kfm 19 profile

KFM 19: a potential cognitive enhancer and a selective adenosine A1 receptor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	131584
CHEMBL ID	84545
SCHEMBL ID	194999
MeSH ID	M0215445

Synonym
CHEMBL84545 ,
L001424
bdbm50003018
8-(3-oxo-cyclopentyl)-1,3-dipropyl-3,7-dihydro-purine-2,6-dione
8-(3-oxocyclopentyl)-1,3-dipropyl-7h-purine-2,6-dione
biip 20
((s)-(-)-8-(3-oxocyclopentyl)-1,3-dipropyl-7h-purine-2,6-dione)
1h-purine-2,6-dione, 3,7-dihydro-8-(3-oxocyclopentyl)-1,3-dipropyl-
133058-72-7
biip-20
kfm-19
kfm 19
SCHEMBL194999
1,3-dipropyl-8-(3-oxocyclopentyl)-xanthine
1,3-dipropyl-8-(1-oxo-3-cyclopentyl)xanthine
RUHGOZFOVBMWOO-UHFFFAOYSA-N
kfm19
HY-U00251
CS-7436
154601-67-9
(r)-8-(3-oxocyclopentyl)-1,3-dipropyl-1h-purine-2,6(3h,7h)-dione
MS-24700
8-(3-oxocyclopentyl)-1,3-dipropyl-3,7-dihydro-1h-purine-2,6-dione
DTXSID20870000
AKOS040741912

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Adenosine receptor A1	Rattus norvegicus (Norway rat)	Ki	0.0105	0.0001	1.2092	9.9700	AID32177
Adenosine receptor A1	Bos taurus (cattle)	Ki	0.0150	0.0000	0.7131	6.0000	AID31984
Adenosine receptor A2a	Homo sapiens (human)	Ki	1.9080	0.0000	1.0609	9.7920	AID30486; AID30502
Adenosine receptor A2b	Homo sapiens (human)	Ki	2.1060	0.0002	1.6352	10.0000	AID30486; AID30502
Adenosine receptor A2b	Rattus norvegicus (Norway rat)	Ki	2.7000	0.0006	1.3536	10.0000	AID33740
Adenosine receptor A1	Homo sapiens (human)	Ki	0.0105	0.0002	0.9316	10.0000	AID31833
Adenosine receptor A2a	Rattus norvegicus (Norway rat)	Ki	2.7000	0.0002	1.4940	10.0000	AID33740
Adenosine receptor A1	Cavia porcellus (domestic guinea pig)	Ki	0.0150	0.0003	0.4546	6.9000	AID32289; AID32294
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Adenosine receptor A2b	Rattus norvegicus (Norway rat)	Ratio	1.5100	0.0033	0.8292	9.6000	AID33746
Adenosine receptor A2a	Rattus norvegicus (Norway rat)	Ratio	1.5100	0.0033	0.8230	9.6000	AID33746
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

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

Process	via Protein(s)	Taxonomy
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (34)

Assay ID	Title	Year	Journal	Article
AID108720	Acquisition time in (R)-PIA) induced avoidance test (performed in mice) for antagonistic activity after peroral administration of 0.31 mg/kg (n=15)	1993	Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17	Adenosine A1 antagonists. 3. Structure-activity relationships on amelioration against scopolamine- or N6-((R)-phenylisopropyl)adenosine-induced cognitive disturbance.
AID108723	Acquisition time in (R)-PIA) induced avoidance test (performed in mice) for antagonistic activity after peroral administration of 1.25 mg/kg (n=15)	1993	Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17	Adenosine A1 antagonists. 3. Structure-activity relationships on amelioration against scopolamine- or N6-((R)-phenylisopropyl)adenosine-induced cognitive disturbance.
AID170575	Acquisition time in Scopolamine induced avoidance test (performed in rat) for antagonistic activity after peroral administration of 0.02 mg/kg (n=18)	1993	Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17	Adenosine A1 antagonists. 3. Structure-activity relationships on amelioration against scopolamine- or N6-((R)-phenylisopropyl)adenosine-induced cognitive disturbance.
AID30503	Ratio of binding to adenosine A2 and A1 receptors	1992	Journal of medicinal chemistry, Sep-18, Volume: 35, Issue:19	7,8-Dihydro-8-ethyl-2-(3-noradamantyl)-4-propyl-1H-imidazo[2,1-i]purin-5(4H)-one: a potent and water-soluble adenosine A1 antagonist.
AID30486	Binding affinity against Adenosine A2 receptor from rhesus moneky striatum with N-[3H] ethyladenosin-5''-uronamide (NECA) and 30 nM (R)-PIA	1993	Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17	Adenosine A1 antagonists. 3. Structure-activity relationships on amelioration against scopolamine- or N6-((R)-phenylisopropyl)adenosine-induced cognitive disturbance.
AID32289	Binding affinity towards adenosine A1 receptor using N6-[3H]cyclohexyladenosine in guinea pig forebrain membranes	1992	Journal of medicinal chemistry, Sep-18, Volume: 35, Issue:19	7,8-Dihydro-8-ethyl-2-(3-noradamantyl)-4-propyl-1H-imidazo[2,1-i]purin-5(4H)-one: a potent and water-soluble adenosine A1 antagonist.
AID33740	Binding affinity at Adenosine A2 receptor from rat striatal membranes by N-[3H] ethyladenosin-5'- uronamide displacement.	1993	Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17	Adenosine A1 antagonists. 3. Structure-activity relationships on amelioration against scopolamine- or N6-((R)-phenylisopropyl)adenosine-induced cognitive disturbance.
AID191563	Retention time in Scopolamine induced avoidance test (performed in rat) for antagonistic activity after peroral administration of 0.31 mg/kg (n=18) (P<0.005)	1993	Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17	Adenosine A1 antagonists. 3. Structure-activity relationships on amelioration against scopolamine- or N6-((R)-phenylisopropyl)adenosine-induced cognitive disturbance.
AID170586	Acquisition time in Scopolamine induced avoidance test (performed in rat) for antagonistic activity after peroral administration of 1.25 mg/kg (n=18)	1993	Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17	Adenosine A1 antagonists. 3. Structure-activity relationships on amelioration against scopolamine- or N6-((R)-phenylisopropyl)adenosine-induced cognitive disturbance.
AID191546	Retention time in Scopolamine induced avoidance test (performed in mice) for antagonistic activity after peroral administration of 1.25 mg/kg (n=18) (P<0.05)	1993	Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17	Adenosine A1 antagonists. 3. Structure-activity relationships on amelioration against scopolamine- or N6-((R)-phenylisopropyl)adenosine-induced cognitive disturbance.
AID108852	Acquisition time in (R)-PIA) induced avoidance test (performed in mice) for antagonistic activity after peroral administration of 5 mg/kg (n=15)	1993	Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17	Adenosine A1 antagonists. 3. Structure-activity relationships on amelioration against scopolamine- or N6-((R)-phenylisopropyl)adenosine-induced cognitive disturbance.
AID170584	Acquisition time in Scopolamine induced avoidance test (performed in rat) for antagonistic activity after peroral administration of 0.31 mg/kg (n=18)	1993	Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17	Adenosine A1 antagonists. 3. Structure-activity relationships on amelioration against scopolamine- or N6-((R)-phenylisopropyl)adenosine-induced cognitive disturbance.
AID33752	Ratio of A2 to A1.	1992	Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3	Adenosine receptors: pharmacology, structure-activity relationships, and therapeutic potential.
AID32177	Binding affinity against adenosine A1 receptor using [3H]-CHA or [3H]PIA as radioligand	1992	Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3	Adenosine receptors: pharmacology, structure-activity relationships, and therapeutic potential.
AID191554	Retention time in Scopolamine induced avoidance test (performed in rat) for antagonistic activity after peroral administration of 0.02 mg/kg (n=18) (P<0.05)	1993	Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17	Adenosine A1 antagonists. 3. Structure-activity relationships on amelioration against scopolamine- or N6-((R)-phenylisopropyl)adenosine-induced cognitive disturbance.
AID32294	Binding affinity against Adenosine A1 receptor from guinea pig forebrain membranes by N6-[3H]- cyclohexyladenosine displacement.	1993	Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17	Adenosine A1 antagonists. 3. Structure-activity relationships on amelioration against scopolamine- or N6-((R)-phenylisopropyl)adenosine-induced cognitive disturbance.
AID21763	Solubility was measured in saline	1992	Journal of medicinal chemistry, Sep-18, Volume: 35, Issue:19	7,8-Dihydro-8-ethyl-2-(3-noradamantyl)-4-propyl-1H-imidazo[2,1-i]purin-5(4H)-one: a potent and water-soluble adenosine A1 antagonist.
AID118926	Retention time in (R)-PIA) induced avoidance test (performed in mice) for antagonistic activity after peroral administration of 0.31 mg/kg (n=15) (P<0.01)	1993	Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17	Adenosine A1 antagonists. 3. Structure-activity relationships on amelioration against scopolamine- or N6-((R)-phenylisopropyl)adenosine-induced cognitive disturbance.
AID30502	Binding affinity for adenosine A2 receptor using N-[3H]-ethyladenosin-5''-uronamide in guinea pig forebrain membranes	1992	Journal of medicinal chemistry, Sep-18, Volume: 35, Issue:19	7,8-Dihydro-8-ethyl-2-(3-noradamantyl)-4-propyl-1H-imidazo[2,1-i]purin-5(4H)-one: a potent and water-soluble adenosine A1 antagonist.
AID108717	Acquisition time in (R)-PIA) induced avoidance test (performed in mice) for antagonistic activity after peroral administration of 0.08 mg/kg (n=15)	1993	Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17	Adenosine A1 antagonists. 3. Structure-activity relationships on amelioration against scopolamine- or N6-((R)-phenylisopropyl)adenosine-induced cognitive disturbance.
AID229793	Ratio of Ki for A2 and A1 adenosine receptors	1993	Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17	Adenosine A1 antagonists. 3. Structure-activity relationships on amelioration against scopolamine- or N6-((R)-phenylisopropyl)adenosine-induced cognitive disturbance.
AID118933	Retention time in (R)-PIA) induced avoidance test (performed in mice) for antagonistic activity after peroral administration of 20 mg/kg (n=15) (P<0.05)	1993	Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17	Adenosine A1 antagonists. 3. Structure-activity relationships on amelioration against scopolamine- or N6-((R)-phenylisopropyl)adenosine-induced cognitive disturbance.
AID31833	Binding affinity against Adenosine A1 receptor from rat forebrain membranes with N6-[3H]- cyclohexyladenosine	1993	Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17	Adenosine A1 antagonists. 3. Structure-activity relationships on amelioration against scopolamine- or N6-((R)-phenylisopropyl)adenosine-induced cognitive disturbance.
AID170593	Acquisition time in Scopolamine induced avoidance test (performed in rat) for antagonistic activity after peroral administration of 5 mg/kg (n=18)	1993	Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17	Adenosine A1 antagonists. 3. Structure-activity relationships on amelioration against scopolamine- or N6-((R)-phenylisopropyl)adenosine-induced cognitive disturbance.
AID118929	Retention time in (R)-PIA) induced avoidance test (performed in mice) for antagonistic activity after peroral administration of 1.25 mg/kg (n=15) (P<0.005)	1993	Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17	Adenosine A1 antagonists. 3. Structure-activity relationships on amelioration against scopolamine- or N6-((R)-phenylisopropyl)adenosine-induced cognitive disturbance.
AID21767	Solubility of the compound(10 mg) was measured in water(2.5 mL) at 20 degree celsius for 1 hr	1992	Journal of medicinal chemistry, Sep-18, Volume: 35, Issue:19	7,8-Dihydro-8-ethyl-2-(3-noradamantyl)-4-propyl-1H-imidazo[2,1-i]purin-5(4H)-one: a potent and water-soluble adenosine A1 antagonist.
AID115113	Tested for locomotor activity after oral administration of 2.5 mg/kg for 120 min	1993	Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17	Adenosine A1 antagonists. 3. Structure-activity relationships on amelioration against scopolamine- or N6-((R)-phenylisopropyl)adenosine-induced cognitive disturbance.
AID118921	Retention time in (R)-PIA) induced avoidance test (performed in mice) for antagonistic activity after peroral administration of 0.08 mg/kg (n=15) (P<0.005)	1993	Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17	Adenosine A1 antagonists. 3. Structure-activity relationships on amelioration against scopolamine- or N6-((R)-phenylisopropyl)adenosine-induced cognitive disturbance.
AID31984	Binding affinity at bovine Adenosine A1 receptor.	2002	Journal of medicinal chemistry, Oct-24, Volume: 45, Issue:22	Synthesis, molecular modeling studies, and pharmacological activity of selective A(1) receptor antagonists.
AID33746	Binding affinity against adenosine A2 receptor using [3H]- NECA as radioligand	1992	Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3	Adenosine receptors: pharmacology, structure-activity relationships, and therapeutic potential.
AID115112	Tested for locomotor activity after oral administration of 10 mg/kg for 120 min	1993	Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17	Adenosine A1 antagonists. 3. Structure-activity relationships on amelioration against scopolamine- or N6-((R)-phenylisopropyl)adenosine-induced cognitive disturbance.
AID191574	Retention time in Scopolamine induced avoidance test (performed in rat) for antagonistic activity after peroral administration of 5 mg/kg (n=18) (P<0.05)	1993	Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17	Adenosine A1 antagonists. 3. Structure-activity relationships on amelioration against scopolamine- or N6-((R)-phenylisopropyl)adenosine-induced cognitive disturbance.
AID191558	Retention time in Scopolamine induced avoidance test (performed in rat) for antagonistic activity after peroral administration of 0.08 mg/kg (n=18) (P<0.05)	1993	Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17	Adenosine A1 antagonists. 3. Structure-activity relationships on amelioration against scopolamine- or N6-((R)-phenylisopropyl)adenosine-induced cognitive disturbance.
AID170579	Acquisition time in Scopolamine induced avoidance test (performed in rat) for antagonistic activity after peroral administration of 0.08 mg/kg (n=18)	1993	Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17	Adenosine A1 antagonists. 3. Structure-activity relationships on amelioration against scopolamine- or N6-((R)-phenylisopropyl)adenosine-induced cognitive disturbance.
[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	5 (83.33)	18.2507
2000's	1 (16.67)	29.6817
2010's	0 (0.00)	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 (16.67%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	5 (83.33%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
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.	4.18	5	oxopurine	adenosine A1 receptor antagonist; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor
8-(4-sulfophenyl)theophylline 8-(4-sulfophenyl)theophylline: adenosine antagonist	3.08	1
8-cyclopentyl-1,3-dimethylxanthine 8-cyclopentyl-1,3-dimethylxanthine: prolongs epileptic seizures in rats	3.08	1	oxopurine
8-phenyltheophylline 8-phenyltheophylline: purinergic P1 receptor antagonist	3.08	1
theophylline [no description available]	3.48	2	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
caffeine [no description available]	3.77	3	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
carbamazepine Carbamazepine: A dibenzazepine that acts as a sodium channel blocker. It is used as an anticonvulsant for the treatment of grand mal and psychomotor or focal SEIZURES. It may also be used in the management of BIPOLAR DISORDER, and has analgesic properties.. carbamazepine : A dibenzoazepine that is 5H-dibenzo[b,f]azepine carrying a carbamoyl substituent at the azepine nitrogen, used as an anticonvulsant.	1.98	1	dibenzoazepine; ureas	analgesic; anticonvulsant; antimanic drug; drug allergen; EC 3.5.1.98 (histone deacetylase) inhibitor; environmental contaminant; glutamate transporter activator; mitogen; non-narcotic analgesic; sodium channel blocker; 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.	3.08	1	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
8-(4-((2-aminoethyl)aminocarbonylmethyloxy)phenyl)-1,3-dipropylxanthine 8-(4-((2-aminoethyl)aminocarbonylmethyloxy)phenyl)-1,3-dipropylxanthine: adenosine receptor antagonist	3.49	2
2-chloroadenosine 5-chloroformycin A: structure given in first source	3.08	1	purine nucleoside
oxcarbazepine Oxcarbazepine: A carbamazepine derivative that acts as a voltage-gated sodium channel blocker. It is used for the treatment of PARTIAL SEIZURES with or without secondary generalization. It is also an inducer of CYTOCHROME P-450 CYP3A4.. oxcarbazepine : A dibenzoazepine derivative, having a carbamoyl group at the ring nitrogen, substituted with an oxo group at C-4 of the azepeine ring which is also hydrogenated at C-4 and C-5. It is a anticholinergic anticonvulsant and mood stabilizing drug, used primarily in the treatment of epilepsy.	1.98	1	cyclic ketone; dibenzoazepine	anticonvulsant; drug allergen
rolofylline rolofylline: selective antagonist for adenosine receptors; a cardiovascular agent	3.78	3	oxopurine
1,3-dipropyl-8-(2-amino-4-chlorophenyl)xanthine [no description available]	3.08	1
phenylisopropyladenosine [no description available]	3.08	1	aromatic amine; benzenes; hydrocarbyladenosine; purine nucleoside; secondary amino compound	adenosine A1 receptor agonist; neuroprotective agent
3,7-dimethyl-1-propargylxanthine 3,7-dimethyl-1-propargylxanthine: potent & selective in vivo antagonist of adenosine analogs	3.08	1
n(6)-phenyladenosine [no description available]	3.08	1	purine nucleoside
2-chloro-n(6)cyclopentyladenosine 2-chloro-N(6)cyclopentyladenosine: highly selective agonist at A1 adenosine receptors	3.08	1
cp 66713 CP 66713: adenosine receptor antagonist; structure given in first source	3.08	1
adenosine amine congener adenosine amine congener: a highly potent & selective adenosine A1 receptor agonist	3.08	1
8-(4-carboxymethyloxy)phenyl-1,3-dipropylxanthine 8-(4-carboxymethyloxy)phenyl-1,3-dipropylxanthine: used to localize adenosine receptors in the brain	3.08	1
8-(dicyclopropylmethyl)-1,3-dipropylxanthine 8-(dicyclopropylmethyl)-1,3-dipropylxanthine: selective A1 adenosine receptor antagonist; structure given in first source	3.77	3
2-(1-octynyl)adenosine YT 146: an adenosine receptor agonist; structure given in first source	3.08	1
8-cyclohexylcaffeine [no description available]	3.08	1
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.	3.08	1	adenosines; monocarboxylic acid amide	adenosine A1 receptor agonist; adenosine A2A receptor agonist; antineoplastic agent; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; vasodilator agent
n(6)-cyclopentyladenosine [no description available]	3.08	1
fk 838 FK 838: an adenosine subtype-1 receptor antagonist; structure given in first source	2.01	1
2-((2-aminoethylamino)carbonylethylphenylethylamino)-5'-n-ethylcarboxamidoadenosine 2-((2-aminoethylamino)carbonylethylphenylethylamino)-5'-N-ethylcarboxamidoadenosine: structure given in first source	3.08	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.	3.08	1	adenosines; dicarboxylic acid monoamide; monocarboxylic acid	adenosine A2A receptor agonist; anti-inflammatory agent
kf 17837 [no description available]	1.98	1
cv 1808 2-phenylaminoadenosine: has coronary & cardiohemodynamic effects	3.08	1	purine nucleoside
n(6)-cyclohexyladenosine N(6)-cyclohexyladenosine: structure given in first source; receptors, purinergic P1 agonist	3.08	1
n(6)-(2,2-diphenylethyl)adenosine N(6)-(2,2-diphenylethyl)adenosine: adenosine receptor agonist; structure given in first source	3.08	1
cgs 24012 CGS 24012: adenosine agonist with both high affinity & selectivity for the adenosine A2 receptor	3.08	1
scopolamine hydrobromide [no description available]	1.99	1

Condition	Indicated	Relationship Strength	Studies	Trials
Amnesia-Memory Loss [description not available]	0	1.98	1	0
Amnesia Pathologic partial or complete loss of the ability to recall past experiences (AMNESIA, RETROGRADE) or to form new memories (AMNESIA, ANTEROGRADE). This condition may be of organic or psychologic origin. Organic forms of amnesia are usually associated with dysfunction of the DIENCEPHALON or HIPPOCAMPUS. (From Adams et al., Principles of Neurology, 6th ed, pp426-7)	0	1.98	1	0

kfm 19

Description

Cross-References

Synonyms (25)

Protein Targets (8)

Inhibition Measurements

Other Measurements

Biological Processes (101)

Molecular Functions (16)

Ceullar Components (19)

Bioassays (34)

Research

Studies (6)

Market Indicators

Research Demand Index: 17.42

Study Types

kfm 19

Description

Cross-References

Synonyms (25)

Protein Targets (8)

Inhibition Measurements

Other Measurements

Biological Processes (101)

Molecular Functions (16)

Ceullar Components (19)

Bioassays (34)

Research

Studies (6)

Market Indicators

Research Demand Index: 17.42

Study Types

Related Drugs (34)

Related Conditions (2)