor A2a	Cavia porcellus (domestic guinea pig)	Ki	0.2300	0.1100	2.6385	8.0000	AID462309
Adenosine receptor A1	Cavia porcellus (domestic guinea pig)	Ki	0.0012	0.0003	0.4546	6.9000	AID32163; AID32168; AID32289; AID32292; AID462310
Solute carrier family 22 member 6	Homo sapiens (human)	Ki	7.8200	0.0300	3.2043	7.8200	AID678999
Adenosine receptor A1	Mus musculus (house mouse)	Ki	0.0001	0.0001	0.4242	4.4300	AID462308
Solute carrier family 22 member 8	Homo sapiens (human)	Ki	3.7000	0.0400	4.2297	9.0000	AID678987
Solute carrier family 22 member 11	Homo sapiens (human)	Ki	20.7000	0.2000	2.5771	6.1500	AID679295
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Adenosine receptor A2a	Homo sapiens (human)	Kd	0.0830	0.0002	0.4731	9.6000	AID1342781; AID1342783
Adenosine receptor A1	Homo sapiens (human)	Kd	0.0114	0.0002	0.4621	5.9000	AID1342822
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Adenosine receptor A2b	Rattus norvegicus (Norway rat)	Ratio	0.3800	0.0033	0.8292	9.6000	AID33746
Adenosine receptor A2a	Rattus norvegicus (Norway rat)	Ratio	0.3800	0.0033	0.8230	9.6000	AID33746
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
inflammatory response	Adenosine receptor A3	Homo sapiens (human)
signal transduction	Adenosine receptor A3	Homo sapiens (human)
activation of adenylate cyclase activity	Adenosine receptor A3	Homo sapiens (human)
regulation of heart contraction	Adenosine receptor A3	Homo sapiens (human)
negative regulation of cell population proliferation	Adenosine receptor A3	Homo sapiens (human)
response to wounding	Adenosine receptor A3	Homo sapiens (human)
regulation of norepinephrine secretion	Adenosine receptor A3	Homo sapiens (human)
negative regulation of cell migration	Adenosine receptor A3	Homo sapiens (human)
negative regulation of NF-kappaB transcription factor activity	Adenosine receptor A3	Homo sapiens (human)
presynaptic modulation of chemical synaptic transmission	Adenosine receptor A3	Homo sapiens (human)
G protein-coupled adenosine receptor signaling pathway	Adenosine receptor A3	Homo sapiens (human)
G protein-coupled adenosine receptor signaling pathway	Adenosine receptor A1	Bos taurus (cattle)
response to purine-containing compound	Adenosine receptor A1	Bos taurus (cattle)
synaptic transmission, dopaminergic	Adenosine receptor A2a	Homo sapiens (human)
response to amphetamine	Adenosine receptor A2a	Homo sapiens (human)
regulation of DNA-templated transcription	Adenosine receptor A2a	Homo sapiens (human)
phagocytosis	Adenosine receptor A2a	Homo sapiens (human)
apoptotic process	Adenosine receptor A2a	Homo sapiens (human)
inflammatory response	Adenosine receptor A2a	Homo sapiens (human)
cellular defense response	Adenosine receptor A2a	Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	Adenosine receptor A2a	Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathway	Adenosine receptor A2a	Homo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathway	Adenosine receptor A2a	Homo sapiens (human)
cell-cell signaling	Adenosine receptor A2a	Homo sapiens (human)
synaptic transmission, cholinergic	Adenosine receptor A2a	Homo sapiens (human)
central nervous system development	Adenosine receptor A2a	Homo sapiens (human)
blood coagulation	Adenosine receptor A2a	Homo sapiens (human)
sensory perception	Adenosine receptor A2a	Homo sapiens (human)
locomotory behavior	Adenosine receptor A2a	Homo sapiens (human)
blood circulation	Adenosine receptor A2a	Homo sapiens (human)
negative regulation of cell population proliferation	Adenosine receptor A2a	Homo sapiens (human)
response to xenobiotic stimulus	Adenosine receptor A2a	Homo sapiens (human)
response to inorganic substance	Adenosine receptor A2a	Homo sapiens (human)
positive regulation of glutamate secretion	Adenosine receptor A2a	Homo sapiens (human)
positive regulation of acetylcholine secretion, neurotransmission	Adenosine receptor A2a	Homo sapiens (human)
regulation of norepinephrine secretion	Adenosine receptor A2a	Homo sapiens (human)
response to purine-containing compound	Adenosine receptor A2a	Homo sapiens (human)
response to caffeine	Adenosine receptor A2a	Homo sapiens (human)
positive regulation of synaptic transmission, GABAergic	Adenosine receptor A2a	Homo sapiens (human)
synaptic transmission, glutamatergic	Adenosine receptor A2a	Homo sapiens (human)
positive regulation of urine volume	Adenosine receptor A2a	Homo sapiens (human)
vasodilation	Adenosine receptor A2a	Homo sapiens (human)
eating behavior	Adenosine receptor A2a	Homo sapiens (human)
negative regulation of vascular permeability	Adenosine receptor A2a	Homo sapiens (human)
negative regulation of neuron apoptotic process	Adenosine receptor A2a	Homo sapiens (human)
positive regulation of circadian sleep/wake cycle, sleep	Adenosine receptor A2a	Homo sapiens (human)
negative regulation of alpha-beta T cell activation	Adenosine receptor A2a	Homo sapiens (human)
astrocyte activation	Adenosine receptor A2a	Homo sapiens (human)
neuron projection morphogenesis	Adenosine receptor A2a	Homo sapiens (human)
positive regulation of protein secretion	Adenosine receptor A2a	Homo sapiens (human)
negative regulation of inflammatory response	Adenosine receptor A2a	Homo sapiens (human)
regulation of mitochondrial membrane potential	Adenosine receptor A2a	Homo sapiens (human)
membrane depolarization	Adenosine receptor A2a	Homo sapiens (human)
regulation of calcium ion transport	Adenosine receptor A2a	Homo sapiens (human)
positive regulation of synaptic transmission, glutamatergic	Adenosine receptor A2a	Homo sapiens (human)
excitatory postsynaptic potential	Adenosine receptor A2a	Homo sapiens (human)
inhibitory postsynaptic potential	Adenosine receptor A2a	Homo sapiens (human)
prepulse inhibition	Adenosine receptor A2a	Homo sapiens (human)
apoptotic signaling pathway	Adenosine receptor A2a	Homo sapiens (human)
presynaptic modulation of chemical synaptic transmission	Adenosine receptor A2a	Homo sapiens (human)
positive regulation of long-term synaptic potentiation	Adenosine receptor A2a	Homo sapiens (human)
positive regulation of apoptotic signaling pathway	Adenosine receptor A2a	Homo sapiens (human)
G protein-coupled adenosine receptor signaling pathway	Adenosine receptor A2a	Homo sapiens (human)
G protein-coupled adenosine receptor signaling pathway	Adenosine receptor A2b	Homo sapiens (human)
positive regulation of chronic inflammatory response to non-antigenic stimulus	Adenosine receptor A2b	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Adenosine receptor A2b	Homo sapiens (human)
activation of adenylate cyclase activity	Adenosine receptor A2b	Homo sapiens (human)
positive regulation of vascular endothelial growth factor production	Adenosine receptor A2b	Homo sapiens (human)
positive regulation of cGMP-mediated signaling	Adenosine receptor A2b	Homo sapiens (human)
cGMP-mediated signaling	Adenosine receptor A2b	Homo sapiens (human)
positive regulation of chemokine production	Adenosine receptor A2b	Homo sapiens (human)
positive regulation of interleukin-6 production	Adenosine receptor A2b	Homo sapiens (human)
mast cell degranulation	Adenosine receptor A2b	Homo sapiens (human)
positive regulation of mast cell degranulation	Adenosine receptor A2b	Homo sapiens (human)
relaxation of vascular associated smooth muscle	Adenosine receptor A2b	Homo sapiens (human)
presynaptic modulation of chemical synaptic transmission	Adenosine receptor A2b	Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathway	Adenosine receptor A2b	Homo sapiens (human)
vasodilation	Adenosine receptor A2b	Homo sapiens (human)
temperature homeostasis	Adenosine receptor A1	Homo sapiens (human)
response to hypoxia	Adenosine receptor A1	Homo sapiens (human)
G protein-coupled adenosine receptor signaling pathway	Adenosine receptor A1	Homo sapiens (human)
regulation of respiratory gaseous exchange by nervous system process	Adenosine receptor A1	Homo sapiens (human)
negative regulation of acute inflammatory response	Adenosine receptor A1	Homo sapiens (human)
negative regulation of leukocyte migration	Adenosine receptor A1	Homo sapiens (human)
positive regulation of peptide secretion	Adenosine receptor A1	Homo sapiens (human)
positive regulation of systemic arterial blood pressure	Adenosine receptor A1	Homo sapiens (human)
negative regulation of systemic arterial blood pressure	Adenosine receptor A1	Homo sapiens (human)
regulation of glomerular filtration	Adenosine receptor A1	Homo sapiens (human)
protein targeting to membrane	Adenosine receptor A1	Homo sapiens (human)
phagocytosis	Adenosine receptor A1	Homo sapiens (human)
inflammatory response	Adenosine receptor A1	Homo sapiens (human)
signal transduction	Adenosine receptor A1	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	Adenosine receptor A1	Homo sapiens (human)
cell-cell signaling	Adenosine receptor A1	Homo sapiens (human)
nervous system development	Adenosine receptor A1	Homo sapiens (human)
negative regulation of cell population proliferation	Adenosine receptor A1	Homo sapiens (human)
response to inorganic substance	Adenosine receptor A1	Homo sapiens (human)
negative regulation of glutamate secretion	Adenosine receptor A1	Homo sapiens (human)
response to purine-containing compound	Adenosine receptor A1	Homo sapiens (human)
lipid catabolic process	Adenosine receptor A1	Homo sapiens (human)
negative regulation of synaptic transmission, GABAergic	Adenosine receptor A1	Homo sapiens (human)
positive regulation of nucleoside transport	Adenosine receptor A1	Homo sapiens (human)
negative regulation of neurotrophin production	Adenosine receptor A1	Homo sapiens (human)
positive regulation of protein dephosphorylation	Adenosine receptor A1	Homo sapiens (human)
vasodilation	Adenosine receptor A1	Homo sapiens (human)
negative regulation of circadian sleep/wake cycle, non-REM sleep	Adenosine receptor A1	Homo sapiens (human)
negative regulation of apoptotic process	Adenosine receptor A1	Homo sapiens (human)
positive regulation of potassium ion transport	Adenosine receptor A1	Homo sapiens (human)
positive regulation of MAPK cascade	Adenosine receptor A1	Homo sapiens (human)
negative regulation of hormone secretion	Adenosine receptor A1	Homo sapiens (human)
cognition	Adenosine receptor A1	Homo sapiens (human)
leukocyte migration	Adenosine receptor A1	Homo sapiens (human)
detection of temperature stimulus involved in sensory perception of pain	Adenosine receptor A1	Homo sapiens (human)
negative regulation of lipid catabolic process	Adenosine receptor A1	Homo sapiens (human)
positive regulation of lipid catabolic process	Adenosine receptor A1	Homo sapiens (human)
regulation of sensory perception of pain	Adenosine receptor A1	Homo sapiens (human)
negative regulation of synaptic transmission, glutamatergic	Adenosine receptor A1	Homo sapiens (human)
fatty acid homeostasis	Adenosine receptor A1	Homo sapiens (human)
excitatory postsynaptic potential	Adenosine receptor A1	Homo sapiens (human)
long-term synaptic depression	Adenosine receptor A1	Homo sapiens (human)
mucus secretion	Adenosine receptor A1	Homo sapiens (human)
negative regulation of mucus secretion	Adenosine receptor A1	Homo sapiens (human)
triglyceride homeostasis	Adenosine receptor A1	Homo sapiens (human)
regulation of cardiac muscle cell contraction	Adenosine receptor A1	Homo sapiens (human)
apoptotic signaling pathway	Adenosine receptor A1	Homo sapiens (human)
regulation of presynaptic cytosolic calcium ion concentration	Adenosine receptor A1	Homo sapiens (human)
negative regulation of long-term synaptic potentiation	Adenosine receptor A1	Homo sapiens (human)
negative regulation of long-term synaptic depression	Adenosine receptor A1	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Adenosine receptor A1	Homo sapiens (human)
monoatomic anion transport	Solute carrier family 22 member 6	Homo sapiens (human)
response to organic cyclic compound	Solute carrier family 22 member 6	Homo sapiens (human)
inorganic anion transport	Solute carrier family 22 member 6	Homo sapiens (human)
organic anion transport	Solute carrier family 22 member 6	Homo sapiens (human)
prostaglandin transport	Solute carrier family 22 member 6	Homo sapiens (human)
alpha-ketoglutarate transport	Solute carrier family 22 member 6	Homo sapiens (human)
xenobiotic transport	Solute carrier family 22 member 6	Homo sapiens (human)
sodium-independent organic anion transport	Solute carrier family 22 member 6	Homo sapiens (human)
transmembrane transport	Solute carrier family 22 member 6	Homo sapiens (human)
metanephric proximal tubule development	Solute carrier family 22 member 6	Homo sapiens (human)
renal tubular secretion	Solute carrier family 22 member 6	Homo sapiens (human)
monoatomic ion transport	Solute carrier family 22 member 8	Homo sapiens (human)
response to toxic substance	Solute carrier family 22 member 8	Homo sapiens (human)
inorganic anion transport	Solute carrier family 22 member 8	Homo sapiens (human)
prostaglandin transport	Solute carrier family 22 member 8	Homo sapiens (human)
xenobiotic transport	Solute carrier family 22 member 8	Homo sapiens (human)
transmembrane transport	Solute carrier family 22 member 8	Homo sapiens (human)
transport across blood-brain barrier	Solute carrier family 22 member 8	Homo sapiens (human)
monoatomic ion transport	Solute carrier family 22 member 11	Homo sapiens (human)
inorganic anion transport	Solute carrier family 22 member 11	Homo sapiens (human)
organic anion transport	Solute carrier family 22 member 11	Homo sapiens (human)
prostaglandin transport	Solute carrier family 22 member 11	Homo sapiens (human)
urate metabolic process	Solute carrier family 22 member 11	Homo sapiens (human)
transmembrane transport	Solute carrier family 22 member 11	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
G protein-coupled adenosine receptor activity	Adenosine receptor A3	Homo sapiens (human)
G protein-coupled adenosine receptor activity	Adenosine receptor A2a	Homo sapiens (human)
protein binding	Adenosine receptor A2a	Homo sapiens (human)
calmodulin binding	Adenosine receptor A2a	Homo sapiens (human)
lipid binding	Adenosine receptor A2a	Homo sapiens (human)
enzyme binding	Adenosine receptor A2a	Homo sapiens (human)
type 5 metabotropic glutamate receptor binding	Adenosine receptor A2a	Homo sapiens (human)
identical protein binding	Adenosine receptor A2a	Homo sapiens (human)
protein-containing complex binding	Adenosine receptor A2a	Homo sapiens (human)
alpha-actinin binding	Adenosine receptor A2a	Homo sapiens (human)
G protein-coupled adenosine receptor activity	Adenosine receptor A2b	Homo sapiens (human)
protein binding	Adenosine receptor A2b	Homo sapiens (human)
G protein-coupled receptor activity	Adenosine receptor A2b	Homo sapiens (human)
G protein-coupled receptor binding	Adenosine receptor A1	Homo sapiens (human)
purine nucleoside binding	Adenosine receptor A1	Homo sapiens (human)
protein binding	Adenosine receptor A1	Homo sapiens (human)
heat shock protein binding	Adenosine receptor A1	Homo sapiens (human)
G-protein beta/gamma-subunit complex binding	Adenosine receptor A1	Homo sapiens (human)
heterotrimeric G-protein binding	Adenosine receptor A1	Homo sapiens (human)
protein heterodimerization activity	Adenosine receptor A1	Homo sapiens (human)
G protein-coupled adenosine receptor activity	Adenosine receptor A1	Homo sapiens (human)
G protein-coupled adenosine receptor activity	Adenosine receptor A2a	Rattus norvegicus (Norway rat)
solute:inorganic anion antiporter activity	Solute carrier family 22 member 6	Homo sapiens (human)
protein binding	Solute carrier family 22 member 6	Homo sapiens (human)
organic anion transmembrane transporter activity	Solute carrier family 22 member 6	Homo sapiens (human)
prostaglandin transmembrane transporter activity	Solute carrier family 22 member 6	Homo sapiens (human)
alpha-ketoglutarate transmembrane transporter activity	Solute carrier family 22 member 6	Homo sapiens (human)
antiporter activity	Solute carrier family 22 member 6	Homo sapiens (human)
transmembrane transporter activity	Solute carrier family 22 member 6	Homo sapiens (human)
chloride ion binding	Solute carrier family 22 member 6	Homo sapiens (human)
identical protein binding	Solute carrier family 22 member 6	Homo sapiens (human)
xenobiotic transmembrane transporter activity	Solute carrier family 22 member 6	Homo sapiens (human)
sodium-independent organic anion transmembrane transporter activity	Solute carrier family 22 member 6	Homo sapiens (human)
solute:inorganic anion antiporter activity	Solute carrier family 22 member 8	Homo sapiens (human)
organic anion transmembrane transporter activity	Solute carrier family 22 member 8	Homo sapiens (human)
prostaglandin transmembrane transporter activity	Solute carrier family 22 member 8	Homo sapiens (human)
xenobiotic transmembrane transporter activity	Solute carrier family 22 member 8	Homo sapiens (human)
solute:inorganic anion antiporter activity	Solute carrier family 22 member 11	Homo sapiens (human)
protein binding	Solute carrier family 22 member 11	Homo sapiens (human)
organic anion transmembrane transporter activity	Solute carrier family 22 member 11	Homo sapiens (human)
prostaglandin transmembrane transporter activity	Solute carrier family 22 member 11	Homo sapiens (human)
sodium-independent organic anion transmembrane transporter activity	Solute carrier family 22 member 11	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
plasma membrane	Adenosine receptor A3	Homo sapiens (human)
presynaptic membrane	Adenosine receptor A3	Homo sapiens (human)
Schaffer collateral - CA1 synapse	Adenosine receptor A3	Homo sapiens (human)
dendrite	Adenosine receptor A3	Homo sapiens (human)
plasma membrane	Adenosine receptor A3	Homo sapiens (human)
synapse	Adenosine receptor A3	Homo sapiens (human)
plasma membrane	Adenosine receptor A2a	Homo sapiens (human)
intermediate filament	Adenosine receptor A2a	Homo sapiens (human)
plasma membrane	Adenosine receptor A2a	Homo sapiens (human)
membrane	Adenosine receptor A2a	Homo sapiens (human)
dendrite	Adenosine receptor A2a	Homo sapiens (human)
axolemma	Adenosine receptor A2a	Homo sapiens (human)
asymmetric synapse	Adenosine receptor A2a	Homo sapiens (human)
presynaptic membrane	Adenosine receptor A2a	Homo sapiens (human)
neuronal cell body	Adenosine receptor A2a	Homo sapiens (human)
postsynaptic membrane	Adenosine receptor A2a	Homo sapiens (human)
presynaptic active zone	Adenosine receptor A2a	Homo sapiens (human)
glutamatergic synapse	Adenosine receptor A2a	Homo sapiens (human)
plasma membrane	Adenosine receptor A2b	Homo sapiens (human)
Schaffer collateral - CA1 synapse	Adenosine receptor A2b	Homo sapiens (human)
presynapse	Adenosine receptor A2b	Homo sapiens (human)
glutamatergic synapse	Adenosine receptor A2b	Homo sapiens (human)
plasma membrane	Adenosine receptor A2b	Homo sapiens (human)
plasma membrane	Adenosine receptor A1	Homo sapiens (human)
plasma membrane	Adenosine receptor A1	Homo sapiens (human)
basolateral plasma membrane	Adenosine receptor A1	Homo sapiens (human)
axolemma	Adenosine receptor A1	Homo sapiens (human)
asymmetric synapse	Adenosine receptor A1	Homo sapiens (human)
presynaptic membrane	Adenosine receptor A1	Homo sapiens (human)
neuronal cell body	Adenosine receptor A1	Homo sapiens (human)
terminal bouton	Adenosine receptor A1	Homo sapiens (human)
dendritic spine	Adenosine receptor A1	Homo sapiens (human)
calyx of Held	Adenosine receptor A1	Homo sapiens (human)
postsynaptic membrane	Adenosine receptor A1	Homo sapiens (human)
presynaptic active zone	Adenosine receptor A1	Homo sapiens (human)
synapse	Adenosine receptor A1	Homo sapiens (human)
dendrite	Adenosine receptor A1	Homo sapiens (human)
Golgi membrane	Adenosine receptor A2a	Rattus norvegicus (Norway rat)
plasma membrane	Solute carrier family 22 member 6	Homo sapiens (human)
caveola	Solute carrier family 22 member 6	Homo sapiens (human)
basal plasma membrane	Solute carrier family 22 member 6	Homo sapiens (human)
basolateral plasma membrane	Solute carrier family 22 member 6	Homo sapiens (human)
extracellular exosome	Solute carrier family 22 member 6	Homo sapiens (human)
protein-containing complex	Solute carrier family 22 member 6	Homo sapiens (human)
plasma membrane	Solute carrier family 22 member 8	Homo sapiens (human)
basolateral plasma membrane	Solute carrier family 22 member 8	Homo sapiens (human)
apical plasma membrane	Solute carrier family 22 member 8	Homo sapiens (human)
extracellular exosome	Solute carrier family 22 member 8	Homo sapiens (human)
plasma membrane	Solute carrier family 22 member 11	Homo sapiens (human)
external side of plasma membrane	Solute carrier family 22 member 11	Homo sapiens (human)
basal plasma membrane	Solute carrier family 22 member 11	Homo sapiens (human)
apical plasma membrane	Solute carrier family 22 member 11	Homo sapiens (human)
extracellular exosome	Solute carrier family 22 member 11	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (101)

Assay ID	Title	Year	Journal	Article
AID31984	Binding affinity at bovine Adenosine A1 receptor.	2002	Journal of medicinal chemistry, Oct-24, Volume: 45, Issue:22	Synthesis, molecular modeling studies, and pharmacological activity of selective A(1) receptor antagonists.
AID188101	Effect on urinary excretion potassium and sodium after oral administration of 25 mg/kg to rats(potassium and sodium excretion in control rat is 0.138+/-0.008)	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID1427600	Diuretic activity in Wistar rat at 0.1 mg/kg, po via gavage measured after 4 hrs	2017	Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6	Design and synthesis of novel, potent and selective hypoxanthine analogs as adenosine A
AID191191	Oral diuretic activity was measured after oral administration of 1.6 mg/kg to rats(control volume is 1.06+/-0.02)	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID189933	Ratio of urinary excretion value (urinary volume) in treated rats to that in control rats, at a peroral dose of 0.4 mg/Kg	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID190333	Urea nitrogen concentration measured after intraperitoneal administration of 1 mg/kg of compound to rats(vehicle 123.2+/-14.2)	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID189939	Ratio of urinary excretion value (urinary volume) in treated rats to that in control rats, at a peroral dose of 6.25 mg/Kg	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID30772	Inhibition of binding to membranes from HEK293 cells expressing human Adenosine A1 receptor	1997	Journal of medicinal chemistry, Jun-06, Volume: 40, Issue:12	Synthesis and biological evaluation of the enantiomers of the potent and selective A1-adenosine antagonist 1,3-dipropyl-8-[2-(5,6-epoxynorbonyl)]-xanthine.
AID1687722	Displacement of [3H]PSB-11 from human adenosine receptor A3 expressed in CHO cell membranes incubated for 60 mins by radioligand competition assay
AID189925	Ratio of urinary excretion value (Na+ concentration) in treated rats to that in control rats, at a peroral dose of 25 mg/Kg	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID462310	Binding affinity to guinea pig adenosine A1 receptor	2010	Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6	2-Amino-5-benzoyl-4-phenylthiazoles: Development of potent and selective adenosine A1 receptor antagonists.
AID189932	Ratio of urinary excretion value (urinary volume) in treated rats to that in control rats, at a peroral dose of 0.1 mg/Kg	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID462305	Binding affinity to rat adenosine A1 receptor	2010	Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6	2-Amino-5-benzoyl-4-phenylthiazoles: Development of potent and selective adenosine A1 receptor antagonists.
AID1412903	Binding affinity to human adenosine A1 receptor by radioligand displacement assay	2018	MedChemComm, Jun-01, Volume: 9, Issue:6	Tricyclic xanthine derivatives containing a basic substituent: adenosine receptor affinity and drug-related properties.
AID1687718	Displacement of [3H]MSX2 from human adenosine receptor A2A expressed in HEK293 cell membranes incubated for 30 mins by radioligand competition assay
AID189772	Ratio of urinary excretion value (Na+ concentration) in treated rats to that in control rats, at a peroral dose of 0.005 mg/Kg	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID462302	Binding affinity to human adenosine A1 receptor	2010	Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6	2-Amino-5-benzoyl-4-phenylthiazoles: Development of potent and selective adenosine A1 receptor antagonists.
AID1412906	Binding affinity to human adenosine A3 receptor by radioligand displacement assay	2018	MedChemComm, Jun-01, Volume: 9, Issue:6	Tricyclic xanthine derivatives containing a basic substituent: adenosine receptor affinity and drug-related properties.
AID1687716	Displacement of [3H]CCPA from human adenosine receptor A1 expressed in CHO cell membranes incubated for 90 mins by radioligand competition assay
AID188278	Ratio of sodium ion/potassium ion concentration in treated rats to that in control rats, at a peroral dose of 0.4 mg/Kg	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID189929	Ratio of urinary excretion value (urinary volume) in treated rats to that in control rats, at a peroral dose of 0.005 mg/Kg	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID185099	Effect on urinary excretion potassium and sodium after oral administration of 0.005 mg/kg to rats(potassium and sodium excretion in control rat is 0.160+/-0.006)	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID191352	Oral diuretic activity was measured after oral administration of 6.25 mg/kg to rats(control volume is 0.80+/-0.02)	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID188272	Ratio of sodium ion/potassium ion concentration in treated rats to that in control rats, at a peroral dose of 0.0025 mg/Kg	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID32193	Binding affinity towards adenosine A1 receptor in rat forebrain membranes using N6-[3H]cyclohexyladenosine	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID1687717	Displacement of [3H]CCPA from adenosine receptor A1 in rat brain cortex membranes incubated for 90 mins by radioligand competition assay
AID188407	Ratio of sodium ion/potassium ion concentration in urine of rats following 6.25 mg/kg p.o.	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID30790	Inhibition of binding to membranes from HEK293 cells expressing human Adenosine A2 receptor	1997	Journal of medicinal chemistry, Jun-06, Volume: 40, Issue:12	Synthesis and biological evaluation of the enantiomers of the potent and selective A1-adenosine antagonist 1,3-dipropyl-8-[2-(5,6-epoxynorbonyl)]-xanthine.
AID32163	Binding affinity against adenosine A1 receptor using N6-[3H]cyclohexyladenosine as radioligand in guinea pig forebrain membranes	1992	Journal of medicinal chemistry, Mar-06, Volume: 35, Issue:5	8-Polycycloalkyl-1,3-dipropylxanthines as potent and selective antagonists for A1-adenosine receptors.
AID1687720	Displacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assay
AID188248	Effect on urinary excretion potassium and sodium after oral administration of 6.25 mg/kg to rats(potassium and sodium excretion in control rat is 0.146+/-0.005)	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID1871327	Antagonist activity at adenosine A1 receptor (unknown origin)	2022	European journal of medicinal chemistry, Jan-05, Volume: 227	Adenosine receptor antagonists: Recent advances and therapeutic perspective.
AID32289	Binding affinity towards adenosine A1 receptor using N6-[3H]cyclohexyladenosine in guinea pig forebrain membranes	1992	Journal of medicinal chemistry, Sep-18, Volume: 35, Issue:19	7,8-Dihydro-8-ethyl-2-(3-noradamantyl)-4-propyl-1H-imidazo[2,1-i]purin-5(4H)-one: a potent and water-soluble adenosine A1 antagonist.
AID189931	Ratio of urinary excretion value (urinary volume) in treated rats to that in control rats, at a peroral dose of 0.025 mg/Kg	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID188275	Ratio of sodium ion/potassium ion concentration in treated rats to that in control rats, at a peroral dose of 0.025 mg/Kg	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID189928	Ratio of urinary excretion value (urinary volume) in treated rats to that in control rats, at a peroral dose of 0.0025 mg/Kg	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID185098	Effect on urinary excretion potassium and sodium after oral administration of 0.0025 mg/kg to rats(potassium and sodium excretion in control rat is 0.146+/-0.006)	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID174530	Serum creatinine concentration measured after intraperitoneal administration of 1 mg/kg of compound to rats(vehicle 2.75+/-0.43)	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID33752	Ratio of A2 to A1.	1992	Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3	Adenosine receptors: pharmacology, structure-activity relationships, and therapeutic potential.
AID191177	Oral diuretic activity was measured after oral administration of 0.4 mg/kg to rats(control volume is 1.4+/-0.05)	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID32168	Binding affinity for Adenosine A1 receptor from Guinea pig membranes	1997	Journal of medicinal chemistry, Jun-06, Volume: 40, Issue:12	Synthesis and biological evaluation of the enantiomers of the potent and selective A1-adenosine antagonist 1,3-dipropyl-8-[2-(5,6-epoxynorbonyl)]-xanthine.
AID188273	Ratio of sodium ion/potassium ion concentration in treated rats to that in control rats, at a peroral dose of 0.005 mg/Kg	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID679295	TP_TRANSPORTER: inhibition of E1S uptake in OAT4-expressing S2 cells	2002	The Journal of pharmacology and experimental therapeutics, Jun, Volume: 301, Issue:3	Interaction of human organic anion transporters 2 and 4 with organic anion transport inhibitors.
AID232495	Selectivity as ratio of Ki against rat adenosine A2a and A1 receptor binding	1997	Journal of medicinal chemistry, Jun-06, Volume: 40, Issue:12	Synthesis and biological evaluation of the enantiomers of the potent and selective A1-adenosine antagonist 1,3-dipropyl-8-[2-(5,6-epoxynorbonyl)]-xanthine.
AID189920	Ratio of urinary excretion value (Na+ concentration) in treated rats to that in control rats, at a peroral dose of 0.1 mg/Kg	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID192683	Percent inhibition of serum creatinine by the compound given as ratio of Cr value in treated to vehicle treated ones after intraperitoneal administration of 1 mg/kg of compound to rats(vehicle 2.75+/-0.43)	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID187939	Effect on urinary excretion potassium and sodium after oral administration of 0.4 mg/kg to rats(potassium and sodium excretion in control rat is 0.261+/-0.008)	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID21763	Solubility was measured in saline	1992	Journal of medicinal chemistry, Sep-18, Volume: 35, Issue:19	7,8-Dihydro-8-ethyl-2-(3-noradamantyl)-4-propyl-1H-imidazo[2,1-i]purin-5(4H)-one: a potent and water-soluble adenosine A1 antagonist.
AID232493	Selectivity as ratio of Ki against adenosine A2a and A1 receptor binding in guinea pig	1997	Journal of medicinal chemistry, Jun-06, Volume: 40, Issue:12	Synthesis and biological evaluation of the enantiomers of the potent and selective A1-adenosine antagonist 1,3-dipropyl-8-[2-(5,6-epoxynorbonyl)]-xanthine.
AID32033	Binding affinity for Adenosine A1 receptor of rat forebrain	1997	Journal of medicinal chemistry, Jun-06, Volume: 40, Issue:12	Synthesis and biological evaluation of the enantiomers of the potent and selective A1-adenosine antagonist 1,3-dipropyl-8-[2-(5,6-epoxynorbonyl)]-xanthine.
AID189919	Ratio of urinary excretion value (Na+ concentration) in treated rats to that in control rats, at a peroral dose of 0.025 mg/Kg	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID32177	Binding affinity against adenosine A1 receptor using [3H]-CHA or [3H]PIA as radioligand	1992	Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3	Adenosine receptors: pharmacology, structure-activity relationships, and therapeutic potential.
AID232494	Selectivity as ratio of Ki against human adenosine A2a and A1 receptor binding	1997	Journal of medicinal chemistry, Jun-06, Volume: 40, Issue:12	Synthesis and biological evaluation of the enantiomers of the potent and selective A1-adenosine antagonist 1,3-dipropyl-8-[2-(5,6-epoxynorbonyl)]-xanthine.
AID30503	Ratio of binding to adenosine A2 and A1 receptors	1992	Journal of medicinal chemistry, Sep-18, Volume: 35, Issue:19	7,8-Dihydro-8-ethyl-2-(3-noradamantyl)-4-propyl-1H-imidazo[2,1-i]purin-5(4H)-one: a potent and water-soluble adenosine A1 antagonist.
AID189921	Ratio of urinary excretion value (Na+ concentration) in treated rats to that in control rats, at a peroral dose of 0.4 mg/Kg	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID32292	Binding affinity against adenosine A1 receptor in guinea pig forebrain membranes using N6-[3H]cyclohexyladenosine as radioligand	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID188282	Ratio of sodium ion/potassium ion concentration in treated rats to that in control rats, at a peroral dose of 25 mg/Kg	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID189935	Ratio of urinary excretion value (urinary volume) in treated rats to that in control rats, at a peroral dose of 1.6 mg/Kg	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID678962	TP_TRANSPORTER: inhibition of PGF2alpha uptake in OAT2-expressing S2 cells	2002	The Journal of pharmacology and experimental therapeutics, Jun, Volume: 301, Issue:3	Interaction of human organic anion transporters 2 and 4 with organic anion transport inhibitors.
AID188280	Ratio of sodium ion/potassium ion concentration in treated rats to that in control rats, at a peroral dose of 1.6 mg/Kg	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID21767	Solubility of the compound(10 mg) was measured in water(2.5 mL) at 20 degree celsius for 1 hr	1992	Journal of medicinal chemistry, Sep-18, Volume: 35, Issue:19	7,8-Dihydro-8-ethyl-2-(3-noradamantyl)-4-propyl-1H-imidazo[2,1-i]purin-5(4H)-one: a potent and water-soluble adenosine A1 antagonist.
AID189771	Ratio of urinary excretion value (Na+ concentration) in treated rats to that in control rats, at a peroral dose of 0.0025 mg/Kg	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID678999	TP_TRANSPORTER: inhibition of PAH uptake in OAT1-expressing S2 cells	2001	European journal of pharmacology, May-11, Volume: 419, Issue:2-3	Characterization of organic anion transport inhibitors using cells stably expressing human organic anion transporters.
AID191035	Oral diuretic activity was measured after oral administration of 0.025 mg/kg to rats(control volume is 0.82+/-0.05)	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID462308	Binding affinity to mouse adenosine A1 receptor	2010	Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6	2-Amino-5-benzoyl-4-phenylthiazoles: Development of potent and selective adenosine A1 receptor antagonists.
AID33563	Binding affinity against adenosine A2 receptor using N-[3H]-ethyladenosin-5''-uronamide as radioligand in rat striatal membranes.	1992	Journal of medicinal chemistry, Mar-06, Volume: 35, Issue:5	8-Polycycloalkyl-1,3-dipropylxanthines as potent and selective antagonists for A1-adenosine receptors.
AID678987	TP_TRANSPORTER: inhibition of E1S uptake in OAT3-expressing S2 cells	2001	European journal of pharmacology, May-11, Volume: 419, Issue:2-3	Characterization of organic anion transport inhibitors using cells stably expressing human organic anion transporters.
AID191037	Oral diuretic activity was measured after oral administration of 0.1 mg/kg to rats(control volume is 0.92+/-0.05)	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID1687719	Displacement of [3H]MSX2 from adenosine receptor A2A in rat brain striatum membranes incubated for 30 mins by radioligand competition assay
AID187954	Effect on urinary excretion potassium and sodium after oral administration of 1.6 mg/kg to rats(potassium and sodium excretion in control rat is 0.173+/-0.016)	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID191032	Oral diuretic activity was measured after oral administration of 0.005 mg/kg to rats(control volume is 0.76+/-0.01)	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID194944	Percent inhibition of Urea nitrogen by the compound given as ratio of UN value in treated to vehicle treated ones after intraperitoneal administration of 1 mg/kg of compound to rats(vehicle 123.2+/-14.2)	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID1412905	Binding affinity to human adenosine A2B receptor by radioligand displacement assay	2018	MedChemComm, Jun-01, Volume: 9, Issue:6	Tricyclic xanthine derivatives containing a basic substituent: adenosine receptor affinity and drug-related properties.
AID228357	Ratio of Ki at A2 receptor to that of A1 receptor	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID187929	Effect on urinary excretion potassium and sodium after oral administration of 0.1 mg/kg to rats(potassium and sodium excretion in control rat is 0.143+/-0.013)	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID189937	Ratio of urinary excretion value (urinary volume) in treated rats to that in control rats, at a peroral dose of 25 mg/Kg	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID187927	Effect on urinary excretion potassium and sodium after oral administration of 0.025 mg/kg to rats(potassium and sodium excretion in control rat is 0.183+/-0.012)	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID33754	Selectivity is defined as the ratio of Ki(A2 adenosine receptor) / Ki(A1 adenosine receptor)	1992	Journal of medicinal chemistry, Mar-06, Volume: 35, Issue:5	8-Polycycloalkyl-1,3-dipropylxanthines as potent and selective antagonists for A1-adenosine receptors.
AID33576	Binding affinity for Adenosine A2 receptor from rat striatal membranes	1997	Journal of medicinal chemistry, Jun-06, Volume: 40, Issue:12	Synthesis and biological evaluation of the enantiomers of the potent and selective A1-adenosine antagonist 1,3-dipropyl-8-[2-(5,6-epoxynorbonyl)]-xanthine.
AID33587	Binding affinity against adenosine A2 receptor in rat striatal membranes using N-[3H]-ethyladenosin-5''-uronamide as radioligand in the presence of 50 nM cyclopentyladenosine	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID33746	Binding affinity against adenosine A2 receptor using [3H]- NECA as radioligand	1992	Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3	Adenosine receptors: pharmacology, structure-activity relationships, and therapeutic potential.
AID189923	Ratio of urinary excretion value (Na+ concentration) in treated rats to that in control rats, at a peroral dose of 1.6 mg/Kg	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID30625	Binding affinity for Adenosine A2 receptor from Guinea pig membranes	1997	Journal of medicinal chemistry, Jun-06, Volume: 40, Issue:12	Synthesis and biological evaluation of the enantiomers of the potent and selective A1-adenosine antagonist 1,3-dipropyl-8-[2-(5,6-epoxynorbonyl)]-xanthine.
AID191031	Oral diuretic activity was measured after oral administration of 0.0025 mg/kg to rats(control volume is 0.95+/-0.12)	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID1427601	Natriuretic activity in Wistar rat at 0.1 mg/kg, po via gavage measured after 4 hrs	2017	Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6	Design and synthesis of novel, potent and selective hypoxanthine analogs as adenosine A
AID1412904	Binding affinity to human adenosine A2A receptor by radioligand displacement assay	2018	MedChemComm, Jun-01, Volume: 9, Issue:6	Tricyclic xanthine derivatives containing a basic substituent: adenosine receptor affinity and drug-related properties.
AID191197	Oral diuretic activity was measured after oral administration of 25 mg/kg to rats(control volume is 0.66+/-0.04)	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID30502	Binding affinity for adenosine A2 receptor using N-[3H]-ethyladenosin-5''-uronamide in guinea pig forebrain membranes	1992	Journal of medicinal chemistry, Sep-18, Volume: 35, Issue:19	7,8-Dihydro-8-ethyl-2-(3-noradamantyl)-4-propyl-1H-imidazo[2,1-i]purin-5(4H)-one: a potent and water-soluble adenosine A1 antagonist.
AID462309	Binding affinity to guinea pig adenosine A2A receptor	2010	Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6	2-Amino-5-benzoyl-4-phenylthiazoles: Development of potent and selective adenosine A1 receptor antagonists.
AID188277	Ratio of sodium ion/potassium ion concentration in treated rats to that in control rats, at a peroral dose of 0.1 mg/Kg	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID189927	Ratio of urinary excretion value (Na+ concentration) in treated rats to that in control rats, at a peroral dose of 6.25 mg/Kg	1992	Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16	Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
AID462306	Binding affinity to rat adenosine A2A receptor	2010	Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6	2-Amino-5-benzoyl-4-phenylthiazoles: Development of potent and selective adenosine A1 receptor antagonists.
AID1345685	Human A1 receptor (Adenosine receptors)	2006	Journal of medicinal chemistry, Nov-30, Volume: 49, Issue:24	Potent and orally bioavailable 8-bicyclo[2.2.2]octylxanthines as adenosine A1 receptor antagonists.
AID1345618	Human A2A receptor (Adenosine receptors)	2006	Journal of medicinal chemistry, Nov-30, Volume: 49, Issue:24	Potent and orally bioavailable 8-bicyclo[2.2.2]octylxanthines as adenosine A1 receptor antagonists.
AID1345721	Human A2B receptor (Adenosine receptors)	2006	Journal of medicinal chemistry, Nov-30, Volume: 49, Issue:24	Potent and orally bioavailable 8-bicyclo[2.2.2]octylxanthines as adenosine A1 receptor antagonists.
AID1345618	Human A2A receptor (Adenosine receptors)	2003	The Journal of biological chemistry, Dec-19, Volume: 278, Issue:51	Heterodimerization of substance P and mu-opioid receptors regulates receptor trafficking and resensitization.
AID1345690	Rat A2A receptor (Adenosine receptors)	2006	Bioorganic & medicinal chemistry, Jun-01, Volume: 14, Issue:11	Norbornyllactone-substituted xanthines as adenosine A(1) receptor antagonists.
AID1345685	Human A1 receptor (Adenosine receptors)	1997	Journal of medicinal chemistry, Jun-06, Volume: 40, Issue:12	Synthesis and biological evaluation of the enantiomers of the potent and selective A1-adenosine antagonist 1,3-dipropyl-8-[2-(5,6-epoxynorbonyl)]-xanthine.
AID1345630	Rat A1 receptor (Adenosine receptors)	1997	Journal of medicinal chemistry, Jun-06, Volume: 40, Issue:12	Synthesis and biological evaluation of the enantiomers of the potent and selective A1-adenosine antagonist 1,3-dipropyl-8-[2-(5,6-epoxynorbonyl)]-xanthine.
AID1345822	Human A3 receptor (Adenosine receptors)	2006	Journal of medicinal chemistry, Nov-30, Volume: 49, Issue:24	Potent and orally bioavailable 8-bicyclo[2.2.2]octylxanthines as adenosine A1 receptor antagonists.
AID1345690	Rat A2A receptor (Adenosine receptors)	1997	Journal of medicinal chemistry, Jun-06, Volume: 40, Issue:12	Synthesis and biological evaluation of the enantiomers of the potent and selective A1-adenosine antagonist 1,3-dipropyl-8-[2-(5,6-epoxynorbonyl)]-xanthine.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	31 (28.44)	18.2507
2000's	36 (33.03)	29.6817
2010's	40 (36.70)	24.3611
2020's	2 (1.83)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	29 (25.89%)	5.53%
Reviews	9 (8.04%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	74 (66.07%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (7)

Trial Overview

Trial	Phase	Enrollment	Study Type	Start Date	Status
A Randomized, Double-Blind, Placebo Controlled Dose-Ranging Study of The Effects of MK7418, Both as Monotherapy and in Combination With Furosemide, On Diuresis and Renal Function in Patients With Congestive Heart Failure (CHF) And Renal Impairment Treated [NCT00652782]	Phase 2	160 participants (Actual)	Interventional	2004-12-31	Completed
A Multicenter, Randomized, Double-blind, Placebo-controlled Study of the Hemodynamic Effects of Rolofylline Injectable Emulsion in the Treatment of Patients With Heart Failure [NCT00729222]	Phase 2	60 participants (Actual)	Interventional	2008-11-30	Completed
Effect of KW-3902IV in Combination With IV Furosemide on Renal Function in Subjects With Congestive Heart Failure (CHF) and Renal Impairment [NCT00159614]	Phase 2	30 participants	Interventional	2005-09-30	Completed
A Multicenter, Randomized, Double-blind, Placebo-controlled Study of the Effects of KW-3902 Injectable Emulsion on Heart Failure Signs and Symptoms and Renal Function in Subjects With Acute Heart Failure Syndrome and Renal Impairment Who Are Hospitalized [NCT00354458]	Phase 3	1,102 participants (Actual)	Interventional	2006-10-31	Completed
A Randomized, Double-Blind, Placebo Controlled, Dose Escalation Study of the Effects of KW-3902 on Diuresis in Patients With Congestive Heart Failure (CHF) Refractory to High Dose Diuretic Therapy [NCT00159627]	Phase 2	52 participants	Interventional	2004-08-31	Completed
A Multicenter, Randomized, Double-Blind, Placebo-Controlled Study of the Effects of KW-3902 Injectable Emulsion on Heart Failure Signs and Symptoms, Diuresis, Renal Function, and Clinical Outcomes in Subjects Hospitalized With Worsening Renal Function and [NCT00443690]	Phase 3	480 participants (Anticipated)	Interventional	2007-08-31	Completed
A Multicenter, Randomized, Double-blind, Placebo-controlled Study of the Effects of KW-3902 Injectable Emulsion on Heart Failure Signs and Symptoms and Renal Function in Subjects With Acute Heart Failure Syndrome and Renal Impairment Who Are Hospitalized [NCT00328692]	Phase 3	932 participants (Actual)	Interventional	2006-08-31	Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
adenine [no description available]	2.41	2	0	6-aminopurines; purine nucleobase	Daphnia magna metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite
carbon monoxide Carbon Monoxide: Carbon monoxide (CO). A poisonous colorless, odorless, tasteless gas. It combines with hemoglobin to form carboxyhemoglobin, which has no oxygen carrying capacity. The resultant oxygen deprivation causes headache, dizziness, decreased pulse and respiratory rates, unconsciousness, and death. (From Merck Index, 11th ed). carbon monoxide : A one-carbon compound in which the carbon is joined only to a single oxygen. It is a colourless, odourless, tasteless, toxic gas.	1.99	1	0	carbon oxide; gas molecular entity; one-carbon compound	biomarker; EC 1.9.3.1 (cytochrome c oxidase) inhibitor; human metabolite; ligand; metabolite; mitochondrial respiratory-chain inhibitor; mouse metabolite; neurotoxin; neurotransmitter; P450 inhibitor; probe; signalling molecule; vasodilator agent
chlorine chloride : A halide anion formed when chlorine picks up an electron to form an an anion.	4.43	1	1	halide anion; monoatomic chlorine	cofactor; Escherichia coli metabolite; human metabolite
glycerol Moon: The natural satellite of the planet Earth. It includes the lunar cycles or phases, the lunar month, lunar landscapes, geography, and soil.	2.38	2	0	alditol; triol	algal metabolite; detergent; Escherichia coli metabolite; geroprotector; human metabolite; mouse metabolite; osmolyte; Saccharomyces cerevisiae metabolite; solvent
urea pseudourea: clinical use; structure. isourea : A carboximidic acid that is the imidic acid tautomer of urea, H2NC(=NH)OH, and its hydrocarbyl derivatives.	7.22	3	2	isourea; monocarboxylic acid amide; one-carbon compound	Daphnia magna metabolite; Escherichia coli metabolite; fertilizer; flour treatment agent; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite
xanthine 7H-xanthine : An oxopurine in which the purine ring is substituted by oxo groups at positions 2 and 6 and N-7 is protonated.. 9H-xanthine : An oxopurine in which the purine ring is substituted by oxo groups at positions 2 and 6 and N-9 is protonated.	2.03	1	0	xanthine	Saccharomyces cerevisiae metabolite
1,3-dipropyl-8-cyclopentylxanthine DPCPX : An oxopurine that is 7H-xanthine substituted at positions 1 and 3 by propyl groups and at position 8 by a cyclohexyl group.	5.04	13	0	oxopurine	adenosine A1 receptor antagonist; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor
1,3-dipropyl-8-(4-sulfophenyl)xanthine 1,3-dipropyl-8-(4-sulfophenyl)xanthine: adenosine receptor antagonist	2	1	0
enprofylline enprofylline : Xanthine bearing a propyl substituent at position 3. A bronchodilator, it is used for the symptomatic treatment of asthma and chronic obstructive pulmonary disease, and in the management of cerebrovascular insufficiency, sickle cell disease, and diabetic neuropathy.	3.51	1	0	oxopurine	anti-arrhythmia drug; anti-asthmatic drug; bronchodilator agent; non-steroidal anti-inflammatory drug
8-(4-sulfophenyl)theophylline 8-(4-sulfophenyl)theophylline: adenosine antagonist	3.48	2	0
8-cyclopentyl-1,3-dimethylxanthine 8-cyclopentyl-1,3-dimethylxanthine: prolongs epileptic seizures in rats	3.48	2	0	oxopurine
8-phenyltheophylline 8-phenyltheophylline: purinergic P1 receptor antagonist	3.48	2	0
diatrizoic acid Diatrizoate: A commonly used x-ray contrast medium. As DIATRIZOATE MEGLUMINE and as Diatrizoate sodium, it is used for gastrointestinal studies, angiography, and urography.. amidotrizoic acid : A member of the class of benzoic acids that is benzoic acid having iodo substituents at the 2-, 4- and 6-positions and acetamido substituents at the 3- and 5-positions. It is used, mainly as its N-methylglucamine and sodium salts, as an X-ray contrast medium in gastrointestinal studies, angiography, and urography.	2.41	2	0	acetamides; benzoic acids; organoiodine compound	environmental contaminant; radioopaque medium; xenobiotic
p-aminohippuric acid p-Aminohippuric Acid: The glycine amide of 4-aminobenzoic acid. Its sodium salt is used as a diagnostic aid to measure effective renal plasma flow (ERPF) and excretory capacity.. p-aminohippurate : A hippurate that is the conjugate base of p-aminohippuric acid, arising from deprotonation of the carboxy group.. p-aminohippuric acid : An N-acylglycine that is the 4-amino derivative of hippuric acid; used as a diagnostic agent in the measurement of renal plasma flow.	2.39	2	0	N-acylglycine	Daphnia magna metabolite
theophylline [no description available]	5.23	9	0	dimethylxanthine	adenosine receptor antagonist; anti-asthmatic drug; anti-inflammatory agent; bronchodilator agent; drug metabolite; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; fungal metabolite; human blood serum metabolite; immunomodulator; muscle relaxant; vasodilator agent
bumetanide [no description available]	4.4	1	1	amino acid; benzoic acids; sulfonamide	diuretic; EC 3.6.3.49 (channel-conductance-controlling ATPase) inhibitor
caffeine [no description available]	4.88	6	0	purine alkaloid; trimethylxanthine	adenosine A2A receptor antagonist; adenosine receptor antagonist; adjuvant; central nervous system stimulant; diuretic; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; environmental contaminant; food additive; fungal metabolite; geroprotector; human blood serum metabolite; mouse metabolite; mutagen; plant metabolite; psychotropic drug; ryanodine receptor agonist; xenobiotic
verapamil Verapamil: A calcium channel blocker that is a class IV anti-arrhythmia agent.. verapamil : A racemate comprising equimolar amounts of dexverapamil and (S)-verapamil. An L-type calcium channel blocker of the phenylalkylamine class, it is used (particularly as the hydrochloride salt) in the treatment of hypertension, angina pectoris and cardiac arrhythmia, and as a preventive medication for migraine.. 2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile : A tertiary amino compound that is 3,4-dimethoxyphenylethylamine in which the hydrogens attached to the nitrogen are replaced by a methyl group and a 4-cyano-4-(3,4-dimethoxyphenyl)-5-methylhexyl group.	2.15	1	0	aromatic ether; nitrile; polyether; tertiary amino compound
cgs 15943 9-chloro-2-(2-furyl)-(1,2,4)triazolo(1,5-c)quinazolin-5-imine: non-xanthine triazoloquinazoline adenosine antagonist. CGS 15943 : A member of the class of triazoloquinazolines that is [1,2,4]triazolo[1,5-c]quinazoline substited at positions 2, 5 and 9 by furan-2-yl, amino and chloro groups respectively. A potent antagonist at adenosine A1 and adenosine A2A receptors.	3.78	3	0	aromatic amine; biaryl; furans; organochlorine compound; primary amino compound; quinazolines; triazoloquinazoline	adenosine A1 receptor antagonist; adenosine A2A receptor antagonist; antineoplastic agent; central nervous system stimulant
dipyridamole Dipyridamole: A phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells. Dipyridamole also potentiates the antiaggregating action of prostacyclin. (From AMA Drug Evaluations Annual, 1994, p752). dipyridamole : A pyrimidopyrimidine that is 2,2',2'',2'''-(pyrimido[5,4-d]pyrimidine-2,6-diyldinitrilo)tetraethanol substituted by piperidin-1-yl groups at positions 4 and 8 respectively. A vasodilator agent, it inhibits the formation of blood clots.	2.43	2	0	piperidines; pyrimidopyrimidine; tertiary amino compound; tetrol	adenosine phosphodiesterase inhibitor; EC 3.5.4.4 (adenosine deaminase) inhibitor; platelet aggregation inhibitor; vasodilator agent
9-(2-hydroxy-3-nonyl)adenine 9-(2-hydroxy-3-nonyl)adenine: specific inhibitor of adenosine deaminase	1.99	1	0
furosemide Furosemide: A benzoic-sulfonamide-furan. It is a diuretic with fast onset and short duration that is used for EDEMA and chronic RENAL INSUFFICIENCY.. furosemide : A chlorobenzoic acid that is 4-chlorobenzoic acid substituted by a (furan-2-ylmethyl)amino and a sulfamoyl group at position 2 and 5 respectively. It is a diuretic used in the treatment of congestive heart failure.	10.57	18	5	chlorobenzoic acid; furans; sulfonamide	environmental contaminant; loop diuretic; xenobiotic
gentamicin Gentamicins: A complex of closely related aminoglycosides obtained from MICROMONOSPORA purpurea and related species. They are broad-spectrum antibiotics, but may cause ear and kidney damage. They act to inhibit PROTEIN BIOSYNTHESIS.	2.4	2	0
iotrolan iotrolan: nonionic, isotonic contrast medium designed for intrathecal use; RN given refers to cpd without isomeric designation; DL-3-117 refers to stereoisomer; structure given in first source	2	1	0	organic molecular entity
2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one: specific inhibitor of phosphatidylinositol 3-kinase; structure in first source	2.15	1	0	chromones; morpholines; organochlorine compound	autophagy inhibitor; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor; geroprotector
nitroglycerin Nitroglycerin: A volatile vasodilator which relieves ANGINA PECTORIS by stimulating GUANYLATE CYCLASE and lowering cytosolic calcium. It is also sometimes used for TOCOLYSIS and explosives.. nitroglycerol : A nitrate ester that is glycerol in which nitro group(s) replace the hydrogen(s) attached to one or more of the hydroxy groups.. nitroglycerin : A nitroglycerol that is glycerol in which the hydrogen atoms of all three hydroxy groups are replaced by nitro groups. It acts as a prodrug, releasing nitric oxide to open blood vessels and so alleviate heart pain.	3.18	1	0	nitroglycerol	explosive; muscle relaxant; nitric oxide donor; prodrug; tocolytic agent; vasodilator agent; xenobiotic
probenecid Probenecid: The prototypical uricosuric agent. It inhibits the renal excretion of organic anions and reduces tubular reabsorption of urate. Probenecid has also been used to treat patients with renal impairment, and, because it reduces the renal tubular excretion of other drugs, has been used as an adjunct to antibacterial therapy.. probenecid : A sulfonamide in which the nitrogen of 4-sulfamoylbenzoic acid is substituted with two propyl groups.	2.41	2	0	benzoic acids; sulfonamide	uricosuric drug
theobromine Theobromine: 3,7-Dimethylxanthine. The principle alkaloid in Theobroma cacao (the cacao bean) and other plants. A xanthine alkaloid that is used as a bronchodilator and as a vasodilator. It has a weaker diuretic activity than THEOPHYLLINE and is also a less powerful stimulant of smooth muscle. It has practically no stimulant effect on the central nervous system. It was formerly used as a diuretic and in the treatment of angina pectoris and hypertension. (From Martindale, The Extra Pharmacopoeia, 30th ed, pp1318-9). theobromine : A dimethylxanthine having the two methyl groups located at positions 3 and 7. A purine alkaloid derived from the cacao plant, it is found in chocolate, as well as in a number of other foods, and is a vasodilator, diuretic and heart stimulator.	2.03	1	0	dimethylxanthine	adenosine receptor antagonist; bronchodilator agent; food component; human blood serum metabolite; mouse metabolite; plant metabolite; vasodilator agent
trichlormethiazide Trichlormethiazide: A thiazide diuretic with properties similar to those of HYDROCHLOROTHIAZIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p830). trichlormethiazide : A benzothiadiazine, hydrogenated at positions 2, 3 and 4 and substituted with an aminosulfonyl group at C-7, a chloro substituent at C-6 and a dichloromethyl group at C-3 and with S-1 as an S,S-dioxide. A sulfonamide antibiotic, it is used as a diuretic to treat oedema (including that associated with heart failure) and hypertension.	3.49	8	0	benzothiadiazine; sulfonamide antibiotic	antihypertensive agent; diuretic
8-(4-((2-aminoethyl)aminocarbonylmethyloxy)phenyl)-1,3-dipropylxanthine 8-(4-((2-aminoethyl)aminocarbonylmethyloxy)phenyl)-1,3-dipropylxanthine: adenosine receptor antagonist	3.78	3	0
cephaloridine Cephaloridine: A cephalosporin antibiotic.. cefaloridine : A cephalosporin compound having pyridinium-1-ylmethyl and 2-thienylacetamido side-groups. A first-generation semisynthetic derivative of cephalosporin C.	1.98	1	0	beta-lactam antibiotic allergen; cephalosporin; semisynthetic derivative	antibacterial drug
puromycin aminonucleoside 3'-amino-3'-deoxy-N(6),N(6)-dimethyladenosine: structure in first source. 3'-amino-3'-deoxy-N(6),N(6)-dimethyladenosine : Puromycin derivative that lacks the methoxyphenylalanyl group on the amine of the sugar ring.	1.98	1	0	3'-deoxyribonucleoside; adenosines
adenosine diphosphate Adenosine Diphosphate: Adenosine 5'-(trihydrogen diphosphate). An adenine nucleotide containing two phosphate groups esterified to the sugar moiety at the 5'-position.	1.99	1	0	adenosine 5'-phosphate; purine ribonucleoside 5'-diphosphate	fundamental metabolite; human metabolite
levodopa Levodopa: The naturally occurring form of DIHYDROXYPHENYLALANINE and the immediate precursor of DOPAMINE. Unlike dopamine itself, it can be taken orally and crosses the blood-brain barrier. It is rapidly taken up by dopaminergic neurons and converted to DOPAMINE. It is used for the treatment of PARKINSONIAN DISORDERS and is usually given with agents that inhibit its conversion to dopamine outside of the central nervous system.. L-dopa : An optically active form of dopa having L-configuration. Used to treat the stiffness, tremors, spasms, and poor muscle control of Parkinson's disease	3.51	1	0	amino acid zwitterion; dopa; L-tyrosine derivative; non-proteinogenic L-alpha-amino acid	allelochemical; antidyskinesia agent; antiparkinson drug; dopaminergic agent; hapten; human metabolite; mouse metabolite; neurotoxin; plant growth retardant; plant metabolite; prodrug
phlorhizin [no description available]	1.98	1	0	aryl beta-D-glucoside; dihydrochalcones; monosaccharide derivative	antioxidant; plant metabolite
methylene blue Methylene Blue: A compound consisting of dark green crystals or crystalline powder, having a bronze-like luster. Solutions in water or alcohol have a deep blue color. Methylene blue is used as a bacteriologic stain and as an indicator. It inhibits GUANYLATE CYCLASE, and has been used to treat cyanide poisoning and to lower levels of METHEMOGLOBIN.. methylene blue : An organic chloride salt having 3,7-bis(dimethylamino)phenothiazin-5-ium as the counterion. A commonly used dye that also exhibits antioxidant, antimalarial, antidepressant and cardioprotective properties.	1.99	1	0	organic chloride salt	acid-base indicator; antidepressant; antimalarial; antimicrobial agent; antioxidant; cardioprotective agent; EC 1.4.3.4 (monoamine oxidase) inhibitor; EC 3.1.1.8 (cholinesterase) inhibitor; EC 4.6.1.2 (guanylate cyclase) inhibitor; fluorochrome; histological dye; neuroprotective agent; physical tracer
mannitol [no description available]	2	1	0	mannitol	allergen; antiglaucoma drug; compatible osmolytes; Escherichia coli metabolite; food anticaking agent; food bulking agent; food humectant; food stabiliser; food thickening agent; hapten; metabolite; osmotic diuretic; sweetening agent
arginine Arginine: An essential amino acid that is physiologically active in the L-form.. arginine : An alpha-amino acid that is glycine in which the alpha-is substituted by a 3-guanidinopropyl group.	1.99	1	0	arginine; glutamine family amino acid; L-alpha-amino acid; proteinogenic amino acid	biomarker; Escherichia coli metabolite; micronutrient; mouse metabolite; nutraceutical
pyrroles 1H-pyrrole : A tautomer of pyrrole that has the double bonds at positions 2 and 4.. pyrrole : A five-membered monocyclic heteroarene comprising one NH and four CH units which forms the parent compound of the pyrrole group of compounds. Its five-membered ring structure has three tautomers. A 'closed class'.. azole : Any monocyclic heteroarene consisting of a five-membered ring containing nitrogen. Azoles can also contain one or more other non-carbon atoms, such as nitrogen, sulfur or oxygen.	2.03	1	0	pyrrole; secondary amine
2-chloroadenosine 5-chloroformycin A: structure given in first source	3.08	1	0	purine nucleoside
quinazolines Quinazolines: A group of aromatic heterocyclic compounds that contain a bicyclic structure with two fused six-membered aromatic rings, a benzene ring and a pyrimidine ring.. quinazoline : A mancude organic heterobicyclic parent that is naphthalene in which the carbon atoms at positions 1 and 3 have been replaced by nitrogen atoms.. quinazolines : Any organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives.	2.01	1	0	azaarene; mancude organic heterobicyclic parent; ortho-fused heteroarene; quinazolines
adamantane Adamantane: A tricyclo bridged hydrocarbon.	2.41	2	0	adamantanes; polycyclic alkane
alpha-aminopyridine alpha-aminopyridine: RN given refers to parent cpd; structure in Merck Index, 9th ed, #485. aminopyridine : Compounds containing a pyridine skeleton substituted by one or more amine groups.	2.08	1	0
canrenone Canrenone: A synthetic pregnadiene compound with anti-aldosterone activity.	3.42	1	1	steroid lactone
vancomycin Vancomycin: Antibacterial obtained from Streptomyces orientalis. It is a glycopeptide related to RISTOCETIN that inhibits bacterial cell wall assembly and is toxic to kidneys and the inner ear.. vancomycin : A complex glycopeptide from Streptomyces orientalis. It inhibits a specific step in the synthesis of the peptidoglycan layer in the Gram-positive bacteria Staphylococcus aureus and Clostridium difficile.	2.03	1	0	glycopeptide	antibacterial drug; antimicrobial agent; bacterial metabolite
benzolamide Benzolamide: Selective renal carbonic anhydrase inhibitor. It may also be of use in certain cases of respiratory failure.	2.03	1	0
glucaric acid Glucaric Acid: A sugar acid derived from D-glucose in which both the aldehydic carbon atom and the carbon atom bearing the primary hydroxyl group are oxidized to carboxylic acid groups.. D-glucaric acid : The D-enantiomer of glucaric acid.. glucaric acid : A hexaric acid derived by oxidation of sugar such as glucose with nitric acid.	2.03	1	0	glucaric acid	antineoplastic agent
ng-nitroarginine methyl ester NG-Nitroarginine Methyl Ester: A non-selective inhibitor of nitric oxide synthase. It has been used experimentally to induce hypertension.	2	1	0	alpha-amino acid ester; L-arginine derivative; methyl ester; N-nitro compound	EC 1.14.13.39 (nitric oxide synthase) inhibitor
torsemide Torsemide: A pyridine and sulfonamide derivative that acts as a sodium-potassium chloride symporter inhibitor (loop diuretic). It is used for the treatment of EDEMA associated with CONGESTIVE HEART FAILURE; CHRONIC RENAL INSUFFICIENCY; and LIVER DISEASES. It is also used for the management of HYPERTENSION.. torasemide : An N-sulfonylurea obtained by formal condensation of [(3-methylphenyl)amino]pyridine-3-sulfonic acid with the free amino group of N-isopropylurea. It is a potent loop diuretic used for the treatment of hypertension and edema in patients with congestive heart failure.	4.4	1	1	aminopyridine; N-sulfonylurea; secondary amino compound	antihypertensive agent; loop diuretic
atorvastatin [no description available]	2.03	1	0	aromatic amide; dihydroxy monocarboxylic acid; monofluorobenzenes; pyrroles; statin (synthetic)	environmental contaminant; xenobiotic
simendan Simendan: A hydrazone and pyridazine derivative; the levo-form is a phosphodiesterase III inhibitor, calcium-sensitizing agent, and inotropic agent that is used in the treatment of HEART FAILURE.	3.18	1	0
adenosine quinquefolan B: isolated from roots of Panax quinquefolium L.; RN not in Chemline 10/87; RN from Toxlit	5.78	21	0	adenosines; purines D-ribonucleoside	analgesic; anti-arrhythmia drug; fundamental metabolite; human metabolite; vasodilator agent
4-pentenoic acid 4-pentenoic acid: inhibitor of fatty acid oxidation; RN given refers to parent cpd. pent-4-enoic acid : A pentenoic acid having the double bond at position 4.	2	1	0	pentenoic acid
u 37883a U 37883A: an antagonist of vascular ATP-sensitive potassium channel openers; structure given in first source	1.99	1	0
triazoles Triazoles: Heterocyclic compounds containing a five-membered ring with two carbon atoms and three nitrogen atoms with the molecular formula C2H3N3.. triazoles : An azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms.	2.01	1	0	1,2,3-triazole
betamipron [no description available]	2.41	2	0	organonitrogen compound; organooxygen compound
adenosine 5'-methylenediphosphate [no description available]	1.99	1	0	nucleoside diphosphate analogue
1,3-dipropyl-8-(2-amino-4-chlorophenyl)xanthine [no description available]	3.08	1	0
phenylisopropyladenosine [no description available]	3.08	1	0	aromatic amine; benzenes; hydrocarbyladenosine; purine nucleoside; secondary amino compound	adenosine A1 receptor agonist; neuroprotective agent
3,7-dimethyl-1-propargylxanthine 3,7-dimethyl-1-propargylxanthine: potent & selective in vivo antagonist of adenosine analogs	3.5	2	0
n(6)-phenyladenosine [no description available]	3.08	1	0	purine nucleoside
n-(2-(dimethylamino)ethyl)-n-methyl-4-(2,3,6,7-tetrahydro-2,6-dioxo-1,3-dipropyl-1h-purin-8-yl)benzenesulfonamide N-(2-(dimethylamino)ethyl)-N-methyl-4-(2,3,6,7-tetrahydro-2,6-dioxo-1,3-dipropyl-1H-purin-8-yl)benzenesulfonamide: structure given in first source; purinergic receptor antagonist	1.98	1	0
kf 17837s KF 17837: adenosine A(2a) receptor antagonist; KF17837S is the equilibrium mixture of (E)- and (Z)-isomers	4.16	6	0
2-chloro-n(6)cyclopentyladenosine 2-chloro-N(6)cyclopentyladenosine: highly selective agonist at A1 adenosine receptors	3.08	1	0
cp 66713 CP 66713: adenosine receptor antagonist; structure given in first source	3.48	2	0
adenosine amine congener adenosine amine congener: a highly potent & selective adenosine A1 receptor agonist	3.49	2	0
8-(4-carboxymethyloxy)phenyl-1,3-dipropylxanthine 8-(4-carboxymethyloxy)phenyl-1,3-dipropylxanthine: used to localize adenosine receptors in the brain	3.08	1	0
8-(dicyclopropylmethyl)-1,3-dipropylxanthine 8-(dicyclopropylmethyl)-1,3-dipropylxanthine: selective A1 adenosine receptor antagonist; structure given in first source	3.99	4	0
kfm 19 KFM 19: a potential cognitive enhancer and a selective adenosine A1 receptor antagonist	3.78	3	0
2-(1-octynyl)adenosine YT 146: an adenosine receptor agonist; structure given in first source	3.08	1	0
tezosentan tezosentan: structure in first source	3.18	1	0
n(w)-nitroarginine benzyl ester N(w)-nitroarginine benzyl ester: potent irreversible inhibitor of endothelium dependent relaxation	1.99	1	0
cvt 124 1,3-dipropyl-8-(2-(5,6-epoxy)norbornyl)xanthine: CVT-124 is the (S)-isomer	4.05	2	0
r 64719 soluflazine: nucleoside transport inhibitor; analog of mioflazine	1.99	1	0
1,3-dipropylxanthine 1,3-dipropylxanthine: has high affinity for adenosine receptors; structure given in first source	1.98	1	0
angiotensin ii Giapreza: injectable form of angiotensin II used to increase blood pressure in adult patients with septic or other distributive shock. Ile(5)-angiotensin II : An angiotensin II that acts on the central nervous system (PDB entry: 1N9V).	2.01	1	0	amino acid zwitterion; angiotensin II	human metabolite
zm 241385 ZM 241385: a high affinity radioligand selective for the A2a adenosine receptor	3.51	1	0	diamino-1,3,5-triazine
sch 58261 [no description available]	3.51	1	0	triazolopyrimidines
tolvaptan [no description available]	8.14	4	3	benzazepine; benzenedicarboxamide	aquaretic; vasopressin receptor antagonist
8-cyclohexylcaffeine [no description available]	3.08	1	0
adenosine 5'-o-(3-thiotriphosphate) adenosine 5'-O-(3-thiotriphosphate): RN given refers to cpd with unspecified locant for thio group; see also records for 1-thio & 2-thio-isomers. adenosine 5'-[gamma-thio]triphosphate : A nucleoside triphosphate analogue that is ATP in which one of the oxygens attached to 3-phosphate group is replaced by sulfur.	2.01	1	0	nucleoside triphosphate analogue
n-formylmethionine leucyl-phenylalanine N-Formylmethionine Leucyl-Phenylalanine: A formylated tripeptide originally isolated from bacterial filtrates that is positively chemotactic to polymorphonuclear leucocytes, and causes them to release lysosomal enzymes and become metabolically activated.. N-formyl-L-methionyl-L-leucyl-L-phenylalanine : A tripeptide composed of L-Met, L-Leu and L-Phe in a linear sequence with a formyl group at the amino terminus. It acts as a potent inducer of leucocyte chemotaxis and macrophage activator as well as a ligand for the FPR receptor.	2	1	0	tripeptide
adenosine-5'-(n-ethylcarboxamide) Adenosine-5'-(N-ethylcarboxamide): A stable adenosine A1 and A2 receptor agonist. Experimentally, it inhibits cAMP and cGMP phosphodiesterase activity.. N-ethyl-5'-carboxamidoadenosine : A derivative of adenosine in which the 5'-hydroxymethyl group is replaced by an N-ethylcarboxamido group.	4.18	5	0	adenosines; monocarboxylic acid amide	adenosine A1 receptor agonist; adenosine A2A receptor agonist; antineoplastic agent; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; vasodilator agent
ketoconazole (2R,4S)-ketoconazole : A cis-1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine which dioxolane moiety has (2R,4S)-configuration.	2.17	1	0	cis-1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine
enkephalin, leucine Enkephalin, Leucine: One of the endogenous pentapeptides with morphine-like activity. It differs from MET-ENKEPHALIN in the LEUCINE at position 5. Its first four amino acid sequence is identical to the tetrapeptide sequence at the N-terminal of BETA-ENDORPHIN.. Leu-enkephalin : A pentapeptide comprising L-tyrosine, glycine, glycine, L-phenylalanine and L-leucine residues joined in sequence by peptide linkages. It is an endogenous opioid peptide produced in vertebrate species, including rodents, primates and humans that results from decomposition of proenkephalin or dynorphin and exhibits antinociceptive properties.	3.53	1	1	pentapeptide; peptide zwitterion	analgesic; delta-opioid receptor agonist; human metabolite; mu-opioid receptor agonist; neurotransmitter; rat metabolite
n(6)-cyclopentyladenosine [no description available]	4.01	4	0
lithium Lithium: An element in the alkali metals family. It has the atomic symbol Li, atomic number 3, and atomic weight [6.938; 6.997]. Salts of lithium are used in treating BIPOLAR DISORDER.	2.41	2	0	alkali metal atom
fk 838 FK 838: an adenosine subtype-1 receptor antagonist; structure given in first source	2.43	2	0
2-((2-aminoethylamino)carbonylethylphenylethylamino)-5'-n-ethylcarboxamidoadenosine 2-((2-aminoethylamino)carbonylethylphenylethylamino)-5'-N-ethylcarboxamidoadenosine: structure given in first source	3.08	1	0
2-(4-(2-carboxyethyl)phenethylamino)-5'-n-ethylcarboxamidoadenosine 2-(4-(2-carboxyethyl)phenethylamino)-5'-N-ethylcarboxamidoadenosine: A2 adenosine receptor agonist; structure given in first source. CGS-21680 : A derivative of adenosine in which the 5'-hydroxymethyl group is replaced by N-ethylcarboxamido and the hydrogen at position 2 on the adenine is replaced by a 4-(2-carboxyethyl)phenethylamino group.	4.53	4	0	adenosines; dicarboxylic acid monoamide; monocarboxylic acid	adenosine A2A receptor agonist; anti-inflammatory agent
mrs 1523 2,3-diethyl-4,5-dipropyl-6-phenylpyridine-3-thiocarboxylate-5-carboxylate: adenosine A3 receptor antagonist	3.51	1	0
istradefylline [no description available]	3.76	2	0	oxopurine
cilastatin [no description available]	2.41	2	0	carboxamide; L-cysteine derivative; non-proteinogenic L-alpha-amino acid; organic sulfide	EC 3.4.13.19 (membrane dipeptidase) inhibitor; environmental contaminant; protease inhibitor; xenobiotic
fk 453 FK 453: adenosine A1 receptor antagonist; structure given in first source; a new antihypertensive agent with diuretic action in isolated rabbit aorta; FR113452 is the S-(-) enantiomer of FK 453	2.05	1	0
mrs 1754 [no description available]	3.51	1	0	oxopurine
cv 1808 2-phenylaminoadenosine: has coronary & cardiohemodynamic effects	3.08	1	0	purine nucleoside
staurosporine staurosporinium : Conjugate acid of staurosporine.	2	1	0	ammonium ion derivative
1-(3,4-dichlorophenyl)-3-(4-((1-ethyl-3-piperidyl)amino)-6-methyl-2-pyrimidinyl)guanidine 1-(3,4-dichlorophenyl)-3-(4-((1-ethyl-3-piperidyl)amino)-6-methyl-2-pyrimidinyl)guanidine: structure	3.51	1	0
n(6)-cyclohexyladenosine N(6)-cyclohexyladenosine: structure given in first source; receptors, purinergic P1 agonist	3.77	3	0
k201 compound K201 compound: structure given in first source	2.03	1	0
2-(2-furanyl)-7-(2-(4-(4-(2-methoxyethoxy)phenyl)-1-piperazinyl)ethyl)-7h-pyrazolo(4,3-e)(1,2,4)triazolo(1,5-c)pyrimidine-5-amine [no description available]	3.51	1	0
n(6)-(2,2-diphenylethyl)adenosine N(6)-(2,2-diphenylethyl)adenosine: adenosine receptor agonist; structure given in first source	3.08	1	0
cgs 24012 CGS 24012: adenosine agonist with both high affinity & selectivity for the adenosine A2 receptor	3.08	1	0
tozadenant tozadenant: an adenosine A2A receptor antagonist	3.51	1	0	benzothiazoles
psb 36 1-butyl-8-(3-noradamantyl)-3-(3-hydroxypropyl)xanthine: an A1 receptor antagonist	3.6	2	0	oxopurine
omecamtiv mecarbil [no description available]	3.18	1	0	ureas
bay 60-6583 BAY 60-6583: structure in first source. BAY 60-6583 : A member of the class of cyanopyridines that is 6-amino-3,5-dicyano-4-(4-hydroxyphenyl)-2-sulfanylpyridine in which the hydroxy and sulfanyl hydrogens are replaced by cyclopropylmethyl and carboxamidomethyl groups respectively.	2.08	1	0	aminopyridine; aromatic ether; aryl sulfide; cyanopyridine; cyclopropanes; monocarboxylic acid amide	adenosine A2B receptor agonist; anti-inflammatory agent; cardioprotective agent
losartan potassium Erythropoietin: Glycoprotein hormone, secreted chiefly by the KIDNEY in the adult and the LIVER in the FETUS, that acts on erythroid stem cells of the BONE MARROW to stimulate proliferation and differentiation.	2.69	3	0
atrial natriuretic factor Atrial Natriuretic Factor: A potent natriuretic and vasodilatory peptide or mixture of different-sized low molecular weight PEPTIDES derived from a common precursor and secreted mainly by the HEART ATRIUM. All these peptides share a sequence of about 20 AMINO ACIDS.	3.18	1	0	polypeptide
ularitide Ularitide: a 32-amino acid peptide derived from (95-126 residues) of ANP PROHORMONE (1-126 residues); not biologically inactivated by a peptidase from dog kidney cortex membranes	3.18	1	0
phosphatidylcholines Phosphatidylcholines: Derivatives of PHOSPHATIDIC ACIDS in which the phosphoric acid is bound in ester linkage to a CHOLINE moiety.	2.01	1	0	1,2-diacyl-sn-glycero-3-phosphocholine
v 2006 3-(4-amino-3-methylbenzyl)-7-(2-furyl)-3H-(1,2,3)triazolo(4,5-d)pyrimidine-5-amine: antiparkinson agent; structure in first source	3.51	1	0
cardiovascular agents Cardiovascular Agents: Agents that affect the rate or intensity of cardiac contraction, blood vessel diameter, or blood volume.	9.42	6	4
psb603 PSB603: an adenosine A2B receptor antagonist	3.51	1	0
natriuretic peptide, brain Natriuretic Peptide, Brain: A PEPTIDE that is secreted by the BRAIN and the HEART ATRIA, stored mainly in cardiac ventricular MYOCARDIUM. It can cause NATRIURESIS; DIURESIS; VASODILATION; and inhibits secretion of RENIN and ALDOSTERONE. It improves heart function. It contains 32 AMINO ACIDS.	4.1	2	0	polypeptide
ferric oxide, saccharated Ferric Oxide, Saccharated: A glucaric acid-iron conjugate that is used in the treatment of IRON-DEFICIENCY ANEMIA, including in patients with chronic kidney disease, when oral iron therapy is ineffective or impractical.	2.03	1	0
adrenomedullin Adrenomedullin: A 52-amino acid peptide with multi-functions. It was originally isolated from PHEOCHROMOCYTOMA and ADRENAL MEDULLA but is widely distributed throughout the body including lung and kidney tissues. Besides controlling fluid-electrolyte homeostasis, adrenomedullin is a potent vasodilator and can inhibit pituitary ACTH secretion.	3.18	1	0
apyrase Apyrase: A calcium-activated enzyme that catalyzes the hydrolysis of ATP to yield AMP and orthophosphate. It can also act on ADP and other nucleoside triphosphates and diphosphates. EC 3.6.1.5.	2.08	1	0
psb 11 [no description available]	3.51	1	0
n-benzo(1,3)dioxol-5-yl-2-(5-(2,6-dioxo-1,3-dipropyl-2,3,6,7-tetrahydro-1h-purin-8-yl)-1-methyl-1h-pyrazol-3-yloxy)-acetamide [no description available]	3.51	1	0

Condition	Indicated	Relationship Strength	Studies	Trials
Acute Kidney Failure [description not available]	0	3.59	9	0
Acute Kidney Injury Abrupt reduction in kidney function. Acute kidney injury encompasses the entire spectrum of the syndrome including acute kidney failure; ACUTE KIDNEY TUBULAR NECROSIS; and other less severe conditions.	0	3.59	9	0
Cardiac Failure [description not available]	0	18.5	104	84
Acute Disease Disease having a short and relatively severe course.	0	15.83	80	74
Heart Failure A heterogeneous condition in which the heart is unable to pump out sufficient blood to meet the metabolic need of the body. Heart failure can be caused by structural defects, functional abnormalities (VENTRICULAR DYSFUNCTION), or a sudden overload beyond its capacity. Chronic heart failure is more common than acute heart failure which results from sudden insult to cardiac function, such as MYOCARDIAL INFARCTION.	1	23.2	208	168
Kahler Disease [description not available]	0	2.08	1	0
Multiple Myeloma A malignancy of mature PLASMA CELLS engaging in monoclonal immunoglobulin production. It is characterized by hyperglobulinemia, excess Bence-Jones proteins (free monoclonal IMMUNOGLOBULIN LIGHT CHAINS) in the urine, skeletal destruction, bone pain, and fractures. Other features include ANEMIA; HYPERCALCEMIA; and RENAL INSUFFICIENCY.	0	2.08	1	0
Breathlessness [description not available]	0	12.7	21	19
Dyspnea Difficult or labored breathing.	0	12.7	21	19
Chronic Kidney Failure [description not available]	0	6.19	6	0
Kidney Failure, Chronic The end-stage of CHRONIC RENAL INSUFFICIENCY. It is characterized by the severe irreversible kidney damage (as measured by the level of PROTEINURIA) and the reduction in GLOMERULAR FILTRATION RATE to less than 15 ml per min (Kidney Foundation: Kidney Disease Outcome Quality Initiative, 2002). These patients generally require HEMODIALYSIS or KIDNEY TRANSPLANTATION.	0	6.19	6	0
Complications of Diabetes Mellitus [description not available]	0	4.4	1	1
Atherogenesis [description not available]	0	4.4	1	1
Kidney Failure A severe irreversible decline in the ability of kidneys to remove wastes, concentrate URINE, and maintain ELECTROLYTE BALANCE; BLOOD PRESSURE; and CALCIUM metabolism.	0	12.51	26	24
Blood Pressure, Low [description not available]	0	4.4	1	1
Weight Reduction [description not available]	0	4.4	1	1
Hypotension Abnormally low BLOOD PRESSURE that can result in inadequate blood flow to the brain and other vital organs. Common symptom is DIZZINESS but greater negative impacts on the body occur when there is prolonged depravation of oxygen and nutrients.	0	4.4	1	1
Weight Loss Decrease in existing BODY WEIGHT.	0	4.4	1	1
Atherosclerosis A thickening and loss of elasticity of the walls of ARTERIES that occurs with formation of ATHEROSCLEROTIC PLAQUES within the ARTERIAL INTIMA.	0	4.4	1	1
Renal Insufficiency Conditions in which the KIDNEYS perform below the normal level in the ability to remove wastes, concentrate URINE, and maintain ELECTROLYTE BALANCE; BLOOD PRESSURE; and CALCIUM metabolism. Renal insufficiency can be classified by the degree of kidney damage (as measured by the level of PROTEINURIA) and reduction in GLOMERULAR FILTRATION RATE.	0	12.51	26	24
Disease Exacerbation [description not available]	0	11.79	21	19
Anasarca [description not available]	0	2.43	2	0
Heart Disease, Ischemic [description not available]	0	2.43	2	0
Diabetes Mellitus A heterogeneous group of disorders characterized by HYPERGLYCEMIA and GLUCOSE INTOLERANCE.	0	2.13	1	0
Edema Abnormal fluid accumulation in TISSUES or body cavities. Most cases of edema are present under the SKIN in SUBCUTANEOUS TISSUE.	0	2.43	2	0
Myocardial Ischemia A disorder of cardiac function caused by insufficient blood flow to the muscle tissue of the heart. The decreased blood flow may be due to narrowing of the coronary arteries (CORONARY ARTERY DISEASE), to obstruction by a thrombus (CORONARY THROMBOSIS), or less commonly, to diffuse narrowing of arterioles and other small vessels within the heart. Severe interruption of the blood supply to the myocardial tissue may result in necrosis of cardiac muscle (MYOCARDIAL INFARCTION).	0	2.43	2	0
Chronic Kidney Diseases [description not available]	0	3.4	2	0
Renal Insufficiency, Chronic Conditions in which the KIDNEYS perform below the normal level for more than three months. Chronic kidney insufficiency is classified by five stages according to the decline in GLOMERULAR FILTRATION RATE and the degree of kidney damage (as measured by the level of PROTEINURIA). The most severe form is the end-stage renal disease (CHRONIC KIDNEY FAILURE). (Kidney Foundation: Kidney Disease Outcome Quality Initiative, 2002)	0	3.4	2	0
Adverse Effects, Long Term [description not available]	0	7.55	4	4
Tauopathies Neurodegenerative disorders involving deposition of abnormal tau protein isoforms (TAU PROTEINS) in neurons and glial cells in the brain. Pathological aggregations of tau proteins are associated with mutation of the tau gene on chromosome 17 in patients with ALZHEIMER DISEASE; DEMENTIA; PARKINSONIAN DISORDERS; progressive supranuclear palsy (SUPRANUCLEAR PALSY, PROGRESSIVE); and corticobasal degeneration.	0	2.13	1	0
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	0	4.32	7	0
Protein Aggregation, Pathological A biochemical phenomenon in which misfolded proteins aggregate either intra- or extracellularly. Triggered by factors such as MUTATION; POST-TRANSLATIONAL MODIFICATIONS, and environmental stress, it is generally associated with ALZHEIMER DISEASE; PARKINSON DISEASE; HUNTINGTON DISEASE; and TYPE 2 DIABETES MELLITUS.	0	2.13	1	0
Ache [description not available]	0	2.15	1	0
Pain An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.	0	2.15	1	0
Symptom Cluster [description not available]	0	4.44	3	0
Kidney Diseases Pathological processes of the KIDNEY or its component tissues.	0	12.5	19	17
Syndrome A characteristic symptom complex.	0	4.44	3	0
Apoplexy [description not available]	0	7.5	4	4
Stroke A group of pathological conditions characterized by sudden, non-convulsive loss of neurological function due to BRAIN ISCHEMIA or INTRACRANIAL HEMORRHAGES. Stroke is classified by the type of tissue NECROSIS, such as the anatomic location, vasculature involved, etiology, age of the affected individual, and hemorrhagic vs. non-hemorrhagic nature. (From Adams et al., Principles of Neurology, 6th ed, pp777-810)	0	7.5	4	4
Injury, Ischemia-Reperfusion [description not available]	0	2.43	2	0
Reperfusion Injury Adverse functional, metabolic, or structural changes in tissues that result from the restoration of blood flow to the tissue (REPERFUSION) following ISCHEMIA.	0	2.43	2	0
Anemia A reduction in the number of circulating ERYTHROCYTES or in the quantity of HEMOGLOBIN.	0	2.41	2	0
Infections, Staphylococcal [description not available]	0	2.03	1	0
Cardiovascular Diseases Pathological conditions involving the CARDIOVASCULAR SYSTEM including the HEART; the BLOOD VESSELS; or the PERICARDIUM.	0	2.44	2	0
Staphylococcal Infections Infections with bacteria of the genus STAPHYLOCOCCUS.	0	2.03	1	0
Mucositis An INFLAMMATION of the MUCOSA with burning or tingling sensation. It is characterized by atrophy of the squamous EPITHELIUM, vascular damage, inflammatory infiltration, and ulceration. It usually occurs at the mucous lining of the MOUTH, the GASTROINTESTINAL TRACT or the airway due to chemical irritations, CHEMOTHERAPY, or radiation therapy (RADIOTHERAPY).	0	2.03	1	0
Arrhythmia [description not available]	0	3.42	1	1
Arrhythmias, Cardiac Any disturbances of the normal rhythmic beating of the heart or MYOCARDIAL CONTRACTION. Cardiac arrhythmias can be classified by the abnormalities in HEART RATE, disorders of electrical impulse generation, or impulse conduction.	0	3.42	1	1
Ascites Accumulation or retention of free fluid within the peritoneal cavity.	0	1.98	1	0
Nephrosis Pathological processes of the KIDNEY without inflammatory or neoplastic components. Nephrosis may be a primary disorder or secondary complication of other diseases. It is characterized by the NEPHROTIC SYNDROME indicating the presence of PROTEINURIA and HYPOALBUMINEMIA with accompanying EDEMA.	0	1.98	1	0
Anesthesia A state characterized by loss of feeling or sensation. This depression of nerve function is usually the result of pharmacologic action and is induced to allow performance of surgery or other painful procedures.	0	3.6	3	0
Electrolytes Substances that dissociate into two or more ions, to some extent, in water. Solutions of electrolytes thus conduct an electric current and can be decomposed by it (ELECTROLYSIS). (Grant & Hackh's Chemical Dictionary, 5th ed)	0	2.68	3	0
Cardiovascular Stroke [description not available]	0	1.98	1	0
Injury, Myocardial Reperfusion [description not available]	0	2.4	2	0
Myocardial Infarction NECROSIS of the MYOCARDIUM caused by an obstruction of the blood supply to the heart (CORONARY CIRCULATION).	0	1.98	1	0
Sensitivity and Specificity Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)	0	1.98	1	0
Blood Pressure, High [description not available]	0	1.98	1	0
Hypertension Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more.	0	1.98	1	0
Anoxemia [description not available]	0	2.91	4	0
Hypoxia Sub-optimal OXYGEN levels in the ambient air of living organisms.	0	2.91	4	0
Oliguria Decreased URINE output that is below the normal range. Oliguria can be defined as urine output of less than or equal to 0.5 or 1 ml/kg/hr depending on the age.	0	2.92	1	0
Chronic Illness [description not available]	0	2	1	0
Chronic Disease Diseases which have one or more of the following characteristics: they are permanent, leave residual disability, are caused by nonreversible pathological alteration, require special training of the patient for rehabilitation, or may be expected to require a long period of supervision, observation, or care (Dictionary of Health Services Management, 2d ed). For epidemiological studies chronic disease often includes HEART DISEASES; STROKE; CANCER; and diabetes (DIABETES MELLITUS, TYPE 2).	0	2	1	0
Glomerulonephritis, Minimal Change [description not available]	0	2	1	0
Nephrosis, Lipoid A kidney disease with no or minimal histological glomerular changes on light microscopy and with no immune deposits. It is characterized by lipid accumulation in the epithelial cells of KIDNEY TUBULES and in the URINE. Patients usually show NEPHROTIC SYNDROME indicating the presence of PROTEINURIA with accompanying EDEMA.	0	2	1	0
Active Hyperemia [description not available]	0	2.01	1	0
Hyperemia The presence of an increased amount of blood in a body part or an organ leading to congestion or engorgement of blood vessels. Hyperemia can be due to increase of blood flow into the area (active or arterial), or due to obstruction of outflow of blood from the area (passive or venous).	0	2.01	1	0

rolofylline

Description

Cross-References

Synonyms (32)

Research Excerpts

Overview

Treatment

Toxicity

Pharmacokinetics

Bioavailability

Dosage Studied

Drug Classes (1)

Protein Targets (14)

Inhibition Measurements

Activation Measurements

Other Measurements

Biological Processes (120)

Molecular Functions (25)

Ceullar Components (25)

Bioassays (101)

Research

Studies (109)

Market Indicators

Research Demand Index: 22.87

Study Types

Clinical Trials (7)

Trial Overview

rolofylline

Description

Cross-References

Synonyms (32)

Research Excerpts

Overview

Treatment

Toxicity

Pharmacokinetics

Bioavailability

Dosage Studied

Drug Classes (1)

Protein Targets (14)

Inhibition Measurements

Activation Measurements

Other Measurements

Biological Processes (120)

Molecular Functions (25)

Ceullar Components (25)

Bioassays (101)

Research

Studies (109)

Market Indicators

Research Demand Index: 22.87

Study Types

Clinical Trials (7)

Trial Overview

Related Drugs (120)

Related Conditions (67)