tozadenant profile

tozadenant: an adenosine A2A receptor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	11618368
CHEMBL ID	2105747
CHEBI ID	177494
SCHEMBL ID	1628246
MeSH ID	M000600099

Synonym
HY-10995
4-hydroxy-n-(4-methoxy-7-morpholin-4-yl-1,3-benzothiazol-2-yl)-4-methylpiperidine-1-carboxamide
tozadenant
870070-55-6
CHEBI:177494
D10174
tozadenant (usan)
unii-d9k857j81i
syn115
syn-115
ro4494351-002
4-hydroxy-n-(4-methoxy-7-morpholinobenzo(d)thiazol-2-yl)-4-methylpiperidine-1-carboxamide
ro4494351
a2a (3)
ro-4494351
ro4494351-000
d9k857j81i ,
tozadenant [usan:inn]
1-piperidinecarboxamide, 4-hydroxy-n-(4-methoxy-7-(4-morpholinyl)-2-benzothiazolyl)-4-methyl-
4-hydroxy-n-(4-methoxy-7-morpholinobenzo[d]thiazol-2-yl)-4-methylpiperidine-1-carboxamide
a-2a (3)
ro-4494351-000
CHEMBL2105747
a2a-(3)
ro-4494351000
ro-4494351-002
AKOS016005201
4-hydroxy-n-[4-methoxy-7-(4-morpholinyl)-2-benzothiazolyl]-4-methyl-1-piperidinecarboxamide
PB19761
CS-0359
4-hydroxy-n-(4-methoxy-7-(4-morpholinyl)-2-benzothiazolyl)-4-methyl-1-piperidinecarboxamide
gtpl5611
tozadenant [inn]
tozadenant [who-dd]
tozadenant [usan]
SCHEMBL1628246
a2a
bdbm50011294
J-515524
mfcd21642026
NCGC00378653-02
4-hydroxy-n-[4-methoxy-7-(4-morpholinyl)-2-benzo-thiazolyl]-4-methyl-1-piperidinecarboxamide
DB12203
9xw ,
BCP06963
ro-4494351; ro4494351; ro 4494351;syn115; syn 115; tozadenant
4-hydroxy-4-methyl-piperidine-1-carboxylic acid(4-methoxy-7-morpholin-4-yl-benzothiazol-2-yl)-amide
XNBRWUQWSKXMPW-UHFFFAOYSA-N
4-methoxy-7-morpholino-2-[(4-hydroxy-4-methylpiperidino)carbonylamino]benzothiazole
AS-34303
Q27089009
A862938
VJB07055

Excerpt	Reference	Relevance
"Tozadenant (SYN115) is an oral, selective adenosine A2A receptor antagonist that improves motor function in animal models of Parkinson's disease."	( Tozadenant (SYN115) in patients with Parkinson's disease who have motor fluctuations on levodopa: a phase 2b, double-blind, randomised trial. Bandak, S; Docu-Axelerad, A; Hauser, RA; Kenney, C; Kieburtz, KD; Kozyolkin, O; Lew, M; Meya, U; Neale, A; Olanow, CW; Pourcher, E; Resburg, C, 2014)	2.57

Excerpt	Reference	Relevance
" In vitro and preclinical in vivo pharmacokinetic (PK) properties of tozadenant were studied through the developed bioanalytical methods, and human PK profiles were predicted using physiologically based pharmacokinetic (PBPK) modeling based on these values."	( Quantitative Analysis of Tozadenant Using Liquid Chromatography-Mass Spectrometric Method in Rat Plasma and Its Human Pharmacokinetics Prediction Using Physiologically Based Pharmacokinetic Modeling. Byeon, JJ; Choi, J; Kim, N; Lee, BI; Park, MH; Park, Y; Shin, SH; Shin, YG, 2019)	1.05

Excerpt	Reference	Relevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."	( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)	0.51

Excerpt	Relevance	Reference
" Rats were dosed orally with Tozadenant, a selective A2A receptor antagonist, and three different doses of Radiprodil, an NR2B-selective NMDA receptor antagonist."	( Behavioural Assessment of the A2a/NR2B Combination in the Unilateral 6-OHDA-Lesioned Rat Model: A New Method to Examine the Therapeutic Potential of Non-Dopaminergic Drugs. De Wolf, C; Downey, P; Michel, A; Scheller, D; Schwarting, R; Van Damme, X, 2015)	0.71

Class	Description
benzothiazoles
[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 Targets (13)

Potency Measurements

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4	Homo sapiens (human)	Potency	18.9991	0.0123	7.9835	43.2770	AID1645841
G	Vesicular stomatitis virus	Potency	26.8370	0.0123	8.9648	39.8107	AID1645842
cytochrome P450 2D6	Homo sapiens (human)	Potency	16.9330	0.0010	8.3798	61.1304	AID1645840
Interferon beta	Homo sapiens (human)	Potency	26.8370	0.0033	9.1582	39.8107	AID1645842
HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)	Potency	26.8370	0.0123	8.9648	39.8107	AID1645842
Inositol hexakisphosphate kinase 1	Homo sapiens (human)	Potency	26.8370	0.0123	8.9648	39.8107	AID1645842
cytochrome P450 2C9, partial	Homo sapiens (human)	Potency	26.8370	0.0123	8.9648	39.8107	AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Adenosine receptor A3	Homo sapiens (human)	Ki	3.2850	0.0000	0.9306	10.0000	AID1138025; AID1436489
Cytochrome P450 2D6	Homo sapiens (human)	Ki	5.0000	0.0001	1.1986	8.0000	AID1436489
Adenosine receptor A2a	Homo sapiens (human)	Ki	0.0059	0.0000	1.0609	9.7920	AID1138023; AID1436480; AID1436484; AID1687718; AID1696179; AID1731438; AID1871328; AID1871331; AID1873117
Adenosine receptor A2b	Homo sapiens (human)	Ki	2.1333	0.0002	1.6352	10.0000	AID1138021; AID1436488; AID1696176
Adenosine receptor A1	Homo sapiens (human)	Ki	1.9533	0.0002	0.9316	10.0000	AID1138024; AID1436487; AID1687716; AID1696177; AID1731440; AID1873118
Adenosine receptor A2a	Rattus norvegicus (Norway rat)	Ki	0.0187	0.0002	1.4940	10.0000	AID1731439
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (165)

Process	via Protein(s)	Taxonomy
cell surface receptor signaling pathway via JAK-STAT	Interferon beta	Homo sapiens (human)
response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
B cell activation involved in immune response	Interferon beta	Homo sapiens (human)
cell surface receptor signaling pathway	Interferon beta	Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STAT	Interferon beta	Homo sapiens (human)
response to virus	Interferon beta	Homo sapiens (human)
positive regulation of autophagy	Interferon beta	Homo sapiens (human)
cytokine-mediated signaling pathway	Interferon beta	Homo sapiens (human)
natural killer cell activation	Interferon beta	Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT protein	Interferon beta	Homo sapiens (human)
cellular response to interferon-beta	Interferon beta	Homo sapiens (human)
B cell proliferation	Interferon beta	Homo sapiens (human)
negative regulation of viral genome replication	Interferon beta	Homo sapiens (human)
innate immune response	Interferon beta	Homo sapiens (human)
positive regulation of innate immune response	Interferon beta	Homo sapiens (human)
regulation of MHC class I biosynthetic process	Interferon beta	Homo sapiens (human)
negative regulation of T cell differentiation	Interferon beta	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Interferon beta	Homo sapiens (human)
defense response to virus	Interferon beta	Homo sapiens (human)
type I interferon-mediated signaling pathway	Interferon beta	Homo sapiens (human)
neuron cellular homeostasis	Interferon beta	Homo sapiens (human)
cellular response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
cellular response to virus	Interferon beta	Homo sapiens (human)
negative regulation of Lewy body formation	Interferon beta	Homo sapiens (human)
negative regulation of T-helper 2 cell cytokine production	Interferon beta	Homo sapiens (human)
positive regulation of apoptotic signaling pathway	Interferon beta	Homo sapiens (human)
response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
B cell differentiation	Interferon beta	Homo sapiens (human)
natural killer cell activation involved in immune response	Interferon beta	Homo sapiens (human)
adaptive immune response	Interferon beta	Homo sapiens (human)
T cell activation involved in immune response	Interferon beta	Homo sapiens (human)
humoral immune response	Interferon beta	Homo sapiens (human)
positive regulation of T cell mediated cytotoxicity	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
adaptive immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independent	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of T cell anergy	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
defense response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
detection of bacterium	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of interleukin-12 production	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of interleukin-6 production	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protection from natural killer cell mediated cytotoxicity	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
innate immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of dendritic cell differentiation	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class Ib	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
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)
xenobiotic metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
coumarin metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
alkaloid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
alkaloid catabolic process	Cytochrome P450 2D6	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
isoquinoline alkaloid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 2D6	Homo sapiens (human)
retinol metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 2D6	Homo sapiens (human)
negative regulation of binding	Cytochrome P450 2D6	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 2D6	Homo sapiens (human)
negative regulation of cellular organofluorine metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
arachidonic acid metabolic process	Cytochrome P450 2D6	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)
inositol phosphate metabolic process	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic process	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
negative regulation of cold-induced thermogenesis	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol phosphate biosynthetic process	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (41)

Process	via Protein(s)	Taxonomy
cytokine activity	Interferon beta	Homo sapiens (human)
cytokine receptor binding	Interferon beta	Homo sapiens (human)
type I interferon receptor binding	Interferon beta	Homo sapiens (human)
protein binding	Interferon beta	Homo sapiens (human)
chloramphenicol O-acetyltransferase activity	Interferon beta	Homo sapiens (human)
TAP binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
signaling receptor binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protein binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
peptide antigen binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
TAP binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protein-folding chaperone binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
G protein-coupled adenosine receptor activity	Adenosine receptor A3	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 2D6	Homo sapiens (human)
iron ion binding	Cytochrome P450 2D6	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 2D6	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Cytochrome P450 2D6	Homo sapiens (human)
heme binding	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 8,9 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 11,12 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 14,15 epoxidase activity	Cytochrome P450 2D6	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)
inositol-1,3,4,5,6-pentakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol heptakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 5-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
protein binding	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
ATP binding	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 1-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 3-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (41)

Process	via Protein(s)	Taxonomy
extracellular space	Interferon beta	Homo sapiens (human)
extracellular region	Interferon beta	Homo sapiens (human)
Golgi membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
endoplasmic reticulum	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
Golgi apparatus	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
plasma membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
cell surface	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
ER to Golgi transport vesicle membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
secretory granule membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
phagocytic vesicle membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
early endosome membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
recycling endosome membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
extracellular exosome	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
lumenal side of endoplasmic reticulum membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
MHC class I protein complex	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
extracellular space	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
external side of plasma membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
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)
mitochondrion	Cytochrome P450 2D6	Homo sapiens (human)
endoplasmic reticulum	Cytochrome P450 2D6	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 2D6	Homo sapiens (human)
cytoplasm	Cytochrome P450 2D6	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2D6	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)
fibrillar center	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
nucleoplasm	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
cytosol	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
nucleus	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
cytoplasm	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (48)

Assay ID	Title	Year	Journal	Article
AID1138058	Plasma clearance in dog	2014	Journal of medicinal chemistry, May-08, Volume: 57, Issue:9	Adenosine A2A receptor as a drug discovery target.
AID1138054	Selectivity ratio of EC50 for human recombinant adenosine A1 receptor to EC50 for human recombinant adenosine receptor A2a by cAMP formation assay	2014	Journal of medicinal chemistry, May-08, Volume: 57, Issue:9	Adenosine A2A receptor as a drug discovery target.
AID1436487	Displacement of [3H]-DPCPX from human adenosine A1 receptor expressed in HEK293 cell membranes measured after 90 mins	2017	Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2	Design, Synthesis of Novel, Potent, Selective, Orally Bioavailable Adenosine A
AID1436529	Inhibition of CYP2D6 in human liver microsomes at 5 to 25 uM using dextromethorphan as substrate preincubated for 5 mins with substrate followed by NADPH addition measured after 10 mins by LC-MS/MS analysis	2017	Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2	Design, Synthesis of Novel, Potent, Selective, Orally Bioavailable Adenosine A
AID1696177	Inhibition of human adenosine A1 receptor
AID1138049	Plasma clearance in rat	2014	Journal of medicinal chemistry, May-08, Volume: 57, Issue:9	Adenosine A2A receptor as a drug discovery target.
AID1138059	Volume of distribution in rat	2014	Journal of medicinal chemistry, May-08, Volume: 57, Issue:9	Adenosine A2A receptor as a drug discovery target.
AID1696211	Half life in mouse at 2 mg/kg, iv or 10 mg/kg, po measured up to 24 hrs by LC-MS/MS analysis
AID1731440	Displacement of [3H]-DPCPX from recombinant human A1 receptor expressed in CHO-K1 cells incubated for 70 mins by liquid scintillation counting method	2021	European journal of medicinal chemistry, Mar-15, Volume: 214	Design, synthesis and biological evaluation of Tozadenant analogues as adenosine A
AID1436491	Antagonist activity at human adenosine A2B receptor expressed in HEK293 cell membranes assessed as decrease in NECA/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 15 mins and subsequent forskolin stimulation measured	2017	Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2	Design, Synthesis of Novel, Potent, Selective, Orally Bioavailable Adenosine A
AID1138057	Half life in dog	2014	Journal of medicinal chemistry, May-08, Volume: 57, Issue:9	Adenosine A2A receptor as a drug discovery target.
AID1871328	Antagonist activity at adenosine A2A receptor (unknown origin)	2022	European journal of medicinal chemistry, Jan-05, Volume: 227	Adenosine receptor antagonists: Recent advances and therapeutic perspective.
AID1436528	Inhibition of CYP2C19 in human liver microsomes at 5 to 25 uM using (S)mephenytoin as substrate preincubated for 5 mins with substrate followed by NADPH addition measured after 40 mins by LC-MS/MS analysis	2017	Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2	Design, Synthesis of Novel, Potent, Selective, Orally Bioavailable Adenosine A
AID1436480	Displacement of [3H]ZM241385 from human adenosine A2A receptor expressed in HEK293 cell membranes measured after 90 mins	2017	Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2	Design, Synthesis of Novel, Potent, Selective, Orally Bioavailable Adenosine A
AID1696212	Cmax in mouse at 1 mg/kg, iv measured up to 24 hrs by LC-MS/MS analysis
AID1138056	Half life in rat	2014	Journal of medicinal chemistry, May-08, Volume: 57, Issue:9	Adenosine A2A receptor as a drug discovery target.
AID1436492	Inhibition of CYP1A2 in human liver microsomes at 5 to 25 uM using phenacetin as substrate preincubated for 5 mins with substrate followed by NADPH addition measured after 10 mins by LC-MS/MS analysis	2017	Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2	Design, Synthesis of Novel, Potent, Selective, Orally Bioavailable Adenosine A
AID1436488	Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes measured after 90 mins	2017	Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2	Design, Synthesis of Novel, Potent, Selective, Orally Bioavailable Adenosine A
AID1138062	Oral bioavailability in dog at 5 mg/kg	2014	Journal of medicinal chemistry, May-08, Volume: 57, Issue:9	Adenosine A2A receptor as a drug discovery target.
AID1871331	Binding affinity to human adenosine A2A receptor measured by radioligand-based affinity assay	2022	European journal of medicinal chemistry, Jan-05, Volume: 227	Adenosine receptor antagonists: Recent advances and therapeutic perspective.
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.
AID1138061	Oral bioavailability in rat at 5 mg/kg	2014	Journal of medicinal chemistry, May-08, Volume: 57, Issue:9	Adenosine A2A receptor as a drug discovery target.
AID1873118	Antagonist activity at human adenosine A1 receptor	2022	European journal of medicinal chemistry, Jul-05, Volume: 237	Discovery of small-molecule compounds and natural products against Parkinson's disease: Pathological mechanism and structural modification.
AID1687718	Displacement of [3H]MSX2 from human adenosine receptor A2A expressed in HEK293 cell membranes incubated for 30 mins by radioligand competition assay
AID1436527	Inhibition of CYP2C9 in human liver microsomes at 5 to 25 uM using diclofenac as substrate preincubated for 5 mins with substrate followed by NADPH addition measured after 10 mins by LC-MS/MS analysis	2017	Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2	Design, Synthesis of Novel, Potent, Selective, Orally Bioavailable Adenosine A
AID1696176	Inhibition of human adenosine 2B receptor
AID1731439	Displacement of [3H]-ZM241385 from A2A receptor in rat brain corpora striata incubated for 70 mins by liquid scintillation counting method	2021	European journal of medicinal chemistry, Mar-15, Volume: 214	Design, synthesis and biological evaluation of Tozadenant analogues as adenosine A
AID1436526	Neuroprotective activity in 6-OHDA-lesioned Wistar rat model of parkinson disease assessed as increase in L-DOPA induced contralateral rotations at 30 mg/kg, po pretreated for 30 mins followed by benserazide addition and subsequent L-DOPA stimulation for	2017	Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2	Design, Synthesis of Novel, Potent, Selective, Orally Bioavailable Adenosine A
AID1436490	Antagonist activity at human adenosine A1 receptor expressed in HEK293 cell membranes assessed as decrease in CPA/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 15 mins and subsequent forskolin stimulation measured af	2017	Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2	Design, Synthesis of Novel, Potent, Selective, Orally Bioavailable Adenosine A
AID1436530	Inhibition of CYP3A in human liver microsomes at 5 to 25 uM using testosterone as substrate preincubated for 5 mins with substrate followed by NADPH addition measured after 10 mins by LC-MS/MS analysis	2017	Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2	Design, Synthesis of Novel, Potent, Selective, Orally Bioavailable Adenosine A
AID1873117	Antagonist activity at human adenosine A2A receptor	2022	European journal of medicinal chemistry, Jul-05, Volume: 237	Discovery of small-molecule compounds and natural products against Parkinson's disease: Pathological mechanism and structural modification.
AID1138060	Volume of distribution in dog	2014	Journal of medicinal chemistry, May-08, Volume: 57, Issue:9	Adenosine A2A receptor as a drug discovery target.
AID1731438	Displacement of [3H]-ZM241385 from recombinant human A2A receptor expressed in CHO-K1 cells incubated for 70 mins by liquid scintillation counting method	2021	European journal of medicinal chemistry, Mar-15, Volume: 214	Design, synthesis and biological evaluation of Tozadenant analogues as adenosine A
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.
AID1696179	Antagonist activity at human adenosine 2A receptor (409 to 412 residues) expressed in CHO cells using Ysi-poly-1-lysine as substrate incubated for 1 hr in presence of 3H-SCH-58261 by scintillation counting method
AID1436489	Displacement of [3H]-HEMADO from human adenosine A3 receptor expressed in HEK293 cell membranes measured after 90 mins	2017	Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2	Design, Synthesis of Novel, Potent, Selective, Orally Bioavailable Adenosine A
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.
AID1436484	Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation meas	2017	Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2	Design, Synthesis of Novel, Potent, Selective, Orally Bioavailable Adenosine A
AID1731441	Selectivity index, ratio of Ki for recombinant human A2A receptor expressed in CHO-K1 cells to Ki for recombinant human A1 receptor expressed in CHO-K1 cells	2021	European journal of medicinal chemistry, Mar-15, Volume: 214	Design, synthesis and biological evaluation of Tozadenant analogues as adenosine A
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.
AID1687716	Displacement of [3H]CCPA from human adenosine receptor A1 expressed in CHO cell membranes incubated for 90 mins by radioligand competition assay
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.
AID1296008	Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening	2020	SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347159	Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347160	Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1345618	Human A2A receptor (Adenosine receptors)	2014	Journal of medicinal chemistry, May-08, Volume: 57, Issue:9	Adenosine A2A receptor as a drug discovery target.
[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	0 (0.00)	29.6817
2010's	10 (55.56)	24.3611
2020's	8 (44.44)	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	1 (5.56%)	5.53%
Reviews	3 (16.67%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	14 (77.78%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
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
theophylline [no description available]	4.19	2	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
benserazide Benserazide: An inhibitor of DOPA DECARBOXYLASE that does not enter the central nervous system. It is often given with LEVODOPA in the treatment of parkinsonism to prevent the conversion of levodopa to dopamine in the periphery, thereby increasing the amount that reaches the central nervous system and reducing the required dose. It has no antiparkinson actions when given alone.. benserazide : A carbohydrazide that results from the formal condensation of the carboxy group of DL-serine with the primary amino group of 4-(hydrazinylmethyl)benzene-1,2,3-triol. An aromatic-L-amino-acid decarboxylase inhibitor (DOPA decarboxylase inhibitor) that does not enter the central nervous system, it is used as its hydrochloride salt as an adjunct to levodopa in the treatment of parkinsonism. By preventing the conversion of levodopa to dopamine in the periphery, it causes an increase in the amount of levodopa reaching the central nervous system and so reduces the required dose. Benserazide has no antiparkinson actions when given alone.	2.11	1	0	carbohydrazide; catechols; primary alcohol; primary amino compound	antiparkinson drug; dopaminergic agent; EC 4.1.1.28 (aromatic-L-amino-acid decarboxylase) inhibitor
caffeine [no description available]	4.19	2	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.	2.21	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.	3.19	1	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
oxidopamine Oxidopamine: A neurotransmitter analogue that depletes noradrenergic stores in nerve endings and induces a reduction of dopamine levels in the brain. Its mechanism of action is related to the production of cytolytic free-radicals.. oxidopamine : A benzenetriol that is phenethylamine in which the hydrogens at positions 2, 4, and 5 on the phenyl ring are replaced by hydroxy groups. It occurs naturally in human urine, but is also produced as a metabolite of the drug DOPA (used for the treatment of Parkinson's disease).	2.51	2	0	benzenetriol; catecholamine; primary amino compound	drug metabolite; human metabolite; neurotoxin
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	11.65	5	1	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
2-chloroadenosine 5-chloroformycin A: structure given in first source	3.19	1	0	purine nucleoside
adenosine quinquefolan B: isolated from roots of Panax quinquefolium L.; RN not in Chemline 10/87; RN from Toxlit	3.65	2	0	adenosines; purines D-ribonucleoside	analgesic; anti-arrhythmia drug; fundamental metabolite; human metabolite; vasodilator agent
3-n-butylphthalide 3-n-butylphthalide: isolated from phenolic part of Ligusticum wallichii Franch; structure given in first source	3.51	1	0	benzofurans
rolofylline rolofylline: selective antagonist for adenosine receptors; a cardiovascular agent	3.51	1	0	oxopurine
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.	2.8	3	0	1,2,3-triazole
2,3,6-trimethyl-1,4-naphthoquinone 2,3,6-trimethyl-1,4-naphthoquinone: isolated from tobacco; structure in first source	3.51	1	0
ro 8-0576 benserazide, levodopa drug combination: combination of L-Dopa and seryltrihydroxybenzylhydrazine; used in treatment of parkinsonism	2.11	1	0
zm 241385 ZM 241385: a high affinity radioligand selective for the A2a adenosine receptor	4.19	2	0	diamino-1,3,5-triazine
sch 58261 [no description available]	4.86	3	0	triazolopyrimidines
regadenoson [no description available]	3.19	1	0	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.	3.19	1	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
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.	4.19	2	0	[2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol	antimalarial
n-(3-chlorophenyl)picolinamide N-(3-chlorophenyl)picolinamide: a metabotropic glutamate receptor 4 (mGlu4) positive allosteric modulator; structure in first source	3.51	1	0
2-((2-aminoethylamino)carbonylethylphenylethylamino)-5'-n-ethylcarboxamidoadenosine 2-((2-aminoethylamino)carbonylethylphenylethylamino)-5'-N-ethylcarboxamidoadenosine: structure given in first source	3.19	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.	4.19	2	0	adenosines; dicarboxylic acid monoamide; monocarboxylic acid	adenosine A2A receptor agonist; anti-inflammatory agent
2-phenoxy-N-[5-(5,6,7,8-tetrahydronaphthalen-2-yl)-1,3,4-oxadiazol-2-yl]acetamide [no description available]	3.51	1	0	tetralins
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]	4.69	4	0	oxopurine
mrs 1754 [no description available]	3.51	1	0	oxopurine
cv 1808 2-phenylaminoadenosine: has coronary & cardiohemodynamic effects	3.19	1	0	purine nucleoside
pd 174494 PD 174494: structure in first source	2.1	1	0	piperidines
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
binodenoson [no description available]	3.19	1	0
atl 146e BMS-068645: structure in first source	3.19	1	0
st 1535 [no description available]	3.19	1	0
2-(2-(4-chlorophenyl)ethoxy)adenosine 2-(2-(4-chlorophenyl)ethoxy)adenosine: a adenosine A2A receptor agonist	3.19	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]	4.19	2	0
psb 36 1-butyl-8-(3-noradamantyl)-3-(3-hydroxypropyl)xanthine: an A1 receptor antagonist	3.51	1	0	oxopurine
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	4.19	2	0
psb603 PSB603: an adenosine A2B receptor antagonist	3.51	1	0
piperidines Piperidines: A family of hexahydropyridines.	2.1	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
Congenital Zika Syndrome [description not available]	0	2.25	1	0
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	0	2.83	3	0
Zika Virus Infection A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.	0	2.25	1	0
Degenerative Diseases, Central Nervous System [description not available]	0	3.33	1	0
Idiopathic Parkinson Disease [description not available]	0	6.47	5	1
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)	1	8.47	5	1
Neurodegenerative Diseases Hereditary and sporadic conditions which are characterized by progressive nervous system dysfunction. These disorders are often associated with atrophy of the affected central or peripheral nervous system structures.	0	3.33	1	0
Dyskinesia, Medication-Induced [description not available]	0	4.83	2	1
MPTP Neurotoxicity Syndrome [description not available]	0	2.15	1	0
Dyskinesia, Drug-Induced Abnormal movements, including HYPERKINESIS; HYPOKINESIA; TREMOR; and DYSTONIA, associated with the use of certain medications or drugs. Muscles of the face, trunk, neck, and extremities are most commonly affected. Tardive dyskinesia refers to abnormal hyperkinetic movements of the muscles of the face, tongue, and neck associated with the use of neuroleptic agents (see ANTIPSYCHOTIC AGENTS). (Adams et al., Principles of Neurology, 6th ed, p1199)	0	4.83	2	1
Atherosclerotic Parkinsonism [description not available]	0	2.1	1	0
Parkinson Disease, Secondary Conditions which feature clinical manifestations resembling primary Parkinson disease that are caused by a known or suspected condition. Examples include parkinsonism caused by vascular injury, drugs, trauma, toxin exposure, neoplasms, infections and degenerative or hereditary conditions. Clinical features may include bradykinesia, rigidity, parkinsonian gait, and masked facies. In general, tremor is less prominent in secondary parkinsonism than in the primary form. (From Joynt, Clinical Neurology, 1998, Ch38, pp39-42)	0	2.1	1	0

tozadenant

Description

Cross-References

Synonyms (53)

Research Excerpts

Overview

Pharmacokinetics

Bioavailability

Dosage Studied

Drug Classes (1)

Protein Targets (13)

Potency Measurements

Inhibition Measurements

Biological Processes (165)

Molecular Functions (41)

Ceullar Components (41)

Bioassays (48)

Research

Studies (18)

Market Indicators

Research Demand Index: 24.92

Study Types

tozadenant

Description

Cross-References

Synonyms (53)

Research Excerpts

Overview

Pharmacokinetics

Bioavailability

Dosage Studied

Drug Classes (1)

Protein Targets (13)

Potency Measurements

Inhibition Measurements

Biological Processes (165)

Molecular Functions (41)

Ceullar Components (41)

Bioassays (48)

Research

Studies (18)

Market Indicators

Research Demand Index: 24.92

Study Types

Related Drugs (41)

Related Conditions (12)