PMID-sentid	Pub_year	Sent_text	compound_name	comp_offset	prot_official_name	organism	prot_offset
33673282-5	2021	The reduction of the BDNF serum level after co-administration of DPCPX and istradefylline with Mg2+ and Zn2+ was noted.	istradefylline	75-89	brain derived neurotrophic factor	Mus musculus	21-25
33673282-7	2021	Moreover, the changes obtained in Ogg1, MsrA, Nrf2 expression show that DPCPX-Mg2+, DPCPX-Zn2+, istradefylline-Mg2+ and istradefylline-Zn2+ co-treatment may have greater antioxidant capacity benefits than administration of DPCPX and istradefylline alone.	istradefylline	96-110	8-oxoguanine DNA-glycosylase 1	Mus musculus	34-38
33673282-6	2021	Additionally, Mg2+ or Zn2+, both alone and in combination with DPCPX or istradefylline, causes changes in Adora1 expression, DPCPX or istradefylline co-administered with Zn2+ increases Slc6a15 expression as compared to a single-drug treatment, co-administration of tested agents does not have a more favourable effect on Comt expression.	istradefylline	72-86	adenosine A1 receptor	Mus musculus	106-112
33673282-7	2021	Moreover, the changes obtained in Ogg1, MsrA, Nrf2 expression show that DPCPX-Mg2+, DPCPX-Zn2+, istradefylline-Mg2+ and istradefylline-Zn2+ co-treatment may have greater antioxidant capacity benefits than administration of DPCPX and istradefylline alone.	istradefylline	96-110	methionine sulfoxide reductase A	Mus musculus	40-44
33673282-6	2021	Additionally, Mg2+ or Zn2+, both alone and in combination with DPCPX or istradefylline, causes changes in Adora1 expression, DPCPX or istradefylline co-administered with Zn2+ increases Slc6a15 expression as compared to a single-drug treatment, co-administration of tested agents does not have a more favourable effect on Comt expression.	istradefylline	72-86	solute carrier family 6 (neurotransmitter transporter), member 15	Mus musculus	185-192
33673282-7	2021	Moreover, the changes obtained in Ogg1, MsrA, Nrf2 expression show that DPCPX-Mg2+, DPCPX-Zn2+, istradefylline-Mg2+ and istradefylline-Zn2+ co-treatment may have greater antioxidant capacity benefits than administration of DPCPX and istradefylline alone.	istradefylline	96-110	nuclear factor, erythroid derived 2, like 2	Mus musculus	46-50
33673282-7	2021	Moreover, the changes obtained in Ogg1, MsrA, Nrf2 expression show that DPCPX-Mg2+, DPCPX-Zn2+, istradefylline-Mg2+ and istradefylline-Zn2+ co-treatment may have greater antioxidant capacity benefits than administration of DPCPX and istradefylline alone.	istradefylline	120-134	8-oxoguanine DNA-glycosylase 1	Mus musculus	34-38
33673282-7	2021	Moreover, the changes obtained in Ogg1, MsrA, Nrf2 expression show that DPCPX-Mg2+, DPCPX-Zn2+, istradefylline-Mg2+ and istradefylline-Zn2+ co-treatment may have greater antioxidant capacity benefits than administration of DPCPX and istradefylline alone.	istradefylline	120-134	methionine sulfoxide reductase A	Mus musculus	40-44
33673282-7	2021	Moreover, the changes obtained in Ogg1, MsrA, Nrf2 expression show that DPCPX-Mg2+, DPCPX-Zn2+, istradefylline-Mg2+ and istradefylline-Zn2+ co-treatment may have greater antioxidant capacity benefits than administration of DPCPX and istradefylline alone.	istradefylline	120-134	nuclear factor, erythroid derived 2, like 2	Mus musculus	46-50
33673282-6	2021	Additionally, Mg2+ or Zn2+, both alone and in combination with DPCPX or istradefylline, causes changes in Adora1 expression, DPCPX or istradefylline co-administered with Zn2+ increases Slc6a15 expression as compared to a single-drug treatment, co-administration of tested agents does not have a more favourable effect on Comt expression.	istradefylline	72-86	catechol-O-methyltransferase	Mus musculus	321-325
33673282-7	2021	Moreover, the changes obtained in Ogg1, MsrA, Nrf2 expression show that DPCPX-Mg2+, DPCPX-Zn2+, istradefylline-Mg2+ and istradefylline-Zn2+ co-treatment may have greater antioxidant capacity benefits than administration of DPCPX and istradefylline alone.	istradefylline	120-134	8-oxoguanine DNA-glycosylase 1	Mus musculus	34-38
33673282-7	2021	Moreover, the changes obtained in Ogg1, MsrA, Nrf2 expression show that DPCPX-Mg2+, DPCPX-Zn2+, istradefylline-Mg2+ and istradefylline-Zn2+ co-treatment may have greater antioxidant capacity benefits than administration of DPCPX and istradefylline alone.	istradefylline	120-134	methionine sulfoxide reductase A	Mus musculus	40-44
33673282-7	2021	Moreover, the changes obtained in Ogg1, MsrA, Nrf2 expression show that DPCPX-Mg2+, DPCPX-Zn2+, istradefylline-Mg2+ and istradefylline-Zn2+ co-treatment may have greater antioxidant capacity benefits than administration of DPCPX and istradefylline alone.	istradefylline	120-134	nuclear factor, erythroid derived 2, like 2	Mus musculus	46-50
33673282-6	2021	Additionally, Mg2+ or Zn2+, both alone and in combination with DPCPX or istradefylline, causes changes in Adora1 expression, DPCPX or istradefylline co-administered with Zn2+ increases Slc6a15 expression as compared to a single-drug treatment, co-administration of tested agents does not have a more favourable effect on Comt expression.	istradefylline	134-148	solute carrier family 6 (neurotransmitter transporter), member 15	Mus musculus	185-192
33547274-6	2021	To verify if chronic A2AR blockade could reverse the FXS phenotypes, we treated the Fmr1 KO mice with istradefylline, an A2AR antagonist.	istradefylline	102-116	fragile X messenger ribonucleoprotein 1	Mus musculus	84-88
33547274-6	2021	To verify if chronic A2AR blockade could reverse the FXS phenotypes, we treated the Fmr1 KO mice with istradefylline, an A2AR antagonist.	istradefylline	102-116	adenosine A2a receptor	Mus musculus	121-125
33547274-8	2021	Furthermore, istradefylline corrected aberrant dendritic spine density, specific behavioral alterations, and overactive mTOR, TrkB, and STEP signaling in Fmr1 KO mice.	istradefylline	13-27	mechanistic target of rapamycin kinase	Mus musculus	120-124
33547274-8	2021	Furthermore, istradefylline corrected aberrant dendritic spine density, specific behavioral alterations, and overactive mTOR, TrkB, and STEP signaling in Fmr1 KO mice.	istradefylline	13-27	neurotrophic tyrosine kinase, receptor, type 2	Mus musculus	126-130
33547274-8	2021	Furthermore, istradefylline corrected aberrant dendritic spine density, specific behavioral alterations, and overactive mTOR, TrkB, and STEP signaling in Fmr1 KO mice.	istradefylline	13-27	protein tyrosine phosphatase, non-receptor type 5	Mus musculus	136-140
33547274-8	2021	Furthermore, istradefylline corrected aberrant dendritic spine density, specific behavioral alterations, and overactive mTOR, TrkB, and STEP signaling in Fmr1 KO mice.	istradefylline	13-27	fragile X messenger ribonucleoprotein 1	Mus musculus	154-158
33390888-8	2020	Importantly, since the first clinical trial in 2003, United States FDA has finally approved clinical use of the A2AR antagonist istradefylline for the treatment of PD with OFF-time in Sept. 2019.	istradefylline	128-142	adenosine A2a receptor	Mus musculus	112-116
33200448-0	2021	Adenosine A2A Receptor Occupancy by Long-Term Istradefylline Administration in Parkinson"s Disease.	istradefylline	46-60	adenosine A2a receptor	Homo sapiens	0-22
32452837-5	2020	In in vitro human and in vivo mouse studies, Tfh generation and germinal center responses were enhanced by reducing CD39 expression through the inhibition of the cAMP/PKA/p-CREB pathway, or by blocking adenosine signaling downstream of CD39 using the selective adenosine A2a receptor antagonist istradefylline.	istradefylline	295-309	ectonucleoside triphosphate diphosphohydrolase 1	Mus musculus	116-120
33302331-5	2020	Istradefylline, a novel adenosine A2A receptor antagonist, is indicated as a treatment addition to levodopa/carbidopa in patients experiencing "off episodes".	istradefylline	0-14	adenosine A2a receptor	Homo sapiens	24-46
32311420-6	2020	Chronic treatment with the A2AR antagonist KW-6002, rescued LTP and A2AR values.	istradefylline	43-50	adenosine A2a receptor	Mus musculus	27-31
32311420-6	2020	Chronic treatment with the A2AR antagonist KW-6002, rescued LTP and A2AR values.	istradefylline	43-50	adenosine A2a receptor	Mus musculus	68-72
31900336-8	2020	Pimonidazole and CCL-2 positive staining diminished when B16-F1 cell-inoculated animals were treated with trolox, nifedipine, or the adenosine receptor 2A antagonist KW6002.	istradefylline	166-172	chemokine (C-C motif) ligand 2	Mus musculus	17-22
32061899-7	2020	(iii) A2AR antagonist KW6002 promotes instrumental actions by invigorating motivation.	istradefylline	22-28	adenosine A2a receptor	Homo sapiens	6-10
32357548-15	2020	A2AR antagonists such as istradefylline, which is already approved for Parkinson"s disease (Nouriast  in Japan and Nourianz  in the US), have potential to afford neuroprotection in AD in a synergistic-like fashion.	istradefylline	25-39	adenosine A2a receptor	Mus musculus	0-4
32236790-0	2020	The belated US FDA approval of the adenosine A2A receptor antagonist istradefylline for treatment of Parkinson"s disease.	istradefylline	69-83	adenosine A2a receptor	Homo sapiens	35-57
32236790-1	2020	After more than two decades of preclinical and clinical studies, on August 27, 2019, the US Food and Drug Administration (FDA) approved the adenosine A2A receptor antagonist Nourianz  (istradefylline) developed by Kyowa Hakko Kirin Inc., Japan, as an add-on treatment to levodopa in Parkinson"s disease (PD) with "OFF" episodes.	istradefylline	185-199	adenosine A2a receptor	Homo sapiens	140-162
30253174-1	2018	Istradefylline, an adenosine A2A receptor (A2AR) antagonist, is effective as an adjunct to levodopa and can alleviate "off" time and motor symptoms in patients with Parkinson"s disease (PD).	istradefylline	0-14	adenosine A2a receptor	Homo sapiens	19-41
30392131-3	2019	METHODS: Sprague-Dawley rats were used to assess the differential effects of SCH 442416 and istradefylline that antagonize presynaptic and postsynaptic A2AR, respectively.	istradefylline	92-106	adenosine A2a receptor	Rattus norvegicus	152-156
32163528-0	2020	Istradefylline: adenosine A2A receptor antagonist to reduce "OFF" time in Parkinson"s disease.	istradefylline	0-14	adenosine A2a receptor	Homo sapiens	16-38
32163528-4	2020	Istradefylline is an adenosine A2A receptor antagonist that significantly reduces the "OFF" time and improves the motor function of patients with PD, as measured by the Unified Parkinson"s Disease Rating Scale (UPDRS) Part III, while increasing the time without troublesome dyskinesia.	istradefylline	0-14	adenosine A2a receptor	Homo sapiens	21-43
31629857-8	2020	The A2A receptor antagonist istradefylline given after CtB-Saporin: 1) reduced phrenic motor neuron death (~20% survival) and 2) preserved diaphragm EMG activity (~46%).	istradefylline	28-42	phosphate cytidylyltransferase 1B, choline	Rattus norvegicus	55-58
31408967-6	2019	The administration of istradefylline (a clinically approved A2AR antagonist) reduced deafferentation of inner hair cells and improved the survival of afferent synapses after excitotoxic injury.	istradefylline	22-36	adenosine A2a receptor	Rattus norvegicus	60-64
31039621-3	2019	Istradefylline is a first-in-class selective adenosine A2A receptor antagonist with benefits for motor complications associated with Parkinson"s disease.	istradefylline	0-14	adenosine A2a receptor	Homo sapiens	45-67
31469906-1	2019	INTRODUCTION: In the current edition, Fujioka and colleagues report on four Japanese patients with Parkinson disease (PD) and severe postural abnormalities treated with istradefylline (adenosine A2A receptor antagonist); further, dopamine agonists were with- drawn.	istradefylline	169-183	adenosine A2a receptor	Homo sapiens	185-207
30253174-1	2018	Istradefylline, an adenosine A2A receptor (A2AR) antagonist, is effective as an adjunct to levodopa and can alleviate "off" time and motor symptoms in patients with Parkinson"s disease (PD).	istradefylline	0-14	adenosine A2a receptor	Homo sapiens	43-47
30281377-1	2018	BACKGROUND: Istradefylline is a first-in-class, non-dopaminergic, selective adenosine A2A receptor antagonist for the treatment of Parkinson"s disease (PD) in patients experiencing the wearing-off phenomenon with levodopa (L-DOPA).	istradefylline	12-26	adenosine A2a receptor	Homo sapiens	76-98
30134834-8	2018	RESULTS: The A2AR antagonist KW6002 (P7-P17) did not affect normal postnatal development of retinal vasculature, but selectively reduced avascular areas and neovascularization, with the reduced cellular apoptosis and proliferation, and enhanced astrocyte and tip cell functions in OIR.	istradefylline	29-35	adenosine A2a receptor	Mus musculus	13-17
30134834-8	2018	RESULTS: The A2AR antagonist KW6002 (P7-P17) did not affect normal postnatal development of retinal vasculature, but selectively reduced avascular areas and neovascularization, with the reduced cellular apoptosis and proliferation, and enhanced astrocyte and tip cell functions in OIR.	istradefylline	29-35	family with sequence similarity 72, member A	Mus musculus	40-43
27424102-1	2016	Istradefylline (KW-6002), an adenosine A2A receptor antagonist, is used adjunct with optimal doses of L-3,4-dihydroxyphenylalanine (l-DOPA) to extend on-time in Parkinson"s disease (PD) patients experiencing motor fluctuations.	istradefylline	0-14	adenosine A2a receptor	Homo sapiens	29-51
29672326-2	2018	Istradefylline is adenosine A2A receptor antagonist approved for PD patients with wearing-off symptoms.	istradefylline	0-14	adenosine A2a receptor	Homo sapiens	18-40
29406892-2	2018	METHODS: We analyzed the effects of istradefylline, a selective adenosine A2A receptor antagonist, on posture in 21 levodopa-treated PD patients from the subanalysis of a three-month open-label study.	istradefylline	36-50	adenosine A2a receptor	Homo sapiens	64-86
28667836-3	2017	Wnt-signaling reporter mice (Tcf/Lef:H2B-GFP) were challenged with bleomycin and treated with the selective A2aR antagonist istradefylline (KW6002) or vehicle.	istradefylline	124-138	adenosine A2a receptor	Mus musculus	108-112
28667836-7	2017	Moreover, KW6002 significantly inhibited nuclear translocation of Tcf/Lef:H2B-GFP reporter, as well as dephosphorylated beta-catenin and beta-catenin phosphorylated at Ser552.	istradefylline	10-16	catenin (cadherin associated protein), beta 1	Mus musculus	120-132
28667836-7	2017	Moreover, KW6002 significantly inhibited nuclear translocation of Tcf/Lef:H2B-GFP reporter, as well as dephosphorylated beta-catenin and beta-catenin phosphorylated at Ser552.	istradefylline	10-16	catenin (cadherin associated protein), beta 1	Mus musculus	137-149
27835671-2	2016	Here we identified that an anti-Parkinson"s disease drug, Istradefylline, could enhance Abeta generation in various cell lines and primary neuronal cells of APP/PS1 mouse.	istradefylline	58-72	amyloid beta (A4) precursor protein	Mus musculus	157-164
27835671-3	2016	Moreover, the increased generation of Abeta42 was detected in the cortex of APP/PS1 mouse after chronic treatment with Istradefylline.	istradefylline	119-133	amyloid beta (A4) precursor protein	Mus musculus	76-83
27835671-5	2016	These effects of Istradefylline were reduced by the knockdown of A2AR but independent of A2AR-mediated G protein- or beta-arrestin-dependent signal pathway.	istradefylline	17-31	adenosine A2a receptor	Mus musculus	65-69
29100987-2	2018	The adenosine A2A receptor antagonist istradefylline is approved in Japan for Parkinson"s disease and is being tested in clinical trials for this condition elsewhere.	istradefylline	38-52	adenosine A2a receptor	Mus musculus	4-26
28870576-1	2017	BACKGROUND: Istradefylline, a selective adenosine A2A receptor antagonist, has been reported to improve daily "off time" and motor symptoms in patients with Parkinson"s disease (PD).	istradefylline	12-26	adenosine A2a receptor	Homo sapiens	40-62
28583861-7	2017	In contrast, the locomotor response to the ADORA2A antagonist istradefylline was significantly augmented in GPR52 KO mice compared to WT mice.	istradefylline	62-76	adenosine A2a receptor	Mus musculus	43-50
28583861-7	2017	In contrast, the locomotor response to the ADORA2A antagonist istradefylline was significantly augmented in GPR52 KO mice compared to WT mice.	istradefylline	62-76	G protein-coupled receptor 52	Mus musculus	108-113
28500295-5	2017	Interestingly, by protein-protein docking and molecular dynamics simulations, we described that a stable heterotetrameric interaction may exist between AT1R and A2AR bound to antagonists (i.e. losartan and istradefylline, respectively).	istradefylline	206-220	angiotensin II, type I receptor-associated protein	Mus musculus	152-156
28500295-5	2017	Interestingly, by protein-protein docking and molecular dynamics simulations, we described that a stable heterotetrameric interaction may exist between AT1R and A2AR bound to antagonists (i.e. losartan and istradefylline, respectively).	istradefylline	206-220	adenosine A2a receptor	Mus musculus	161-165
27424102-1	2016	Istradefylline (KW-6002), an adenosine A2A receptor antagonist, is used adjunct with optimal doses of L-3,4-dihydroxyphenylalanine (l-DOPA) to extend on-time in Parkinson"s disease (PD) patients experiencing motor fluctuations.	istradefylline	16-23	adenosine A2a receptor	Homo sapiens	29-51
26211977-5	2016	Very relevant is the recent approval in Japan of the adenosine A2A receptor antagonist, istradefylline, for use in Parkinson"s disease patients.	istradefylline	88-102	adenosine A2a receptor	Homo sapiens	53-75
27835671-10	2016	Istradefylline enhance Abeta generation and gamma-secretase activity possibly via modulating the interaction between A2AR and gamma-secretase, which may bring some undesired effects in the central nervous system (CNS).	istradefylline	0-14	adenosine A2a receptor	Mus musculus	117-121
26415982-0	2015	The adenosine A2A receptor antagonist, istradefylline enhances anti-parkinsonian activity induced by combined treatment with low doses of L-DOPA and dopamine agonists in MPTP-treated common marmosets.	istradefylline	39-53	LOW QUALITY PROTEIN: adenosine receptor A2a	Callithrix jacchus	4-26
26415982-1	2015	The adenosine A2A receptor antagonist, istradefylline improves motor function in patients with advanced Parkinson"s disease (PD) optimally treated with a combination of L-DOPA and a dopamine agonist without increasing the risk of troublesome dyskinesia.	istradefylline	39-53	adenosine A2a receptor	Homo sapiens	4-26
25499739-0	2015	The adenosine A2A receptor antagonist, istradefylline enhances the anti-parkinsonian activity of low doses of dopamine agonists in MPTP-treated common marmosets.	istradefylline	39-53	LOW QUALITY PROTEIN: adenosine receptor A2a	Callithrix jacchus	4-26
26056314-5	2015	Except for anxiety, for which results were mixed, CUS-induced behavioral and synaptic alterations were prevented by (i) caffeine (1 g/L in the drinking water, starting 3 wk before and continued throughout CUS); (ii) the selective A2AR antagonist KW6002 (3 mg/kg, p.o.	istradefylline	246-252	adenosine A2a receptor	Mus musculus	230-234
25768849-1	2015	OBJECTIVES: Istradefylline is a selective adenosine A2A receptor antagonist.	istradefylline	12-26	adenosine A2a receptor	Homo sapiens	42-64
25499739-1	2015	The adenosine A2A receptor antagonist, istradefylline, enhances anti-parkinsonian activity in patients with advanced Parkinson s disease (PD) already treated with combinations of L-DOPA and dopamine agonist drugs but who are still exhibiting prolonged "OFF" periods.	istradefylline	39-53	adenosine A2a receptor	Homo sapiens	4-26
25096504-0	2015	Efficacy of adenosine A2A receptor antagonist istradefylline as augmentation for Parkinson"s disease: a meta-analysis of randomized controlled trials.	istradefylline	46-60	adenosine A2a receptor	Homo sapiens	12-34
25096504-1	2015	Adenosine A2A receptor antagonist istradefylline has been approved this year for manufacturing and marketing in Japan.	istradefylline	34-48	adenosine A2a receptor	Homo sapiens	0-22
24725292-0	2014	Adenosine A2A receptor antagonist istradefylline 20 versus 40 mg/day as augmentation for Parkinson"s disease: a meta-analysis.	istradefylline	34-48	adenosine A2a receptor	Homo sapiens	0-22
24725292-1	2014	BACKGROUND: Adenosine A2A receptor antagonist istradefylline 20 mg/day has been approved this year for manufacturing and market in Japan.	istradefylline	46-60	adenosine A2a receptor	Homo sapiens	12-34
23812646-7	2013	In addition, istradefylline hardly inhibited monoamine oxidase-A, monoamine oxidase-B, or catechol-O-methyl transferase.	istradefylline	13-27	monoamine oxidase A	Homo sapiens	45-64
24747180-5	2014	Therefore in this work we aimed to evaluate the impact of a chronic in vivo oral administration of an A2AR antagonist (KW-6002) in the BDNF actions upon hippocampal CA1 LTP.	istradefylline	119-126	adenosine A2a receptor	Rattus norvegicus	102-106
24747180-5	2014	Therefore in this work we aimed to evaluate the impact of a chronic in vivo oral administration of an A2AR antagonist (KW-6002) in the BDNF actions upon hippocampal CA1 LTP.	istradefylline	119-126	brain-derived neurotrophic factor	Rattus norvegicus	135-139
24747180-5	2014	Therefore in this work we aimed to evaluate the impact of a chronic in vivo oral administration of an A2AR antagonist (KW-6002) in the BDNF actions upon hippocampal CA1 LTP.	istradefylline	119-126	carbonic anhydrase 1	Rattus norvegicus	165-168
24488405-0	2014	Antidepressant activity of the adenosine A2A receptor antagonist, istradefylline (KW-6002) on learned helplessness in rats.	istradefylline	66-80	adenosine A2a receptor	Rattus norvegicus	31-53
24488405-0	2014	Antidepressant activity of the adenosine A2A receptor antagonist, istradefylline (KW-6002) on learned helplessness in rats.	istradefylline	82-89	adenosine A2a receptor	Rattus norvegicus	31-53
24488405-1	2014	RATIONALE: Istradefylline, an adenosine A2A receptor antagonist, improves motor function in animal models of Parkinson"s disease (PD) and in patients with PD.	istradefylline	11-25	adenosine A2a receptor	Homo sapiens	30-52
24681641-0	2014	Adenosine A2A-receptor antagonist istradefylline enhances the motor response of L-DOPA without worsening dyskinesia in MPTP-treated common marmosets.	istradefylline	34-48	LOW QUALITY PROTEIN: adenosine receptor A2a	Callithrix jacchus	0-22
24681641-1	2014	The adenosine A2A-receptor antagonist istradefylline decreases OFF time in patients with Parkinson"s disease who are already treated with optimal doses of dopaminergic medication but can cause an increase in non-troublesome dyskinesia.	istradefylline	38-52	adenosine A2a receptor	Homo sapiens	4-26
23812646-2	2013	Istradefylline is an adenosine A2A receptor antagonist that has been reported to exhibit antiparkinsonian activities in PD patients as well as both rodents and nonhuman primate models of PD.	istradefylline	0-14	adenosine A2a receptor	Homo sapiens	21-43
23812646-7	2013	In addition, istradefylline hardly inhibited monoamine oxidase-A, monoamine oxidase-B, or catechol-O-methyl transferase.	istradefylline	13-27	monoamine oxidase B	Homo sapiens	66-85
23085003-0	2013	Istradefylline, an adenosine A2A receptor antagonist, for patients with Parkinson"s Disease: a meta-analysis.	istradefylline	0-14	adenosine A2a receptor	Homo sapiens	19-41
23483627-0	2013	Adenosine A2A receptor antagonist istradefylline reduces daily OFF time in Parkinson"s disease.	istradefylline	34-48	adenosine A2a receptor	Homo sapiens	0-22
23483627-1	2013	BACKGROUND: We evaluated the efficacy and safety of istradefylline, a selective adenosine A2A receptor antagonist administered as adjunctive treatment to levodopa for 12 weeks in a double-blind manner in Parkinson"s disease patients with motor complications in Japan.	istradefylline	52-66	adenosine A2a receptor	Homo sapiens	80-102
23700273-1	2013	Kyowa Hakko Kirin is developing istradefylline, a selective adenosine A2A receptor antagonist, for the once-daily oral treatment of Parkinson"s disease (PD).	istradefylline	32-46	adenosine A2a receptor	Homo sapiens	60-82
22162533-1	2012	This model-based analysis quantifies the population pharmacokinetic-pharmacodynamic efficacy and safety/tolerability relationships of orally administered istradefylline, a selective adenosine A(2A) receptor antagonist, in healthy participants and patients with Parkinson disease.	istradefylline	154-168	adenosine A2a receptor	Homo sapiens	182-206
20182024-6	2010	The available data also suggest that caffeine can improve the motor deficits of PD and that adenosine A2A receptor antagonists such as istradefylline reduces OFF time and dyskinesia associated with standard "dopamine replacement" treatments.	istradefylline	135-149	adenosine A2a receptor	Homo sapiens	92-114
22000279-1	2012	BACKGROUND: Istradefylline (KW-6002) is a selective adenosine A(2A) receptor antagonist investigated as adjunctive therapy to levodopa in PD patients with motor response complications.	istradefylline	12-26	adenosine A2a receptor	Homo sapiens	52-76
22000279-1	2012	BACKGROUND: Istradefylline (KW-6002) is a selective adenosine A(2A) receptor antagonist investigated as adjunctive therapy to levodopa in PD patients with motor response complications.	istradefylline	28-35	adenosine A2a receptor	Homo sapiens	52-76
20200269-4	2011	Smoking and CYP3A4 inhibitors as concomitant medications were important predictors of istradefylline exposure.	istradefylline	86-100	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	12-18
20200269-5	2011	Istradefylline area under the concentration-time curve at steady-state increased 35% (95% confidence interval, 18%-55%) in the presence of CYP3A4 inhibitors and decreased 38% (95% confidence interval, 26%-50%) in smokers.	istradefylline	0-14	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	139-145
18831530-2	2008	Istradefylline (KW-6002) is an adenosine A(2A) receptor antagonist that in primate models of PD improves motor function without causing or worsening dyskinesia.	istradefylline	0-14	adenosine A2a receptor	Homo sapiens	31-55
18831530-2	2008	Istradefylline (KW-6002) is an adenosine A(2A) receptor antagonist that in primate models of PD improves motor function without causing or worsening dyskinesia.	istradefylline	16-23	adenosine A2a receptor	Homo sapiens	31-55
17310264-10	2007	KW-6002 and Biogen-34 exhibited the highest selectivity for A2A vs A1 (human and rat), respectively.	istradefylline	0-7	spectrin, alpha, non-erythrocytic 1	Rattus norvegicus	60-63
18306243-0	2008	Adenosine A2A receptor antagonist istradefylline (KW-6002) reduces "off" time in Parkinson"s disease: a double-blind, randomized, multicenter clinical trial (6002-US-005).	istradefylline	34-48	adenosine A2a receptor	Homo sapiens	0-22
18306243-0	2008	Adenosine A2A receptor antagonist istradefylline (KW-6002) reduces "off" time in Parkinson"s disease: a double-blind, randomized, multicenter clinical trial (6002-US-005).	istradefylline	50-57	adenosine A2a receptor	Homo sapiens	0-22
17467309-0	2007	The effect of striatal dopamine depletion and the adenosine A2A antagonist KW-6002 on reversal learning in rats.	istradefylline	75-82	spectrin, alpha, non-erythrocytic 1	Rattus norvegicus	60-63
18519872-1	2008	BACKGROUND: The safety and efficacy of istradefylline, a selective adenosine A(2A) receptor antagonist, was evaluated in a 12-week, double-blind study in levodopa-treated Parkinson disease (PD) subjects with motor complications.	istradefylline	39-53	adenosine A2a receptor	Homo sapiens	67-91
24692766-1	2007	BACKGROUND: Studies of istradefylline (KW6002), an adenosine A2A-receptor antagonist, have provided evidence of its efficacy as a nondopaminergic antiparkinsonian drug.	istradefylline	23-37	adenosine A2a receptor	Homo sapiens	51-73
24692766-1	2007	BACKGROUND: Studies of istradefylline (KW6002), an adenosine A2A-receptor antagonist, have provided evidence of its efficacy as a nondopaminergic antiparkinsonian drug.	istradefylline	39-45	adenosine A2a receptor	Homo sapiens	51-73
24692766-3	2007	OBJECTIVES: The aims of this study were to assess the effectiveness and tolerability of istradefylline in the treatment of RLS.	istradefylline	88-102	RLS1	Homo sapiens	123-126
24692766-4	2007	METHODS: This was a single-center, multiparametric, prospective trial of istradefylline as a treatment for moderate to severe idiopathic RLS.	istradefylline	73-87	RLS1	Homo sapiens	137-140
24692766-16	2007	Improvement in RLS symptoms was observed in 3 patients treated with istradefylline for 6 weeks.	istradefylline	68-82	RLS1	Homo sapiens	15-18
17310264-16	2007	Among the six A2A-antagonists, KW-6002 is the best for use in in vivo animal studies, particularly for a CNS target, based on its bioavailability, half life, and brain penetration.	istradefylline	31-38	spectrin, alpha, non-erythrocytic 1	Rattus norvegicus	14-17
12913187-0	2003	Randomized trial of the adenosine A(2A) receptor antagonist istradefylline in advanced PD.	istradefylline	60-74	adenosine A2a receptor	Homo sapiens	24-48
15974638-6	2005	Istradefylline (KW-6002) is the first of several adenosine A2A receptor antagonists in development for PD to advance to phase III clinical trials.	istradefylline	0-14	adenosine A2a receptor	Homo sapiens	49-71
15974638-6	2005	Istradefylline (KW-6002) is the first of several adenosine A2A receptor antagonists in development for PD to advance to phase III clinical trials.	istradefylline	16-23	adenosine A2a receptor	Homo sapiens	49-71
15822104-5	2005	Istradefylline (KW-6002), an adenosine A(2A) receptor antagonist, has been studied for wearing-off and the results will be discussed.	istradefylline	0-14	adenosine A2a receptor	Homo sapiens	29-53
15822104-5	2005	Istradefylline (KW-6002), an adenosine A(2A) receptor antagonist, has been studied for wearing-off and the results will be discussed.	istradefylline	16-23	adenosine A2a receptor	Homo sapiens	29-53
14663007-5	2003	Importantly, the selective A2A antagonist KW6002 reverses motor disability and increases locomotor activity in MPTP-treated primates without provoking dyskinesia established by previous exposure to L-dopa.	istradefylline	42-48	spectrin, alpha, non-erythrocytic 1	Rattus norvegicus	27-30
14663007-7	2003	The data available suggest that A2A antagonists, such as KW6002, may be effective as monotherapy for the management of PD and that they will also produce additional benefit when administered in combination with L-dopa or dopamine agonist therapy.	istradefylline	57-63	spectrin, alpha, non-erythrocytic 1	Rattus norvegicus	32-35
16004599-0	2005	Istradefylline, a novel adenosine A2A receptor antagonist, for the treatment of Parkinson"s disease.	istradefylline	0-14	adenosine A2a receptor	Homo sapiens	24-46
16004599-5	2005	Istradefylline is a novel adenosine A(2A) receptor antagonist currently in Phase III clinical trials for efficacy in patients with PD; results from Phase II clinical trials demonstrated that it provides a clinically meaningful reduction in "off" time and an increased "on" time with non-troublesome dyskinesia in levodopa-treated patients with established motor complications, and is safe and well tolerated.	istradefylline	0-14	adenosine A2a receptor	Homo sapiens	26-50
14663013-2	2003	Adenosine A2A receptor antagonists (e.g., KW-6002) may provide symptomatic relief in PD and perhaps also may display neuroprotective properties based on studies in the 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) mouse model of nigrostriatal neurodegeneration.	istradefylline	42-49	adenosine A2a receptor	Mus musculus	0-22
14663020-0	2003	Progress in pursuit of therapeutic A2A antagonists: the adenosine A2A receptor selective antagonist KW6002: research and development toward a novel nondopaminergic therapy for Parkinson"s disease.	istradefylline	100-106	immunoglobulin kappa variable 2D-29	Homo sapiens	35-38
14663020-0	2003	Progress in pursuit of therapeutic A2A antagonists: the adenosine A2A receptor selective antagonist KW6002: research and development toward a novel nondopaminergic therapy for Parkinson"s disease.	istradefylline	100-106	adenosine A2a receptor	Homo sapiens	56-78
14663020-1	2003	Research and development of the adenosine A2A receptor selective antagonist KW6002 have focused on developing a novel nondopaminergic therapy for Parkinson"s disease (PD).	istradefylline	76-82	adenosine A2a receptor	Homo sapiens	32-54
14637099-3	2003	In rats, KW-6002 reversed the shortened motor response produced by chronic levodopa treatment while reducing levodopa-induced hyperphosphorylation at S845 residues on AMPA receptor GluR1 subunits.	istradefylline	9-16	glutamate ionotropic receptor AMPA type subunit 1	Rattus norvegicus	181-186
12913187-1	2003	OBJECTIVE: To evaluate the safety and efficacy of the adenosine A(2A) receptor antagonist istradefylline (KW-6002) in patients with levodopa-treated Parkinson"s disease (PD) with both motor fluctuations and peak-dose dyskinesias.	istradefylline	90-104	adenosine A2a receptor	Homo sapiens	54-78
12913187-1	2003	OBJECTIVE: To evaluate the safety and efficacy of the adenosine A(2A) receptor antagonist istradefylline (KW-6002) in patients with levodopa-treated Parkinson"s disease (PD) with both motor fluctuations and peak-dose dyskinesias.	istradefylline	106-113	adenosine A2a receptor	Homo sapiens	54-78
12614340-0	2003	Cellular and behavioural effects of the adenosine A2a receptor antagonist KW-6002 in a rat model of l-DOPA-induced dyskinesia.	istradefylline	74-81	adenosine A2a receptor	Rattus norvegicus	40-62
12628657-6	2003	The results of these studies suggest that MAO-B inhibition may contribute to the neuroprotective potential of A(2A) receptor antagonists such as KW-6002 and open the possibility of designing dual targeting drugs that may have enhanced therapeutic potential in the treatment of PD.	istradefylline	145-152	monoamine oxidase B	Mus musculus	42-47
12384245-9	2002	These results are the first to show directly that orally administered KW-6002 is distributed selectively to the striatum and that it modulates the activity of striatopallidal enkephalin-containing neurons but not striatonigral substance P-containing neurons.	istradefylline	70-77	proenkephalin	Rattus norvegicus	175-185
11569945-1	2001	Kyowa Hakko is developing KW-6002, an adenosine A2A receptor antagonist, for the potential treatment of Parkinson"s disease (PD) [183211].	istradefylline	26-33	adenosine A2a receptor	Homo sapiens	38-60
11808320-4	2002	Several lines of evidence indicated that KW-6002, highly selective antagonist of adenosine A2A receptor, showed anti-parkinsonian effect in vivo and in vitro without any problematic side effect which is observed in dopaminergic therapy.	istradefylline	41-48	adenosine A2a receptor	Homo sapiens	81-103
10591873-0	1999	Actions of adenosine A2A receptor antagonist KW-6002 on drug-induced catalepsy and hypokinesia caused by reserpine or MPTP.	istradefylline	45-52	adenosine A2a receptor	Mus musculus	11-33
11090641-0	2000	Adenosine A(2A) receptor antagonists KF17837 and KW-6002 potentiate rotation induced by dopaminergic drugs in hemi-Parkinsonian rats.	istradefylline	49-56	adenosine A2a receptor	Rattus norvegicus	0-24
10591873-3	1999	OBJECTIVES: The purpose of this study is to examine the efficacy and potency of the novel selective adenosine A2A receptor antagonist (E)-1,3-diethyl-8-(3,4-dimethoxystyryl)-7-methyl-3,7-dhydro- 1H-purine-2,6- dione (KW-6002) in ameliorating the motor deficits in various mouse models of Parkinson"s disease.	istradefylline	217-224	adenosine A2a receptor	Mus musculus	100-122
10591873-4	1999	METHODS: We evaluated the efficacy and potency of KW-6002 and other reference compounds in the selective adenosine A2A receptor agonist 2-[p-(2-carboxyethyl)phenethylamino]-5"-N-ethylcarboxamidoadenosin e (CGS 21680)-, haloperidol- or reserpine-induced catalepsy models.	istradefylline	50-57	adenosine A2a receptor	Mus musculus	105-127
10591873-9	1999	Combined administrations of subthreshold doses of KW-6002 and L-dopa (50 mg/kg, PO) exerted prominent effects on haloperidol-induced and reserpine-induced catalepsy, suggesting that there may be a synergism between the adenosine A2A receptor antagonist KW-6002 and dopaminergic agents.	istradefylline	50-57	adenosine A2a receptor	Mus musculus	219-241
10591873-10	1999	CONCLUSIONS: To our knowledge, KW-6002 is the most potent and orally active adenosine A2A receptor antagonist in experimental models of Parkinson"s disease, and may offer a new therapeutic approach to the treatment of Parkinson"s disease.	istradefylline	31-38	adenosine A2a receptor	Mus musculus	76-98
10331698-5	1999	OBJECTIVE: To evaluate the antiparkinsonian effect of a new selective adenosine A2A receptor antagonist, KW-6002, in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-treated monkeys.	istradefylline	105-112	adenosine A2a receptor	Homo sapiens	70-92
9546333-3	1998	The novel adenosine A2A receptor antagonist KW-6002 has been examined for antiparkinsonian activity in MPTP-treated primates.	istradefylline	44-51	LOW QUALITY PROTEIN: adenosine receptor A2a	Callithrix jacchus	10-32
24687255-0	2014	Adenosine A2A receptor antagonists in Parkinson"s disease: progress in clinical trials from the newly approved istradefylline to drugs in early development and those already discontinued.	istradefylline	111-125	adenosine A2a receptor	Homo sapiens	0-22
24687255-5	2014	To date, the clinical research regarding A2A antagonists and their potential utilization in PD therapy continues to evolve between drugs just or previously discontinued (preladenant and vipadenant), new derivatives in development (tozadenant, PBF-509, ST1535, ST4206 and V81444) and the relatively old drug istradefylline, which has finally been licensed as an anti-parkinsonian drug in Japan.	istradefylline	307-321	immunoglobulin kappa variable 2D-29	Homo sapiens	41-44
34927011-3	2021	Here, we identify xanthines including caffeine and istradefylline as TLX modulators that counteract the receptor"s intrinsic repressor activity.	istradefylline	51-65	CD46 molecule	Homo sapiens	69-72
34514988-1	2021	The approval of istradefylline, an adenosine 2A receptor (A2AR) antagonist, as an add-on treatment in adult patients with Parkinson"s disease by the Food and Drug Administration (FDA) and European Medicines Agency (EMA), is the latest proof of the importance of the adenosinergic system in the nervous system.	istradefylline	16-30	adenosine A2a receptor	Homo sapiens	35-56
34514988-1	2021	The approval of istradefylline, an adenosine 2A receptor (A2AR) antagonist, as an add-on treatment in adult patients with Parkinson"s disease by the Food and Drug Administration (FDA) and European Medicines Agency (EMA), is the latest proof of the importance of the adenosinergic system in the nervous system.	istradefylline	16-30	adenosine A2a receptor	Homo sapiens	58-62
34115897-5	2021	The effect of istradefylline, a selective adenosine A2A receptor antagonist at two doses (10 and 20 mg kg-1  day-1 ) on the expression of stereotypy and T-CAT performance in high (H) and non-(N) stereotypical animals, was investigated in comparison to a control intervention (six groups; n = 8 or 9 per group).	istradefylline	14-28	adenosine A2a receptor	Mus musculus	42-64
34339491-5	2022	3) Adenosine A2A receptor (A2AR) antagonist KW6002 selectively improved sequence learning by preferentially improving sequence initiation and shift of sequence learning as well as behavioral reactivity.	istradefylline	44-50	adenosine A2a receptor	Homo sapiens	3-25
34583302-2	2021	This subanalysis of the J-FIRST study evaluated the effect of istradefylline, a selective adenosine A2A receptor antagonist, on NMSs in istradefylline-naive Japanese patients with PD.	istradefylline	62-76	adenosine A2a receptor	Homo sapiens	90-112
34399565-4	2021	Clinical trials have found that the A2AR antagonist istradefylline decreases dyskinesia in PD and could be used as an adjuvant to levodopa treatment.	istradefylline	52-66	adenosine A2a receptor	Homo sapiens	36-40
34339491-5	2022	3) Adenosine A2A receptor (A2AR) antagonist KW6002 selectively improved sequence learning by preferentially improving sequence initiation and shift of sequence learning as well as behavioral reactivity.	istradefylline	44-50	adenosine A2a receptor	Homo sapiens	27-31
34227764-1	2021	Istradefylline is a novel selective adenosine A2A receptor antagonist that is used to treat Parkinson"s disease and improve motor dysfunction in the early stage of this disease.	istradefylline	0-14	adenosine A2a receptor	Homo sapiens	36-58
34360766-0	2021	Istradefylline Mitigates Age-Related Hearing Loss in C57BL/6J Mice.	istradefylline	0-14	renin binding protein	Mus musculus	25-28
34486986-1	2021	BACKGROUND: Istradefylline is a selective adenosine A2A receptor antagonist for the treatment of patients with Parkinson"s disease (PD) experiencing OFF episodes while on levodopa/decarboxylase inhibitor.	istradefylline	12-26	adenosine A2a receptor	Homo sapiens	42-64
35623041-6	2022	We have found that (i) patients show marked IL-8 but not IL-17A responses; (ii) these responses are restricted by HLA-DR; and (iii) IL-8 responses are abrogated by a dopamine D2 like receptor (D2R) agonist, ropinirole, and an adenosine A2a receptor (A2aR) antagonist, istradefylline.	istradefylline	268-282	C-X-C motif chemokine ligand 8	Homo sapiens	132-136
35623041-6	2022	We have found that (i) patients show marked IL-8 but not IL-17A responses; (ii) these responses are restricted by HLA-DR; and (iii) IL-8 responses are abrogated by a dopamine D2 like receptor (D2R) agonist, ropinirole, and an adenosine A2a receptor (A2aR) antagonist, istradefylline.	istradefylline	268-282	dopamine receptor D2	Homo sapiens	193-196
35618883-6	2022	We further showed that pharmacological inhibition of A2AR with istradefylline partially normalised striatal GDNF and striatal and cortical dopamine levels in mice.	istradefylline	63-77	adenosine A2a receptor	Mus musculus	53-57
35618883-6	2022	We further showed that pharmacological inhibition of A2AR with istradefylline partially normalised striatal GDNF and striatal and cortical dopamine levels in mice.	istradefylline	63-77	glial cell line derived neurotrophic factor	Mus musculus	108-112
35631343-6	2022	The MRT of (18F)FLUDA in the striatum of mice was decreased by 30% after treatment with the A2AAR antagonist istradefylline.	istradefylline	109-123	adenosine A2a receptor	Mus musculus	92-97
35149135-2	2022	Here, we studied the effects of the A2AR antagonist KW6002 on retinal injury induced by the mitochondrial oxidative phosphorylation uncoupler, carbonylcyanide m-chlorophenyl hydrazine (CCCP) and alterations in competing endogenous RNA (ceRNA) network.	istradefylline	52-58	adenosine A2a receptor	Homo sapiens	36-40
35041190-7	2022	Treatment with the A2A receptor antagonist KW-6002 blocked the effect of PSB-0777 on SFK Y416 phosphorylation.	istradefylline	43-50	FYN proto-oncogene, Src family tyrosine kinase	Rattus norvegicus	85-88
35149201-1	2022	As an adenosine receptor A2A antagonist, istradefylline is used as an adjunctive agent of levodopa to improve motor symptoms in advanced Parkinson"s disease (PD) patients.	istradefylline	41-55	adenosine A2a receptor	Homo sapiens	6-9
35180864-6	2022	We determined the effect of the A2AR antagonist KW6002 treatment at days 8-12 or 8-14 post-immunization on T cell infiltration across the CP and EAE pathology.	istradefylline	48-54	adenosine A2a receptor	Mus musculus	32-36
35241003-4	2022	Istradefylline, an adenosine A2A receptor antagonist indicated as an adjunctive treatment to levodopa-containing preparations in PD patients experiencing wearing off, is currently available in Japan and the US.	istradefylline	0-14	adenosine A2a receptor	Homo sapiens	32-41
35167016-5	2022	The RNA-seq analysis revealed that the A2AR antagonist KW6002 affected the expression of the cell adhesion molecules" (CAMs) pathway and cell response to IFN-gamma in the CP.	istradefylline	55-61	adenosine A2a receptor	Homo sapiens	39-43
35167016-5	2022	The RNA-seq analysis revealed that the A2AR antagonist KW6002 affected the expression of the cell adhesion molecules" (CAMs) pathway and cell response to IFN-gamma in the CP.	istradefylline	55-61	interferon gamma	Homo sapiens	154-163
35116210-5	2022	Unlike many drugs that treat PD, istradefylline is a nondopaminergic drug that exerts its effects via adenosine A2A receptor antagonism.	istradefylline	33-47	adenosine A2a receptor	Homo sapiens	115-124
35116210-9	2022	Istradefylline is an alternative option to dopaminergic drugs such as dopamine agonists, monoamine oxidase B inhibitors, and catechol-O-methyltransferase inhibitors as an adjunct to L/C in patients with motor fluctuations, but clinical use will further define its role in treatment of PD.	istradefylline	0-14	monoamine oxidase B	Homo sapiens	89-108