st 1535 profile

ID Source	ID
PubMed CID	9860294
CHEMBL ID	197669
SCHEMBL ID	5362208
MeSH ID	M0493042

Synonym
2-butyl-9-methyl-8-(triazol-2-yl)purin-6-amine
st-1535 ,
L001675
CHEMBL197669 ,
st1535
2-butyl-9-methyl-8-(2h-1,2,3-triazol-2-yl)-9h-purin-6-amine
2-butyl-9-methyl-8-[1,2,3]triazol-2-yl-9h-purin-6-ylamine
bdbm50176058
st 1535
496955-42-1
gtpl5613
SCHEMBL5362208
DTXSID60432000
2-butyl-9-methyl-8-(2h-1,2,3-triazol-2-yl)-9h-purin-6-ylamine
AKOS030562134
AS-35290
Q27088881
SB16783
A913876
BS165703
ct-1500
NTK8WWM73W

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Adenosine receptor A3	Homo sapiens (human)	Ki	5.5000	0.0000	0.9306	10.0000	AID1138025; AID254515
Adenosine receptor A2a	Homo sapiens (human)	IC50 (µMol)	0.4300	0.0007	1.5594	10.0000	AID756878
Adenosine receptor A2a	Homo sapiens (human)	Ki	0.0074	0.0000	1.0609	9.7920	AID1138023; AID254542; AID365580; AID747271; AID756879
Adenosine receptor A2b	Homo sapiens (human)	Ki	0.3521	0.0002	1.6352	10.0000	AID1138021; AID254541
Adenosine receptor A1	Homo sapiens (human)	Ki	0.0807	0.0002	0.9316	10.0000	AID1138024; AID254536; AID747272; AID756877
Delta-type opioid receptor	Mus musculus (house mouse)	Ki	0.0066	0.0000	0.5393	9.4000	AID365580
Mu-type opioid receptor	Cavia porcellus (domestic guinea pig)	Ki	0.0066	0.0000	0.2786	9.0000	AID365580
[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)
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)
[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)
[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)
[Information is prepared from geneontology information from the June-17-2024 release]

Assay ID	Title	Year	Journal	Article
AID255282	Percent inhibition against Acetylcholine transporter at 1 uM	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID756877	Displacement of [3H]DPCPX from human recombinant adenosine A1 receptor expressed in CHO-K1 cells after 60 mins	2013	Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13	Synthesis and biological evaluation of metabolites of 2-n-butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine (ST1535), a potent antagonist of the A2A adenosine receptor for the treatment of Parkinson's disease.
AID255262	Percent inhibition against GABA transporter at a compound concentration of 1 uM	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID255257	Percent inhibition against NMDA receptor at a compound concentration of 1 uM	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID255274	Percent inhibition against Dopamine receptor D2 at 1 uM	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID255288	Percent inhibition against ADO transporter at 1 uM nonselective	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID255298	Percent inhibition against Muscarinic acetylcholine receptor M5 at 1 uM	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID255270	Percent inhibition against GABA-B receptor at 1 uM	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID254536	Binding affinity towards human Adenosine A1 receptor expressed in CHO cells using 1 nM [3H]DPCPX	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID255284	Percent inhibition against Beta-1 adrenergic receptor at 1 uM	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID1138036	Selectivity ratio of Ki for human recombinant adenosine receptor A2b to Ki for human recombinant adenosine receptor A2a	2014	Journal of medicinal chemistry, May-08, Volume: 57, Issue:9	Adenosine A2A receptor as a drug discovery target.
AID747271	Antagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assay	2013	Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11	Novel adenosine A(2A) receptor ligands: a synthetic, functional and computational investigation of selected literature adenosine A(2A) receptor antagonists for extending into extracellular space.
AID255315	Percent inhibition against 5-hydroxytryptamine 2C receptor at 1 uM	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID1138021	Inhibition of human recombinant adenosine receptor A2b	2014	Journal of medicinal chemistry, May-08, Volume: 57, Issue:9	Adenosine A2A receptor as a drug discovery target.
AID255256	Percent inhibition against AMPA receptor at 1 uM	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID255268	Percent inhibition against P2Y Purinoceptor at 1 uM	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID255297	Percent inhibition against Muscarinic acetylcholine receptor M4 at 1 uM	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID756879	Displacement of [3H]ZM241385 from human recombinant adenosine A2A receptor expressed in HEK293 cells after 1 hr by competitive binding assay	2013	Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13	Synthesis and biological evaluation of metabolites of 2-n-butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine (ST1535), a potent antagonist of the A2A adenosine receptor for the treatment of Parkinson's disease.
AID747272	Antagonist activity at human adenosine A1 receptor assessed as cAMP level by cell based assay	2013	Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11	Novel adenosine A(2A) receptor ligands: a synthetic, functional and computational investigation of selected literature adenosine A(2A) receptor antagonists for extending into extracellular space.
AID365580	Binding affinity to human adenosine A2A receptor	2008	Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15	2-Amino-6-furan-2-yl-4-substituted nicotinonitriles as A2A adenosine receptor antagonists.
AID255287	Percent inhibition against Alpha-2 adrenergic receptor at 1 uM	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID255254	Percent inhibition against PCP receptor at 1 uM	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID255317	Percent inhibition against 5-hydroxytryptamine transporter at 1 uM nonselective	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID255295	Percent inhibition against Muscarinic acetylcholine receptor M2 at 1 uM	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID1138020	Selectivity ratio of Ki for human recombinant adenosine A1 receptor to Ki for human recombinant adenosine receptor A2a	2014	Journal of medicinal chemistry, May-08, Volume: 57, Issue:9	Adenosine A2A receptor as a drug discovery target.
AID255313	Percent inhibition against 5-hydroxytryptamine 1A receptor at 1 uM	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID756878	Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 10 mins prior to NECA addition	2013	Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13	Synthesis and biological evaluation of metabolites of 2-n-butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine (ST1535), a potent antagonist of the A2A adenosine receptor for the treatment of Parkinson's disease.
AID255277	Percent inhibition against Dopamine receptor D5 at 1 uM	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID255285	Percent inhibition against Beta-2 adrenergic receptor at 1 uM	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID255286	Percent inhibition against Alpha-1 adrenergic receptor at 1 uM	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID255314	Percent inhibition against 5-hydroxytryptamine 2A receptor at 1 uM	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID255303	Percent inhibition against Norepinephrine transporter at 1 uM nonselective	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID254541	Binding affinity towards human Adenosine A2b receptor expressed in HEK293 cells using 5 nM [3H]DPCPX	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID255310	Percent inhibition against 5-hydroxytryptamine 3 receptor at 1 uM	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID1138024	Inhibition of human recombinant adenosine A1 receptor	2014	Journal of medicinal chemistry, May-08, Volume: 57, Issue:9	Adenosine A2A receptor as a drug discovery target.
AID255281	Percent inhibition against P2X Purinergic receptor at 1 uM	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID254515	Binding affinity towards human Adenosine A3 receptor expressed in HEK293 cells using 0.1 nM [3H]AB-MECA	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID255292	Percent inhibition against Dopamine transporter at 1 uM	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID255312	Percent inhibition against 5-hydroxytryptamine 6 receptor at 1 uM	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID255279	Percent inhibition against Histamine H1 receptor at 1 uM	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID255267	Percent inhibition against Kainate receptor at a compound concentration of 1 uM	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID1138023	Inhibition of human recombinant adenosine receptor A2a	2014	Journal of medicinal chemistry, May-08, Volume: 57, Issue:9	Adenosine A2A receptor as a drug discovery target.
AID255296	Percent inhibition against Muscarinic acetylcholine receptor M3 at 1 uM	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID255316	Percent inhibition against 5-hydroxytryptamine 5A receptor at 1 uM	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID255311	Percent inhibition against 5-hydroxytryptamine 4 receptor at 1 uM	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID255275	Percent inhibition against Dopamine receptor D3 at 1 uM	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID255309	Percent inhibition against Opioid receptor at 1 uM	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID255294	Percent inhibition against Muscarinic acetylcholine receptor M1 at 1 uM	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID255280	Percent inhibition against central Benzodiazepine receptor at 1 uM	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID254542	Binding affinity towards human Adenosine A2a receptor expressed in HEK293 cells using 6 nM [3H]CGS-21680	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID255276	Percent inhibition against Dopamine receptor D4 at 1 uM	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID1138025	Inhibition of human recombinant adenosine A3 receptor	2014	Journal of medicinal chemistry, May-08, Volume: 57, Issue:9	Adenosine A2A receptor as a drug discovery target.
AID255370	Selective binding affinity towards human Adenosine A1 receptor expressed in CHO cells using [3H]DPCPX compared to human Adenosine A2a receptor expressed in HEK293 cells using [3H]-CGS-21,680	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID255273	Percent inhibition against Dopamine receptor D1 at 1 uM	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID255278	Percent inhibition against GABAA receptor alpha at a compound concentration of 1 uM	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID255371	Selective binding affinity towards human Adenosine A2b receptor expressed in HEK293 cells using [3H]-DPCPX compared to human Adenosine A2a receptor expressed in HEK293 cells using [3H]CGS-21680	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID1345721	Human A2B receptor (Adenosine receptors)	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID1345822	Human A3 receptor (Adenosine receptors)	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID1345618	Human A2A receptor (Adenosine receptors)	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID1345685	Human A1 receptor (Adenosine receptors)	2005	Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22	2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
[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	0 (0.00)	18.2507
2000's	2 (40.00)	29.6817
2010's	3 (60.00)	24.3611
2020's	0 (0.00)	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	0 (0.00%)	5.53%
Reviews	1 (20.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	4 (80.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
8-hydroxy-2-(di-n-propylamino)tetralin 8-Hydroxy-2-(di-n-propylamino)tetralin: A serotonin 1A-receptor agonist that is used experimentally to test the effects of serotonin.. 8-OH-DPAT : A tetralin substituted at positions 1 and 7 by hydroxy and dipropylamino groups respectively	2.02	1	phenols; tertiary amino compound; tetralins	serotonergic antagonist
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.	2.44	2	oxopurine	adenosine A1 receptor antagonist; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor
theophylline [no description available]	3.19	1	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
atenolol Atenolol: A cardioselective beta-1 adrenergic blocker possessing properties and potency similar to PROPRANOLOL, but without a negative inotropic effect.. atenolol : An ethanolamine compound having a (4-carbamoylmethylphenoxy)methyl group at the 1-position and an N-isopropyl substituent.	2.02	1	ethanolamines; monocarboxylic acid amide; propanolamine	anti-arrhythmia drug; antihypertensive agent; beta-adrenergic antagonist; environmental contaminant; sympatholytic agent; xenobiotic
baclofen [no description available]	2.02	1	amino acid zwitterion; gamma-amino acid; monocarboxylic acid; monochlorobenzenes; primary amino compound	central nervous system depressant; GABA agonist; muscle relaxant
caffeine [no description available]	3.59	2	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
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.	3.57	2	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
diazepam Diazepam: A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of GAMMA-AMINOBUTYRIC ACID activity.. diazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a methyl group at position 1 and a phenyl group at position 5.	2.02	1	1,4-benzodiazepinone; organochlorine compound	anticonvulsant; anxiolytic drug; environmental contaminant; sedative; xenobiotic
ici 118551 [no description available]	2.02	1	indanes
imipramine Imipramine: The prototypical tricyclic antidepressant. It has been used in major depression, dysthymia, bipolar depression, attention-deficit disorders, agoraphobia, and panic disorders. It has less sedative effect than some other members of this therapeutic group.. imipramine : A dibenzoazepine that is 5H-dibenzo[b,f]azepine substituted by a 3-(dimethylamino)propyl group at the nitrogen atom.	2.02	1	dibenzoazepine	adrenergic uptake inhibitor; antidepressant; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor
ketanserin Ketanserin: A selective serotonin receptor antagonist with weak adrenergic receptor blocking properties. The drug is effective in lowering blood pressure in essential hypertension. It also inhibits platelet aggregation. It is well tolerated and is particularly effective in older patients.. ketanserin : A member of the class of quinazolines that is quinazoline-2,4(1H,3H)-dione which is substituted at position 3 by a 2-[4-(p-fluorobenzoyl)piperidin-1-yl]ethyl group.	2.02	1	aromatic ketone; organofluorine compound; piperidines; quinazolines	alpha-adrenergic antagonist; antihypertensive agent; cardiovascular drug; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; serotonergic antagonist
methoctramine [no description available]	2.02	1	aromatic ether; tetramine	muscarinic antagonist
muscimol Muscimol: A neurotoxic isoxazole isolated from species of AMANITA. It is obtained by decarboxylation of IBOTENIC ACID. Muscimol is a potent agonist of GABA-A RECEPTORS and is used mainly as an experimental tool in animal and tissue studies.. muscimol : A member of the class of isoxazoles that is 1,2-oxazol-3(2H)-one substituted by an aminomethyl group at position 5. It has been isolated from mushrooms of the genus Amanita.	2.02	1	alkaloid; isoxazoles; primary amino compound	fungal metabolite; GABA agonist; oneirogen; psychotropic drug
nipecotic acid nipecotic acid: RN given refers to cpd without isomeric designation. nipecotic acid : A piperidinemonocarboxylic acid that is piperidine in which one of the hydrogens at position 3 is substituted by a carboxylic acid group.	2.02	1	beta-amino acid; piperidinemonocarboxylic acid
pirenzepine Pirenzepine: An antimuscarinic agent that inhibits gastric secretion at lower doses than are required to affect gastrointestinal motility, salivary, central nervous system, cardiovascular, ocular, and urinary function. It promotes the healing of duodenal ulcers and due to its cytoprotective action is beneficial in the prevention of duodenal ulcer recurrence. It also potentiates the effect of other antiulcer agents such as CIMETIDINE and RANITIDINE. It is generally well tolerated by patients.	2.02	1	pyridobenzodiazepine	anti-ulcer drug; antispasmodic drug; muscarinic antagonist
prazosin Prazosin: A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION.. prazosin : A member of the class of piperazines that is piperazine substituted by a furan-2-ylcarbonyl group and a 4-amino-6,7-dimethoxyquinazolin-2-yl group at positions 1 and 4 respectively.	2.02	1	aromatic ether; furans; monocarboxylic acid amide; piperazines; quinazolines	alpha-adrenergic antagonist; antihypertensive agent; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor
protriptyline Protriptyline: Tricyclic antidepressant similar in action and side effects to IMIPRAMINE. It may produce excitation.	2.02	1	carbotricyclic compound	antidepressant
pyrilamine Pyrilamine: A histamine H1 antagonist. It has mild hypnotic properties and some local anesthetic action and is used for allergies (including skin eruptions) both parenterally and locally. It is a common ingredient of cold remedies.. mepyramine : An ethylenediamine derivative that is ethylenediamine in which one of the amino nitrogens is substituted by two methyl groups and the remaining amino nitrogen is substituted by a 4-methoxybenzyl and a pyridin-2-yl group.	2.02	1	aromatic ether; ethylenediamine derivative	H1-receptor antagonist
8-(4-((2-aminoethyl)aminocarbonylmethyloxy)phenyl)-1,3-dipropylxanthine 8-(4-((2-aminoethyl)aminocarbonylmethyloxy)phenyl)-1,3-dipropylxanthine: adenosine receptor antagonist	2.08	1
yohimbine Yohimbine: A plant alkaloid with alpha-2-adrenergic blocking activity. Yohimbine has been used as a mydriatic and in the treatment of ERECTILE DYSFUNCTION.. yohimbine : An indole alkaloid with alpha2-adrenoceptor antagonist activity. It is produced by Corynanthe johimbe and Rauwolfia serpentina.	2.02	1	methyl 17-hydroxy-20xi-yohimban-16-carboxylate	alpha-adrenergic antagonist; dopamine receptor D2 antagonist; serotonergic antagonist
2-chloroadenosine 5-chloroformycin A: structure given in first source	3.19	1	purine nucleoside
hemicholinium 3 Hemicholinium 3: A potent inhibitor of the high affinity uptake system for CHOLINE. It has less effect on the low affinity uptake system. Since choline is one of the components of ACETYLCHOLINE, treatment with hemicholinium can deplete acetylcholine from cholinergic terminals. Hemicholinium 3 is commonly used as a research tool in animal and in vitro experiments.	2.02	1
kainic acid Kainic Acid: (2S-(2 alpha,3 beta,4 beta))-2-Carboxy-4-(1-methylethenyl)-3-pyrrolidineacetic acid. Ascaricide obtained from the red alga Digenea simplex. It is a potent excitatory amino acid agonist at some types of excitatory amino acid receptors and has been used to discriminate among receptor types. Like many excitatory amino acid agonists it can cause neurotoxicity and has been used experimentally for that purpose.	2.02	1	dicarboxylic acid; L-proline derivative; non-proteinogenic L-alpha-amino acid; pyrrolidinecarboxylic acid	antinematodal drug; excitatory amino acid agonist
glutamic acid Glutamic Acid: A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.. glutamic acid : An alpha-amino acid that is glutaric acid bearing a single amino substituent at position 2.	2.02	1	glutamic acid; glutamine family amino acid; L-alpha-amino acid; proteinogenic amino acid	Escherichia coli metabolite; ferroptosis inducer; micronutrient; mouse metabolite; neurotransmitter; nutraceutical
butaclamol [no description available]	2.02	1	amino alcohol; organic heteropentacyclic compound; tertiary alcohol; tertiary amino compound	dopaminergic antagonist
adenosine quinquefolan B: isolated from roots of Panax quinquefolium L.; RN not in Chemline 10/87; RN from Toxlit	3.19	1	adenosines; purines D-ribonucleoside	analgesic; anti-arrhythmia drug; fundamental metabolite; human metabolite; vasodilator agent
4-nitrobenzylthioinosine 4-nitrobenzylthioinosine: inhibitor of nucleoside transport; acts on ENT1	2.02	1	purine nucleoside
selfotel selfotel: a N-methyl-D-aspartate (NMDA) antagonist; used to treat stroke-induced impairment	2.02	1	non-proteinogenic alpha-amino acid
mesulergine mesulergine: RN given refers to parent cpd; CU 32-085 is synonymous to mono-HCl; metabolized into dopaminergic agonists; structure given in first source. mesulergine : A member of the class of ergot alkaloids that is known to act on serotonin and dopamine receptors.	2.02	1	ergot alkaloid; sulfamides	antiparkinson drug; dopamine agonist; serotonergic antagonist
alpha,beta-methyleneadenosine 5'-triphosphate alpha,beta-methyleneadenosine 5'-triphosphate: do not confuse with beta,gamma-methylene ATP; RN given refers to parent cpd	2.02	1	nucleoside triphosphate analogue
n(6)-(3-iodobenzyl)-5'-n-methylcarboxamidoadenosine N(6)-(3-iodobenzyl)-5'-N-methylcarboxamidoadenosine: structure given in first source; a selective A(3) adenosine receptor agonist. 3-iodobenzyl-5'-N-methylcarboxamidoadenosine : A derivative of adenosine in which the 5'-hydroxymethyl group is replaced by N-ethylcarboxamido and one of the hydrogens of the exocyclic amino function is substituted by a 3-iodobenzyl group.	2.02	1	adenosines; monocarboxylic acid amide; organoiodine compound	adenosine A3 receptor agonist
zm 241385 ZM 241385: a high affinity radioligand selective for the A2a adenosine receptor	4.07	4	diamino-1,3,5-triazine
sch 58261 [no description available]	3.57	2	triazolopyrimidines
dizocilpine [no description available]	2.02	1	secondary amino compound; tetracyclic antidepressant	anaesthetic; anticonvulsant; neuroprotective agent; nicotinic antagonist; NMDA receptor antagonist
2'-deoxyadenosine 5'-o-(1-thiotriphosphate) 2'-deoxyadenosine 5'-O-(1-thiotriphosphate): RN given refers to cpd without isomeric designation; structure.	2.02	1
regadenoson [no description available]	3.19	1	purine nucleoside
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.	3.57	2	adenosines; monocarboxylic acid amide	adenosine A1 receptor agonist; adenosine A2A receptor agonist; antineoplastic agent; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; vasodilator agent
wr-142,490 (+)-(11R,2'S)-erythro-mefloquine : An optically active form of [2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol having (+)-(11R,2'S)-erythro-configuration. An antimalarial agent, used in racemic form, which acts as a blood schizonticide; its mechanism of action is unknown.	3.19	1	[2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol	antimalarial
n(6)-cyclopentyladenosine [no description available]	2.04	1
bemesetron [no description available]	2.02	1
4-diphenylacetoxy-n-methylpiperidine methiodide 4-DAMP methiodide : A quaternary ammonium salt obtained by combining equimolar amounts of 4-diphenylacetoxy-N-methylpiperidine and iodomethane.	2.02	1	iodide salt; quaternary ammonium salt	cholinergic antagonist; muscarinic antagonist
sch 23390 SCH 23390: a selective D1-receptor antagonist. SCH 23390 : A benzazepine that is 2,3,4,5-tetrahydro-3-benzazepine bearing a phenyl substituent at position 1, a methyl substituent at position 3, a chloro substituent at position 7 and a hydroxy substituent at position 8.	2.02	1	benzazepine
2-((2-aminoethylamino)carbonylethylphenylethylamino)-5'-n-ethylcarboxamidoadenosine 2-((2-aminoethylamino)carbonylethylphenylethylamino)-5'-N-ethylcarboxamidoadenosine: structure given in first source	3.19	1
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.	3.19	1	adenosines; dicarboxylic acid monoamide; monocarboxylic acid	adenosine A2A receptor agonist; anti-inflammatory agent
naloxone Naloxone: A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.. naloxone : A synthetic morphinane alkaloid that is morphinone in which the enone double bond has been reduced to a single bond, the hydrogen at position 14 has been replaced by a hydroxy group, and the methyl group attached to the nitrogen has been replaced by an allyl group. A specific opioid antagonist, it is used (commonly as its hydrochloride salt) to reverse the effects of opioids, both following their use of opioids during surgery and in cases of known or suspected opioid overdose.	2.02	1	morphinane alkaloid; organic heteropentacyclic compound; tertiary alcohol	antidote to opioid poisoning; central nervous system depressant; mu-opioid receptor antagonist
istradefylline [no description available]	3.85	3	oxopurine
isoalloxazine isoalloxazine: structure	2.02	1	benzo[g]pteridine-2,4-dione
cv 1808 2-phenylaminoadenosine: has coronary & cardiohemodynamic effects	3.19	1	purine nucleoside
binodenoson [no description available]	3.19	1
atl 146e BMS-068645: structure in first source	3.19	1
2-(2-(4-chlorophenyl)ethoxy)adenosine 2-(2-(4-chlorophenyl)ethoxy)adenosine: a adenosine A2A receptor agonist	3.19	1
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]	3.19	1
tozadenant tozadenant: an adenosine A2A receptor antagonist	3.19	1	benzothiazoles
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	3.19	1
clozapine Clozapine: A tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity. Agranulocytosis is a major adverse effect associated with administration of this agent.. clozapine : A benzodiazepine that is 5H-dibenzo[b,e][1,4]diazepine substituted by a chloro group at position 8 and a 4-methylpiperazin-1-yl group at position 11. It is a second generation antipsychotic used in the treatment of psychiatric disorders like schizophrenia.	2.02	1	benzodiazepine; N-arylpiperazine; N-methylpiperazine; organochlorine compound	adrenergic antagonist; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; environmental contaminant; GABA antagonist; histamine antagonist; muscarinic antagonist; second generation antipsychotic; serotonergic antagonist; xenobiotic

Condition	Indicated	Relationship Strength	Studies	Trials
Idiopathic Parkinson Disease [description not available]	0	2.08	1	0
Parkinson Disease A progressive, degenerative neurologic disease characterized by a TREMOR that is maximal at rest, retropulsion (i.e. a tendency to fall backwards), rigidity, stooped posture, slowness of voluntary movements, and a masklike facial expression. Pathologic features include loss of melanin containing neurons in the substantia nigra and other pigmented nuclei of the brainstem. LEWY BODIES are present in the substantia nigra and locus coeruleus but may also be found in a related condition (LEWY BODY DISEASE, DIFFUSE) characterized by dementia in combination with varying degrees of parkinsonism. (Adams et al., Principles of Neurology, 6th ed, p1059, pp1067-75)	0	2.08	1	0

st 1535

Cross-References

Synonyms (22)

Protein Targets (6)

Inhibition Measurements

Biological Processes (105)

Molecular Functions (16)

Ceullar Components (18)

Bioassays (60)

Research

Studies (5)

Market Indicators

Research Demand Index: 12.84

Study Types

st 1535

Cross-References

Synonyms (22)

Protein Targets (6)

Inhibition Measurements

Biological Processes (105)

Molecular Functions (16)

Ceullar Components (18)

Bioassays (60)

Research

Studies (5)

Market Indicators

Research Demand Index: 12.84

Study Types

Related Drugs (55)

Related Conditions (2)