| ID Source | ID |
|---|---|
| PubMed CID | 5311037 |
| CHEMBL ID | 431770 |
| CHEBI ID | 134726 |
| SCHEMBL ID | 633262 |
| SCHEMBL ID | 633263 |
| MeSH ID | M0288908 |
| Synonym |
|---|
| kw6002 |
| 8-(2-(3,4-dimethoxyphenyl)ethenyl)-1,3-diethyl-3,7-dihydro-7-methyl-1h-purine-2,6-dione |
| CHEMBL431770 , |
| nouriast |
| LS-14789 |
| HY-10888 |
| istradefylline |
| kw-6002 |
| (e)-8-(3,4-dimethoxystyryl)-1,3-diethyl-7-methyl-3,7-dihydro-1h-purine-2,6-dione |
| 8-((1e)-2-(3,4-dimethoxyphenyl)ethenyl)-1,3-diethyl-7-methyl-3,7-dihydro-1h-purine-2,6-dione |
| 1h-purine-2,6-dione, 3,7-dihydro-1,3-diethyl-8-(2-(3,4-dimethoxyphenyl)ethenyl)-7-methyl-, (e)- |
| (e)-8-(3,4-dimethoxystyryl)-1,3-diethyl-7-methylxanthine |
| nouriast (tn) |
| D04641 |
| nourianz (tn) |
| 155270-99-8 |
| istradefylline (jan/usan/inn) |
| kw 6002 |
| CHEBI:134726 |
| L001483 |
| bdbm50176050 |
| 8-(3,4-dimethoxystyryl)-1,3-diethyl-7-methyl-1h-purine-2,6(3h,7h)-dione |
| 8-[2-(3,4-dimethoxy-phenyl)-vinyl]-1,3-diethyl-7-methyl-3,9-dihydro-purine-2,6-dione |
| 8-[(e)-2-(3,4-dimethoxy-phenyl)-vinyl]-1,3-diethyl-7-methyl-3,7-dihydro-purine-2,6-dione |
| 8-[(e)-2-(3,4-dimethoxyphenyl)ethenyl]-1,3-diethyl-7-methylpurine-2,6-dione |
| AKOS015966268 |
| BCP9000824 |
| 2gz0lik7t4 , |
| unii-2gz0lik7t4 |
| istradefylline [usan:inn:jan] |
| AM84508 |
| 8-[(e)-2-(3,4-dimethoxyphenyl)ethenyl]-1,3-diethyl-7-methyl-purine-2,6 -dione |
| CS-0737 |
| 8-[2-(3,4-dimethoxy-phenyl)-vinyl]-1,3-diethyl-7-methyl-3,7-dihydro-purine-2,6-dione |
| S2790 |
| nourianz |
| gtpl5608 |
| istradefylline [inn] |
| 8-[(1e)-2-(3,4-dimethoxyphenyl)ethenyl]-1,3-diethyl-7-methyl-3,7-dihydro-1h-purine-2,6-dione |
| istradefylline [jan] |
| istradefylline [mi] |
| istradefylline [usan] |
| istradefylline [orange book] |
| istradefylline [who-dd] |
| SCHEMBL633262 |
| SCHEMBL633263 |
| MLS006010633 |
| smr004701638 |
| dtxsid7057652 , |
| dtxcid8031441 |
| cas-155270-99-8 |
| tox21_113855 |
| NCGC00253737-01 |
| (e)- 8-(3,4-dimethoxystyryl)-1,3-diethyl-7-methylxanthine |
| IQVRBWUUXZMOPW-PKNBQFBNSA-N |
| istradefylline (kw-6002) |
| 8-[(1e)-2-(2-(3,4-dimethoxyphenyl)ethenyl]-1,3-diethyl-3,7-dihydro-7-methyl-1h-purine-2,6-dione |
| (e)-8-(3,4-dimethoxystyryl)-1,3-diethyl-7-methyl-1h-purine-2,6(3h,7h)-dione |
| AC-30957 |
| c20h24n4o4 |
| J-519355 |
| SR-01000945278-1 |
| sr-01000945278 |
| istradefylline, >=98% (hplc) |
| J-009183 |
| istradefyline |
| SW220139-1 |
| DB11757 |
| 8-[(e)-2-(3,4-dimethoxyphenyl)vinyl]-1,3-diethyl-7-methyl-3,7-dihydro-1h-purine-2,6-dione |
| mfcd00928421 |
| BCP02194 |
| kw 6002;kw-6002;kw6002 |
| Q905783 |
| 606080-73-3 |
| BRD-K40096621-001-01-2 |
| HMS3884P16 |
| CCG-268457 |
| HB2134 |
| JQ9 , |
| 8-[(~{e})-2-(3,4-dimethoxyphenyl)ethenyl]-1,3-diethyl-7-methyl-purine-2,6-dione |
| istradefyllinum |
| istradefilina |
| I1100 |
| istradefylline impurity 2 |
| (e)-8-[2-(3,4-dimethoxyphenyl)ethenyl]-1,3-diethyl-3,7-dihydro-7-methyl-1h-purine-2,6-dione |
| 8-[(1e)-2-(3,4-dimethoxyphenyl)ethenyl]-1,3-diethyl-7-methyl-2,3,6,7-tetrahydro-1h-purine-2,6-dione |
| EN300-7393038 |
Istradefylline is a first-in-class, non-dopaminergic, selective adenosine A. receptor antagonist. It significantly reduces the "off" time and improves the motor function of patients with PD.
| Excerpt | Reference | Relevance |
|---|---|---|
| "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." | ( Efficacy of Istradefylline, an Adenosine A2A Receptor Antagonist, as Adjunctive Therapy to Levodopa in Parkinson's Disease: A Pooled Analysis of 8 Phase 2b/3 Trials. Fernandez, H; Hattori, N; Hauser, RA; Isaacson, SH; LeWitt, P; Li, J; Mochizuki, H; Mori, A; Nakajima, Y; Rascol, O; Ristuccia, R; Stocchi, F, 2021) | 2.44 |
| "Istradefylline is a selective adenosine A2a receptor (A2aR) antagonist used for the treatment of Parkinson's disease." | ( Istradefylline, an adenosine A2a receptor antagonist, inhibits the CD4 Kawano, M; Matsushita, S; Takagi, R; Tokano, M, 2022) | 2.89 |
| "Istradefylline is a novel drug for PD." | ( A new therapeutic strategy with istradefylline for postural deformities in Parkinson's disease. Fujioka, S; Fukae, J; Hayashi, Y; Kikuchi, H; Kitano, K; Mishima, T; Nose, K; Tsuboi, Y; Yoshida, R, 2019) | 1.52 |
| "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: adenosine A2A receptor antagonist to reduce "OFF" time in Parkinson's disease. Paton, DM, 2020) | 2.72 |
| "Istradefylline (ISD) is a new drug developed for the treatment of Parkinson's disease (PD). " | ( Istradefylline for the treatment of Parkinson's disease: is it a promising strategy? Stocchi, F; Torti, M; Vacca, L, 2018) | 3.37 |
| "Istradefylline is a first-in-class, non-dopaminergic, selective adenosine A" | ( Safety and effectiveness of istradefylline in patients with Parkinson's disease: interim analysis of a post-marketing surveillance study in Japan. Asai, N; Fujita, M; Mori, A; Saki, M; Takahashi, M, 2018) | 2.22 |
| "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." | ( In vitro pharmacological profile of the A2A receptor antagonist istradefylline. Kanda, T; Koshimura, E; Saki, M; Sasaki, K; Yamada, K, 2013) | 1.35 |
| "Istradefylline is a selective adenosine A2A receptor antagonist. " | ( A long-term study of istradefylline safety and efficacy in patients with Parkinson disease. Kondo, T; Mizuno, Y, ) | 1.89 |
| "Istradefylline (KW-6002) is an adenosine A(2A) receptor antagonist that in primate models of PD improves motor function without causing or worsening dyskinesia." | ( Study of istradefylline in patients with Parkinson's disease on levodopa with motor fluctuations. Ballerini, R; Hauser, RA; Mori, A; Roberts, JW; Shulman, LM; Sussman, NM; Trugman, JM, 2008) | 1.48 |
| "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 for Parkinson's disease patients experiencing motor fluctuations: results of the KW-6002-US-018 study. Ballerini, R; Chaikin, P; Fernandez, HH; Mori, A; Pourcher, E; Stacy, M, 2012) | 3.26 |
| "Istradefylline is a selective adenosine A(2A) antagonist that is currently of interest for the treatment of motor complications in PD." | ( Istradefylline for the treatment of Parkinson's disease. Park, A; Stacy, M, 2012) | 2.54 |
| "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, a novel adenosine A2A receptor antagonist, for the treatment of Parkinson's disease. Jenner, P, 2005) | 2.49 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "Istradefylline enhance Aβ generation and γ-secretase activity possibly via modulating the interaction between A2AR and γ-secretase, which may bring some undesired effects in the central nervous system (CNS)." | ( An Anti-Parkinson's Disease Drug via Targeting Adenosine A2A Receptor Enhances Amyloid-β Generation and γ-Secretase Activity. Chen, M; Cui, J; Li, X; Lu, J; Pei, G; Wang, X; Yang, W; Zhao, J; Zhou, Y, 2016) | 1.16 |
Istradefylline treatment at specific doses with sub-optimal l-DOPA specifically alleviated bradykinesia. Subjects had significant placebo-corrected reductions in daily OFF time from baseline to endpoint.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Istradefylline treatment at specific doses with sub-optimal l-DOPA specifically alleviated bradykinesia." | ( An evaluation of istradefylline treatment on Parkinsonian motor and cognitive deficits in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-treated macaque models. Bezard, E; Camus, SM; Ko, WKD; Li, Q; McGuire, S; Pioli, EY; Yang, J, 2016) | 1.5 |
| "Istradefylline-treated subjects had significant placebo-corrected reductions in daily OFF time from baseline to endpoint: 4.6% (P = 0.03) and 0.7 hours (P = 0.03)." | ( Study of istradefylline in patients with Parkinson's disease on levodopa with motor fluctuations. Ballerini, R; Hauser, RA; Mori, A; Roberts, JW; Shulman, LM; Sussman, NM; Trugman, JM, 2008) | 1.48 |
Istradefylline was safe and well tolerated in clinical trials, which have focused on l-DOPA-treated PD patients.
| Excerpt | Reference | Relevance |
|---|---|---|
| " Moreover, the potential drug-drug interaction with istradefylline was determined as well as underlied mechanism." | ( The effect of CYP3A4 genetic polymorphism and drug interaction on the metabolism of istradefylline. Cai, J; Gao, N; Hu, G; Hu, X; Ni, J; Qian, J; Ye, Z, 2022) | 1.2 |
| Excerpt | Relevance | Reference |
|---|---|---|
| " Selective adenosine A(2A) receptor antagonists, such as KW-6002, may be one means of reducing the dosage of L-DOPA used in treating Parkinson's disease and are potentially a novel approach to treating the illness both as monotherapy and in combination with dopaminergic drugs." | ( Combined use of the adenosine A(2A) antagonist KW-6002 with L-DOPA or with selective D1 or D2 dopamine agonists increases antiparkinsonian activity but not dyskinesia in MPTP-treated monkeys. Jackson, MJ; Jenner, P; Kanda, T; Kase, H; Kuwana, Y; Nakamura, J; Pearce, RK; Smith, LA, 2000) | 0.31 |
| " Wearing-off can be treated by dietary manipulation, shortening the dosing interval, substituting sustained-release levodopa, adding amantadine, or monoamine oxidase type B inhibitors, and other options, including catechol-O-methyltransferase inhibitors and the approved dopamine agonists addressed in another chapter." | ( Other pharmacological treatments for motor complications and dyskinesias. Waters, C, 2005) | 0.33 |
| " Time-course and dose-response experiments indicate that DARPP-32 phosphorylation is maximal 30 min following administration of 10mg/kg of THC." | ( Regulation of DARPP-32 phosphorylation by Delta9-tetrahydrocannabinol. Borgkvist, A; Fisone, G; Fuxe, K; Greengard, P; Marcellino, D, 2008) | 0.35 |
| " It had acceptable ADME properties; however, the low intrinsic solubility of this compound was limiting for its developability, because the oral bioavailability from dosing in suspension was significantly lower than the oral bioavailability from solution dosage." | ( Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} ester (Lu AA47070): a phosphonooxymethylene prodrug of a potent and selective hA(2A) receptor antagonist. Bang-Andersen, B; Brennum, LT; Bundgaard, C; Howells, ME; Jørgensen, EB; Kreilgård, M; Langgård, M; Larsen, M; Mikkelsen, GK; Sams, AG; Schrøder, TJ; Torup, L, 2011) | 0.37 |
| " SCH-442416 produced a significant shift to the right of the THC self-administration dose-response curves, consistent with antagonism of the reinforcing effects of THC." | ( Differential effects of presynaptic versus postsynaptic adenosine A2A receptor blockade on Δ9-tetrahydrocannabinol (THC) self-administration in squirrel monkeys. Ferré, S; Goldberg, SR; Justinová, Z; Redhi, GH, 2014) | 0.4 |
| "4 mg/kg) produced a downward shift in the cocaine dose-response curve under a fixed ratio schedule of reinforcement and decreased the cocaine breaking point." | ( On the role of adenosine (A)₂A receptors in cocaine-induced reward: a pharmacological and neurochemical analysis in rats. Filip, M; Fuxe, K; Gołembiowska, K; Kamińska, K; Suder, A; Wydra, K, 2015) | 0.42 |
| " In early PD, this may avoid dose escalation or allow a reduction in dopamine agonist dosage without a loss of efficacy and prevent dopaminergic side-effects from becoming treatment limiting." | ( The adenosine A2A receptor antagonist, istradefylline enhances the anti-parkinsonian activity of low doses of dopamine agonists in MPTP-treated common marmosets. Jenner, P; Kanda, T; Kawai-Uchida, M; Mori, A; Okita, E; Soshiroda, K; Uchida, S, 2015) | 0.69 |
| " All patients recovered after changing the timing of the ISD dosage from evening to morning." | ( Istradefylline is recommended for morning use: a report of 4 cases. Matsuura, K; Tomimoto, H, 2015) | 1.86 |
| " Istradefylline was administered for 52 weeks at a starting dosage of 20 mg/d, with or without dosage adjustment up to 40 mg/d." | ( A long-term study of istradefylline safety and efficacy in patients with Parkinson disease. Kondo, T; Mizuno, Y, ) | 1.36 |
| " Increasing dosing of levodopa weakens the methylation potential in the brain as a result of the methyl group consuming conversion of levodopa to 3-O-methyldopa in glial cells." | ( The role of istradefylline in the Parkinson's disease armamentarium. Müller, T, 2023) | 1.29 |
| Class | Description |
|---|---|
| oxopurine | |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Pathway | Proteins | Compounds |
|---|---|---|
| Purinergic signaling | 0 | 53 |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 14.9601 | 0.0060 | 38.0041 | 19,952.5996 | AID1159523 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 10.4579 | 0.0007 | 14.5928 | 83.7951 | AID1259369; AID1259392 |
| AR protein | Homo sapiens (human) | Potency | 18.9586 | 0.0002 | 21.2231 | 8,912.5098 | AID1259243; AID1259247 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 0.6085 | 0.0010 | 22.6508 | 76.6163 | AID1224838; AID1224893 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 20.1293 | 0.0015 | 30.6073 | 15,848.9004 | AID1224848; AID1224849; AID1259403 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 26.6032 | 0.0054 | 28.0263 | 1,258.9301 | AID1346982 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 33.4915 | 0.0002 | 29.3054 | 16,493.5996 | AID1259244 |
| peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 29.8470 | 0.0010 | 24.5048 | 61.6448 | AID743215 |
| Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 33.4915 | 0.0015 | 57.7890 | 15,848.9004 | AID1259244 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 33.4915 | 0.0015 | 51.7393 | 15,848.9004 | AID1259244 |
| [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) |
|---|---|---|---|---|---|---|---|
| Cytochrome P450 1A2 | Homo sapiens (human) | IC50 (µMol) | 40.0000 | 0.0001 | 1.7740 | 10.0000 | AID569671 |
| Cytochrome P450 3A4 | Homo sapiens (human) | IC50 (µMol) | 40.0000 | 0.0001 | 1.7536 | 10.0000 | AID569675 |
| Adenosine receptor A3 | Homo sapiens (human) | Ki | 3.9187 | 0.0000 | 0.9306 | 10.0000 | AID1057067; AID1138025; AID1412906; AID1639027; AID1696178; AID692306; AID747662; AID747679 |
| Cytochrome P450 2D6 | Homo sapiens (human) | IC50 (µMol) | 40.0000 | 0.0000 | 2.0151 | 10.0000 | AID569674 |
| Cytochrome P450 2C9 | Homo sapiens (human) | IC50 (µMol) | 13.0000 | 0.0000 | 2.8005 | 10.0000 | AID569672 |
| Adenosine receptor A1 | Rattus norvegicus (Norway rat) | Ki | 0.2300 | 0.0001 | 1.2092 | 9.9700 | AID1639021 |
| Amine oxidase [flavin-containing] B | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0000 | 1.8914 | 9.5700 | AID723213 |
| Amine oxidase [flavin-containing] B | Homo sapiens (human) | Ki | 0.0270 | 0.0006 | 1.7771 | 10.0000 | AID1637752 |
| Adenosine receptor A2a | Homo sapiens (human) | IC50 (µMol) | 5.2490 | 0.0007 | 1.5594 | 10.0000 | AID747270 |
| Adenosine receptor A2a | Homo sapiens (human) | Ki | 0.0468 | 0.0000 | 1.0609 | 9.7920 | AID1057070; AID1138023; AID1193095; AID1402799; AID1412904; AID1639022; AID1696175; AID1854970; AID1871328; AID254542; AID312873; AID424225; AID501542; AID569664; AID607198; AID692486; AID723214; AID747271; AID747664; AID747681 |
| Adenosine receptor A2b | Homo sapiens (human) | Ki | 7.6571 | 0.0002 | 1.6352 | 10.0000 | AID1057072; AID1138021; AID1412905; AID1639025; AID1696176; AID692304; AID747680 |
| Adenosine receptor A1 | Homo sapiens (human) | Ki | 1.9050 | 0.0002 | 0.9316 | 10.0000 | AID1057068; AID1138024; AID1193096; AID1412903; AID1639019; AID1696177; AID254536; AID501540; AID569665; AID691842; AID747272; AID747660; AID747682 |
| Adenosine receptor A2a | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.2280 | 0.0012 | 0.4828 | 9.0000 | AID1152967 |
| Adenosine receptor A2a | Rattus norvegicus (Norway rat) | Ki | 2.1704 | 0.0002 | 1.4940 | 10.0000 | AID1057068; AID1639024; AID312884; AID387203; AID747680 |
| Cytochrome P450 2C19 | Homo sapiens (human) | IC50 (µMol) | 40.0000 | 0.0000 | 2.3983 | 10.0000 | AID569673 |
| [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) |
|---|---|---|---|---|---|---|---|
| NPYLR7B | Aedes aegypti (yellow fever mosquito) | EC50 (µMol) | 20.0000 | 0.0390 | 2.2899 | 18.3000 | AID1259426 |
| Adenosine receptor A2a | Homo sapiens (human) | Kd | 1.2589 | 0.0002 | 0.4731 | 9.6000 | AID607198 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1637752 | Inhibition of human MAOB | 2019 | MedChemComm, Jan-01, Volume: 10, Issue:1 | Discovery of monoamine oxidase inhibitors by medicinal chemistry approaches. |
| AID1412905 | Binding affinity to human adenosine A2B receptor by radioligand displacement assay | 2018 | MedChemComm, Jun-01, Volume: 9, Issue:6 | Tricyclic xanthine derivatives containing a basic substituent: adenosine receptor affinity and drug-related properties. |
| AID312884 | Displacement of [3H]ZM241385 from rat recombinant adenosine A2A receptor expressed in CHO cells | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3 | Identification of novel, water-soluble, 2-amino-N-pyrimidin-4-yl acetamides as A2A receptor antagonists with in vivo efficacy. |
| AID569672 | Inhibition of recombinant CYP2C9 after 45 mins | 2011 | Journal of medicinal chemistry, Feb-10, Volume: 54, Issue:3 | Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} ester (Lu AA47070): a phosphonooxymethylene prodrug of a potent and selective hA(2A) receptor antagonist. |
| AID1056829 | Antagonist activity at adenosine A2A receptor in C57/BL6 mouse lymphocytes assessed as inhibition of CGS-21680-mediated cAMP accumulation at 0.5 to 10 uM after 15 mins by ELISA | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 | Design and evaluation of xanthine based adenosine receptor antagonists: potential hypoxia targeted immunotherapies. |
| AID1193095 | Antagonist activity at human adenosine A2A receptor | 2015 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6 | Synthesis and SAR studies of analogues of 4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-N-thiazol-2-yl-benzamide (Lu AA41063) as adenosine A2A receptor ligands with improved aqueous solubility. |
| AID569674 | Inhibition of recombinant CYP2D6 after 45 mins | 2011 | Journal of medicinal chemistry, Feb-10, Volume: 54, Issue:3 | Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} ester (Lu AA47070): a phosphonooxymethylene prodrug of a potent and selective hA(2A) receptor antagonist. |
| 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. |
| AID1248384 | Displacement of [3H]-ZM241385 from Adenosine A2A receptor in Lister hooded rat brain membranes | 2015 | Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20 | 1,3,7-Triethyl-substituted xanthines--possess nanomolar affinity for the adenosine A1 receptor. |
| AID424227 | Selectivity for human adenosine A2A receptor over human adenosine A1 receptor | 2009 | Bioorganic & medicinal chemistry letters, May-15, Volume: 19, Issue:10 | Antagonists of the human A(2A) receptor. Part 5: Highly bio-available pyrimidine-4-carboxamides. |
| 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. |
| AID1056822 | Half life in rat | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 | Design and evaluation of xanthine based adenosine receptor antagonists: potential hypoxia targeted immunotherapies. |
| AID747684 | Displacement of [3H]CCPA from adenosine A1 receptor in rat brain cortical membranes after 90 mins by liquid scintillation counting analysis | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Dual targeting of adenosine A(2A) receptors and monoamine oxidase B by 4H-3,1-benzothiazin-4-ones. |
| AID747660 | Displacement of [3H]CCPA from human recombinant adenosine A1 receptor expressed in CHO cells | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Dual targeting of adenosine A(2A) receptors and monoamine oxidase B by 4H-3,1-benzothiazin-4-ones. |
| AID692304 | Displacement of [3H]PSB-298 from human recombinant adenosine A2B receptor expressed in CHO cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and biological activity of tricyclic cycloalkylimidazo-, pyrimido- and diazepinopurinediones. |
| AID723213 | Inhibition of human MAOB after 1 hr by luminescence assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Synthesis of (E)-8-(3-chlorostyryl)caffeine analogues leading to 9-deazaxanthine derivatives as dual A(2A) antagonists/MAO-B inhibitors. |
| AID536230 | Reversal of haloperidol-induced catalepsy in po dosed BALB/c mouse administered 30 mins after haloperidol challenge measured for 60 seconds after 1 hr | 2010 | Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22 | In vivo characterization of a dual adenosine A2A/A1 receptor antagonist in animal models of Parkinson's disease. |
| AID747662 | Displacement of [3H]PSB-11 from human recombinant adenosine A3 receptor expressed in CHO cells | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Dual targeting of adenosine A(2A) receptors and monoamine oxidase B by 4H-3,1-benzothiazin-4-ones. |
| AID692305 | Displacement of [3H]PSB-298 from human recombinant adenosine A2B receptor expressed in CHO cells at 10 uM | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and biological activity of tricyclic cycloalkylimidazo-, pyrimido- and diazepinopurinediones. |
| AID307861 | Displacement of [3H]CCPA from adenosine A1 receptor in rat brain cortical membrane at 25 uM | 2007 | Bioorganic & medicinal chemistry, Jul-15, Volume: 15, Issue:14 | N9-benzyl-substituted 1,3-dimethyl- and 1,3-dipropyl-pyrimido[2,1-f]purinediones: synthesis and structure-activity relationships at adenosine A1 and A2A receptors. |
| AID569703 | Reversal of haloperidol-induced hypolocomotion in po dosed NMRI mouse administered 30 mins before haloperidol challenge measured for 20 mins | 2011 | Journal of medicinal chemistry, Feb-10, Volume: 54, Issue:3 | Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} ester (Lu AA47070): a phosphonooxymethylene prodrug of a potent and selective hA(2A) receptor antagonist. |
| AID1402799 | Antagonist activity at adenosine A2A receptor (unknown origin) | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Antagonists of the adenosine A |
| AID412514 | Reversal of haloperidol-induced hypolocomotion in Sprague-Dawley rat assessed as time spent for locomotor activity at 1 mg/kg, po administered 120 mins prior to testing done for 60 mins | 2009 | Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1 | Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines. |
| AID607202 | Binding affinity at human adenosine receptor A2a receptor Y271A'7.36 mutant expressed in HEK293 cells followed by receptor capturing on Biocore chips assessed as log difference in receptor affinity by SPR method relative to wild type stabilized A2A recept | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Biophysical mapping of the adenosine A2A receptor. |
| AID1152973 | Anticataleptogenic activity in in po dosed ddY mouse assessed as reduction in haloperidol-induced catelepsy measured after 5 hrs | 2014 | Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12 | 8-Substituted 2-alkynyl-N(9)-propargyladenines as A2A adenosine receptor antagonists. |
| AID691842 | Displacement of [3H]CCPA from human recombinant adenosine A1 receptor expressed in CHO cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and biological activity of tricyclic cycloalkylimidazo-, pyrimido- and diazepinopurinediones. |
| AID1639027 | Displacement of [3H]PSB11 from recombinant human adenosine A3 receptor expressed in CHO cells | 2019 | Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7 | Novel multi-target directed ligands based on annelated xanthine scaffold with aromatic substituents acting on adenosine receptor and monoamine oxidase B. Synthesis, in vitro and in silico studies. |
| AID747681 | Displacement of [3H]MSX2 from human recombinant adenosine A2A receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Dual targeting of adenosine A(2A) receptors and monoamine oxidase B by 4H-3,1-benzothiazin-4-ones. |
| AID1696178 | Inhibition of human adenosine A3 receptor | |||
| AID692486 | Displacement of [3H]MSX-2 from human recombinant adenosine A2A receptor expressed in CHO cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and biological activity of tricyclic cycloalkylimidazo-, pyrimido- and diazepinopurinediones. |
| AID424233 | Selectivity for human adenosine A2A receptor over human adenosine A3 receptor | 2009 | Bioorganic & medicinal chemistry letters, May-15, Volume: 19, Issue:10 | Antagonists of the human A(2A) receptor. Part 5: Highly bio-available pyrimidine-4-carboxamides. |
| AID301679 | Displacement of [3H]MSX2 from adenosine A2A receptor in rat brain striatal membrane | 2007 | Bioorganic & medicinal chemistry, Nov-15, Volume: 15, Issue:22 | Phenylethyl-substituted pyrimido[2,1-f]purinediones and related compounds: structure-activity relationships as adenosine A(1) and A(2A) receptor ligands. |
| AID1696177 | Inhibition of human adenosine A1 receptor | |||
| AID1248378 | Displacement of [3H]-DPCPX from Adenosine A1 receptor in Lister hooded rat brain membranes | 2015 | Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20 | 1,3,7-Triethyl-substituted xanthines--possess nanomolar affinity for the adenosine A1 receptor. |
| AID387203 | Displacement of [3H]NECA from Sprague-Dawley rat adenosine A2A receptor by scintillation counting | 2008 | Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18 | Dual inhibition of monoamine oxidase B and antagonism of the adenosine A(2A) receptor by (E,E)-8-(4-phenylbutadien-1-yl)caffeine analogues. |
| AID607203 | Binding affinity at human adenosine receptor A2a I66A'2.64 mutant expressed in HEK293 cells followed by receptor capturing on Biocore chips assessed as log difference in receptor affinity by SPR method relative to wild type stabilized A2A receptor | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Biophysical mapping of the adenosine A2A receptor. |
| AID569675 | Inhibition of recombinant CYP3A4 after 30 mins | 2011 | Journal of medicinal chemistry, Feb-10, Volume: 54, Issue:3 | Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} ester (Lu AA47070): a phosphonooxymethylene prodrug of a potent and selective hA(2A) receptor antagonist. |
| AID569667 | Intrinsic clearance in human liver microsomes at 1 uM after 60 mins by LC-MS/MS analysis | 2011 | Journal of medicinal chemistry, Feb-10, Volume: 54, Issue:3 | Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} ester (Lu AA47070): a phosphonooxymethylene prodrug of a potent and selective hA(2A) receptor antagonist. |
| AID569671 | Inhibition of recombinant CYP1A2 after 28 mins | 2011 | Journal of medicinal chemistry, Feb-10, Volume: 54, Issue:3 | Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} ester (Lu AA47070): a phosphonooxymethylene prodrug of a potent and selective hA(2A) receptor antagonist. |
| AID747664 | Displacement of [3H]MSX2 from human recombinant adenosine A2A receptor expressed in CHO cells | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Dual targeting of adenosine A(2A) receptors and monoamine oxidase B by 4H-3,1-benzothiazin-4-ones. |
| AID424232 | Selectivity for human adenosine A2A receptor over human adenosine A2B receptor | 2009 | Bioorganic & medicinal chemistry letters, May-15, Volume: 19, Issue:10 | Antagonists of the human A(2A) receptor. Part 5: Highly bio-available pyrimidine-4-carboxamides. |
| AID1705446 | Half life in human | 2020 | European journal of medicinal chemistry, Nov-01, Volume: 205 | New drug approvals for 2019: Synthesis and clinical applications. |
| AID569673 | Inhibition of recombinant CYP2C19 after 45 mins | 2011 | Journal of medicinal chemistry, Feb-10, Volume: 54, Issue:3 | Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} ester (Lu AA47070): a phosphonooxymethylene prodrug of a potent and selective hA(2A) receptor antagonist. |
| AID607200 | Binding affinity at human adenosine receptor A2a L167A'extracellular loop 2 mutant expressed in HEK293 cells followed by receptor capturing on Biocore chips assessed as log difference in receptor affinity by SPR method relative to wild type stabilized A2A | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Biophysical mapping of the adenosine A2A receptor. |
| AID1816611 | Reversal of haloperidol-induced catalepsy in Sprague-Dawley rat assessed as reduction in catalepsy at 0.6 mg/kg, ip measured after 120 min | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14 | First-Time Disclosure of CVN424, a Potent and Selective GPR6 Inverse Agonist for the Treatment of Parkinson's Disease: Discovery, Pharmacological Validation, and Identification of a Clinical Candidate. |
| AID692306 | Displacement of [3H]PSB-11 from human recombinant adenosine A3 receptor expressed in CHO cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and biological activity of tricyclic cycloalkylimidazo-, pyrimido- and diazepinopurinediones. |
| AID1639019 | Displacement of [3H]CCPA from recombinant human adenosine A1 receptor expressed in CHO cells | 2019 | Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7 | Novel multi-target directed ligands based on annelated xanthine scaffold with aromatic substituents acting on adenosine receptor and monoamine oxidase B. Synthesis, in vitro and in silico studies. |
| AID569665 | Displacement of [3H]-DPCPX from human adenosine A1 receptor expressed in CHO cells after 30 mins by scintillation counting | 2011 | Journal of medicinal chemistry, Feb-10, Volume: 54, Issue:3 | Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} ester (Lu AA47070): a phosphonooxymethylene prodrug of a potent and selective hA(2A) receptor antagonist. |
| AID1152967 | Antagonist activity at adenosine A2A receptor in 5-HT-treated Wistar rat femoral vein assessed as inhibition of 2-octyn-1-yladenosine-induced vasodilation incubated for 10 mins prior to addition of 5-HT | 2014 | Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12 | 8-Substituted 2-alkynyl-N(9)-propargyladenines as A2A adenosine receptor antagonists. |
| AID301667 | Displacement of [3H]CCPA from adenosine A1 receptor in rat brain cortical membrane | 2007 | Bioorganic & medicinal chemistry, Nov-15, Volume: 15, Issue:22 | Phenylethyl-substituted pyrimido[2,1-f]purinediones and related compounds: structure-activity relationships as adenosine A(1) and A(2A) receptor ligands. |
| AID1057072 | Binding affinity to human adenosine A2B receptor | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 | 1,3-Dialkyl-substituted tetrahydropyrimido[1,2-f]purine-2,4-diones as multiple target drugs for the potential treatment of neurodegenerative diseases. |
| AID1152972 | Anticataleptogenic activity in ddY mouse assessed as reduction in haloperidol-induced catelepsy at 3 mg/kg, po measured after 1 to 7 hrs | 2014 | Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12 | 8-Substituted 2-alkynyl-N(9)-propargyladenines as A2A adenosine receptor antagonists. |
| AID607231 | Binding affinity at human adenosine receptor A2a N181A'5.42 mutant expressed in HEK293 cells followed by receptor capturing on Biocore chips assessed as log difference in receptor affinity by SPR method relative to wild type stabilized A2A receptor | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Biophysical mapping of the adenosine A2A receptor. |
| AID1057069 | Displacement of [3H]DPCPX from adenosine A1 receptor in rat brain after 60 mins by scintillation counting analysis | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 | 1,3-Dialkyl-substituted tetrahydropyrimido[1,2-f]purine-2,4-diones as multiple target drugs for the potential treatment of neurodegenerative diseases. |
| AID747271 | Antagonist activity at human adenosine A2A receptor assessed as cAMP level by cell based assay | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | Novel adenosine A(2A) receptor ligands: a synthetic, functional and computational investigation of selected literature adenosine A(2A) receptor antagonists for extending into extracellular space. |
| AID747679 | Displacement of [3H]PSB-11 from human recombinant adenosine A3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting analysis | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Dual targeting of adenosine A(2A) receptors and monoamine oxidase B by 4H-3,1-benzothiazin-4-ones. |
| AID1057070 | Displacement of [3H]CGS21680 from human adenosine A2A receptor expressed in CHO cells after 60 mins by scintillation counting analysis | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 | 1,3-Dialkyl-substituted tetrahydropyrimido[1,2-f]purine-2,4-diones as multiple target drugs for the potential treatment of neurodegenerative diseases. |
| AID1152966 | Selectivity for adenosine A2A receptor (unknown origin) over adenosine A1 receptor (unknown origin) | 2014 | Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12 | 8-Substituted 2-alkynyl-N(9)-propargyladenines as A2A adenosine receptor antagonists. |
| AID691848 | Displacement of [3H]CCPA from adenosine A1 receptor in rat brain cortical membrane | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and biological activity of tricyclic cycloalkylimidazo-, pyrimido- and diazepinopurinediones. |
| AID1056825 | Photostability of the compound assessed as compound remaining measured within 24 hrs by HPLC analysis | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 | Design and evaluation of xanthine based adenosine receptor antagonists: potential hypoxia targeted immunotherapies. |
| AID1056824 | Photostability of the compound assessed as compound remaining measured within 7 days by HPLC analysis | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 | Design and evaluation of xanthine based adenosine receptor antagonists: potential hypoxia targeted immunotherapies. |
| AID307866 | Displacement of [3H]MSX2 from adenosine A2A receptor in rat striatal membrane at 25 uM | 2007 | Bioorganic & medicinal chemistry, Jul-15, Volume: 15, Issue:14 | N9-benzyl-substituted 1,3-dimethyl- and 1,3-dipropyl-pyrimido[2,1-f]purinediones: synthesis and structure-activity relationships at adenosine A1 and A2A receptors. |
| AID747272 | Antagonist activity at human adenosine A1 receptor assessed as cAMP level by cell based assay | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | Novel adenosine A(2A) receptor ligands: a synthetic, functional and computational investigation of selected literature adenosine A(2A) receptor antagonists for extending into extracellular space. |
| AID501545 | Reversal of haloperidol-induced hypolocomotion in po dosed NMRI mouse model of Parkinson's disease measured for 20 mins | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17 | Hit-to-lead optimization of a series of carboxamides of ethyl 2-amino-4-phenylthiazole-5-carboxylates as novel adenosine A2A receptor antagonists. |
| AID312873 | Displacement of [3H]ZM-241385 from human recombinant adenosine A2A receptor expressed in HEK293 cells | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3 | Identification of novel, water-soluble, 2-amino-N-pyrimidin-4-yl acetamides as A2A receptor antagonists with in vivo efficacy. |
| AID747270 | Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | Novel adenosine A(2A) receptor ligands: a synthetic, functional and computational investigation of selected literature adenosine A(2A) receptor antagonists for extending into extracellular space. |
| AID747680 | Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysis | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Dual targeting of adenosine A(2A) receptors and monoamine oxidase B by 4H-3,1-benzothiazin-4-ones. |
| AID691844 | Selectivity ratio of Ki for adenosine A1 receptor in rat brain cortical membrane to Ki for adenosine A2A receptor in rat brain striatal membrane | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and biological activity of tricyclic cycloalkylimidazo-, pyrimido- and diazepinopurinediones. |
| AID1412906 | Binding affinity to human adenosine A3 receptor by radioligand displacement assay | 2018 | MedChemComm, Jun-01, Volume: 9, Issue:6 | Tricyclic xanthine derivatives containing a basic substituent: adenosine receptor affinity and drug-related properties. |
| AID536330 | Reversal of haloperidol-induced catalepsy in BALB/c mouse at 3 mg/kg, po administered 30 mins after haloperidol challenge measured for 60 seconds after 4 hrs | 2010 | Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22 | In vivo characterization of a dual adenosine A2A/A1 receptor antagonist in animal models of Parkinson's disease. |
| AID607198 | Displacement of [3H]ZM241385 from stabilized human adenosine receptor A2a expressed in HEK293 cells followed by receptor capturing on Biocore chips by SPR method | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Biophysical mapping of the adenosine A2A receptor. |
| 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. |
| AID607201 | Binding affinity at human adenosine receptor A2a M177A'5.38 mutant expressed in HEK293 cells followed by receptor capturing on Biocore chips assessed as log difference in receptor affinity by SPR method relative to wild type stabilized A2A receptor | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Biophysical mapping of the adenosine A2A receptor. |
| AID1639024 | Displacement of [3H]CCPA from rat adenosine A2a receptor | 2019 | Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7 | Novel multi-target directed ligands based on annelated xanthine scaffold with aromatic substituents acting on adenosine receptor and monoamine oxidase B. Synthesis, in vitro and in silico studies. |
| AID254536 | Binding affinity towards human Adenosine A1 receptor expressed in CHO cells using 1 nM [3H]DPCPX | 2005 | Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22 | 2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization. |
| AID1056821 | Partition coefficient, log K of the compound | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 | Design and evaluation of xanthine based adenosine receptor antagonists: potential hypoxia targeted immunotherapies. |
| AID1057068 | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells after 60 mins by scintillation counting analysis | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 | 1,3-Dialkyl-substituted tetrahydropyrimido[1,2-f]purine-2,4-diones as multiple target drugs for the potential treatment of neurodegenerative diseases. |
| AID307859 | Displacement of [3H]CCPA from adenosine A1 receptor in rat brain cortical membrane | 2007 | Bioorganic & medicinal chemistry, Jul-15, Volume: 15, Issue:14 | N9-benzyl-substituted 1,3-dimethyl- and 1,3-dipropyl-pyrimido[2,1-f]purinediones: synthesis and structure-activity relationships at adenosine A1 and A2A receptors. |
| AID1639021 | Displacement of [3H]CCPA from adenosine A1 receptor in rat brain cortical membranes | 2019 | Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7 | Novel multi-target directed ligands based on annelated xanthine scaffold with aromatic substituents acting on adenosine receptor and monoamine oxidase B. Synthesis, in vitro and in silico studies. |
| AID747682 | Displacement of [3H]CCPA from human recombinant adenosine A1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting analysis | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Dual targeting of adenosine A(2A) receptors and monoamine oxidase B by 4H-3,1-benzothiazin-4-ones. |
| AID747659 | Displacement of [3H]MSX2 from adenosine A2A receptor in rat brain striatal membranes | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Dual targeting of adenosine A(2A) receptors and monoamine oxidase B by 4H-3,1-benzothiazin-4-ones. |
| AID1696175 | Antagonist activity at human adenosine 2A receptor | |||
| AID307864 | Displacement of [3H]MSX2 from adenosine A2A receptor in rat striatal membrane | 2007 | Bioorganic & medicinal chemistry, Jul-15, Volume: 15, Issue:14 | N9-benzyl-substituted 1,3-dimethyl- and 1,3-dipropyl-pyrimido[2,1-f]purinediones: synthesis and structure-activity relationships at adenosine A1 and A2A receptors. |
| AID1056826 | Octanol-water partition coefficient, log P of the compound by HPLC analysis | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 | Design and evaluation of xanthine based adenosine receptor antagonists: potential hypoxia targeted immunotherapies. |
| 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. |
| AID424225 | Displacement of [3H]CGS21680 from human adenosine A2A receptor | 2009 | Bioorganic & medicinal chemistry letters, May-15, Volume: 19, Issue:10 | Antagonists of the human A(2A) receptor. Part 5: Highly bio-available pyrimidine-4-carboxamides. |
| AID1057067 | Displacement of [3H]NECA from human adenosine A3 receptor expressed in CHO cells after 60 mins by scintillation counting analysis | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 | 1,3-Dialkyl-substituted tetrahydropyrimido[1,2-f]purine-2,4-diones as multiple target drugs for the potential treatment of neurodegenerative diseases. |
| AID1057071 | Displacement of [3H]CGS21680 from adenosine A2A receptor in rat brain after 60 mins by scintillation counting analysis | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 | 1,3-Dialkyl-substituted tetrahydropyrimido[1,2-f]purine-2,4-diones as multiple target drugs for the potential treatment of neurodegenerative diseases. |
| AID691845 | Displacement of [3H]MSX-2 from adenosine A2A receptor in rat brain striatal membrane | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and biological activity of tricyclic cycloalkylimidazo-, pyrimido- and diazepinopurinediones. |
| AID1639025 | Displacement of [3H]PSB603 from recombinant human adenosine A2b receptor expressed in HEK293 cells | 2019 | Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7 | Novel multi-target directed ligands based on annelated xanthine scaffold with aromatic substituents acting on adenosine receptor and monoamine oxidase B. Synthesis, in vitro and in silico studies. |
| AID1248357 | Selectivity ratio of Ki for Adenosine A1 receptor in Lister hooded rat brain membranes to Ki for Adenosine A2A receptor in Lister hooded rat brain membranes | 2015 | Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20 | 1,3,7-Triethyl-substituted xanthines--possess nanomolar affinity for the adenosine A1 receptor. |
| AID1056827 | Induction of mAB-CD3-mediated IFN-gamma production in CGS-21680-treated C57/BL6 mouse lymphocytes at 0.5 uM after 24 hrs by ELISA | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 | Design and evaluation of xanthine based adenosine receptor antagonists: potential hypoxia targeted immunotherapies. |
| AID569670 | Efflux ratio of permeability from apical to basolateral over basolateral to apical side in human Caco2 cells after 21 to 28 days by LC-MS/MS analysis | 2011 | Journal of medicinal chemistry, Feb-10, Volume: 54, Issue:3 | Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} ester (Lu AA47070): a phosphonooxymethylene prodrug of a potent and selective hA(2A) receptor antagonist. |
| AID412515 | Reversal of haloperidol-induced hypolocomotion in TO mouse assessed as time spent for locomotor activity at 0.3 mg/kg, po administered 15 mins prior to testing done for 60 mins | 2009 | Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1 | Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines. |
| AID424234 | Reversal of haloperidol-induced locomotor movement deficit in po dosed mouse assessed as minimum effective dose administered 15 mins before haloperidol challenge | 2009 | Bioorganic & medicinal chemistry letters, May-15, Volume: 19, Issue:10 | Antagonists of the human A(2A) receptor. Part 5: Highly bio-available pyrimidine-4-carboxamides. |
| AID569668 | Intrinsic clearance in rat liver microsomes at 1 uM after 60 mins by LC-MS/MS analysis | 2011 | Journal of medicinal chemistry, Feb-10, Volume: 54, Issue:3 | Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} ester (Lu AA47070): a phosphonooxymethylene prodrug of a potent and selective hA(2A) receptor antagonist. |
| AID1639022 | Displacement of [3H]MSX2 from recombinant human adenosine A2a receptor expressed in HEK293 cells | 2019 | Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7 | Novel multi-target directed ligands based on annelated xanthine scaffold with aromatic substituents acting on adenosine receptor and monoamine oxidase B. Synthesis, in vitro and in silico studies. |
| AID607232 | Inverse agonist activity at human adenosine receptor A2a S277A'7.42 mutant expressed in HEK293 cells followed by receptor capturing on Biocore chips assessed as log difference in receptor affinity by SPR method relative to wild type stabilized A2A recepto | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Biophysical mapping of the adenosine A2A receptor. |
| AID1193096 | Antagonist activity at human adenosine A1 receptor | 2015 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6 | Synthesis and SAR studies of analogues of 4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-N-thiazol-2-yl-benzamide (Lu AA41063) as adenosine A2A receptor ligands with improved aqueous solubility. |
| AID536329 | Reversal of haloperidol-induced catalepsy in BALB/c mouse at 1 mg/kg, po administered 30 mins after haloperidol challenge measured for 60 seconds after 4 hrs | 2010 | Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22 | In vivo characterization of a dual adenosine A2A/A1 receptor antagonist in animal models of Parkinson's disease. |
| AID569669 | Apparent permeability across human Caco2 cell membrane after 21 to 28 days by LC-MS/MS analysis | 2011 | Journal of medicinal chemistry, Feb-10, Volume: 54, Issue:3 | Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} ester (Lu AA47070): a phosphonooxymethylene prodrug of a potent and selective hA(2A) receptor antagonist. |
| AID1816612 | Reversal of haloperidol-induced catalepsy in GPR6 knock out mouse assessed as reduction in catalepsy at 0.3 mg/kg, ip measured after 120 min | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14 | First-Time Disclosure of CVN424, a Potent and Selective GPR6 Inverse Agonist for the Treatment of Parkinson's Disease: Discovery, Pharmacological Validation, and Identification of a Clinical Candidate. |
| AID1412904 | Binding affinity to human adenosine A2A receptor by radioligand displacement assay | 2018 | MedChemComm, Jun-01, Volume: 9, Issue:6 | Tricyclic xanthine derivatives containing a basic substituent: adenosine receptor affinity and drug-related properties. |
| AID1696176 | Inhibition of human adenosine 2B receptor | |||
| 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. |
| AID1412903 | Binding affinity to human adenosine A1 receptor by radioligand displacement assay | 2018 | MedChemComm, Jun-01, Volume: 9, Issue:6 | Tricyclic xanthine derivatives containing a basic substituent: adenosine receptor affinity and drug-related properties. |
| AID255370 | Selective binding affinity towards human Adenosine A1 receptor expressed in CHO cells using [3H]DPCPX compared to human Adenosine A2a receptor expressed in HEK293 cells using [3H]-CGS-21,680 | 2005 | Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22 | 2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization. |
| AID1854970 | Displacement of [3H]ZM241385 from human adenosine A2A receptor expressed in HEK293 cell membrane incubated for 1 hr by microplate beta scintillation counting based radioligand inhibition assay | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | High ligand efficiency quinazoline compounds as novel A |
| AID723214 | Displacement of [3H]ZM241385 from human adenosine A2A receptor expressed in HEK293 cells after 1 hr by microbeta scintillation counting analysis | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Synthesis of (E)-8-(3-chlorostyryl)caffeine analogues leading to 9-deazaxanthine derivatives as dual A(2A) antagonists/MAO-B inhibitors. |
| AID501542 | Displacement of [3H]ZM241385 from human adenosine A2A receptor expressed in buculovirus system by liquid scintillation counting | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17 | Hit-to-lead optimization of a series of carboxamides of ethyl 2-amino-4-phenylthiazole-5-carboxylates as novel adenosine A2A receptor antagonists. |
| AID501540 | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells by liquid scintillation counting | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17 | Hit-to-lead optimization of a series of carboxamides of ethyl 2-amino-4-phenylthiazole-5-carboxylates as novel adenosine A2A receptor antagonists. |
| AID254542 | Binding affinity towards human Adenosine A2a receptor expressed in HEK293 cells using 6 nM [3H]CGS-21680 | 2005 | Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22 | 2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization. |
| AID1816613 | Reversal of haloperidol-induced catalepsy in C57BL/6 mouse assessed as reduction in catalepsy at 0.3 mg/kg, ip measured after 120 min | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14 | First-Time Disclosure of CVN424, a Potent and Selective GPR6 Inverse Agonist for the Treatment of Parkinson's Disease: Discovery, Pharmacological Validation, and Identification of a Clinical Candidate. |
| AID607199 | Binding affinity at stabilized human adenosine receptor A2a L85A'3.33 mutant expressed in HEK293 cells followed by receptor capturing on Biocore chips assessed as log difference in receptor affinity by SPR method relative to wild type stabilized A2A recep | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Biophysical mapping of the adenosine A2A receptor. |
| AID569664 | Displacement of [3H]-ZM241385 from human adenosine A2A receptor expressed in high five cells after 30 mins by scintillation counting | 2011 | Journal of medicinal chemistry, Feb-10, Volume: 54, Issue:3 | Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} ester (Lu AA47070): a phosphonooxymethylene prodrug of a potent and selective hA(2A) receptor antagonist. |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
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| AID1345618 | Human A2A receptor (Adenosine receptors) | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4 | 2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists. |
| AID1345690 | Rat A2A receptor (Adenosine receptors) | 2008 | Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18 | Dual inhibition of monoamine oxidase B and antagonism of the adenosine A(2A) receptor by (E,E)-8-(4-phenylbutadien-1-yl)caffeine analogues. |
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| AID1345685 | Human A1 receptor (Adenosine receptors) | 2011 | Pharmacological reviews, Mar, Volume: 63, Issue:1 | International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and classification of adenosine receptors--an update. |
| AID1345630 | Rat A1 receptor (Adenosine receptors) | 2011 | Pharmacological reviews, Mar, Volume: 63, Issue:1 | International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and classification of adenosine receptors--an update. |
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| [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 | 4 (1.93) | 18.2507 |
| 2000's | 74 (35.75) | 29.6817 |
| 2010's | 89 (43.00) | 24.3611 |
| 2020's | 40 (19.32) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.
| This Compound (57.82) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 18 (8.49%) | 5.53% |
| Reviews | 40 (18.87%) | 6.00% |
| Case Studies | 5 (2.36%) | 4.05% |
| Observational | 1 (0.47%) | 0.25% |
| Other | 148 (69.81%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
|---|---|---|---|---|---|---|---|
| Acute Adenosine Receptor Antagonism to Promote Breathing Plasticity in ALS [NCT05377424] | Phase 1/Phase 2 | 40 participants (Anticipated) | Interventional | 2022-06-21 | Recruiting | ||
| Effect of Mild Hepatic Impairment (Child-Pugh Class A) on the Single-dose Pharmacokinetics of Istradefylline [NCT02256033] | Phase 1 | 20 participants (Actual) | Interventional | 2014-08-31 | Completed | ||
| Istradefylline Effect on Parkinson's Disease Tremor, Motor Symptoms and Non-motor Symptoms [NCT05885360] | Phase 4 | 27 participants (Actual) | Interventional | 2023-01-20 | Active, not recruiting | ||
| Effect of a Strong Enzyme Inducer, Rifampin, on the Single-Dose Pharmacokinetics of Istradefylline in Healthy Subjects [NCT02174250] | Phase 1 | 20 participants (Actual) | Interventional | 2014-06-30 | Completed | ||
| A Selective Adenosine 2a Antagonist to Enhance Training-related Gains in Walking Function for Persons With Chronic, Incomplete Spinal Cord Injury [NCT05217498] | Phase 1/Phase 2 | 40 participants (Anticipated) | Interventional | 2024-09-01 | Not yet recruiting | ||
| Placebo-Controlled, Double-Blind, Parallel Group, Fixed Dose Study of KW-6002 (Istradefylline) in the Treatment of Parkinson's Disease (Phase 3) [NCT00955526] | Phase 3 | 373 participants (Actual) | Interventional | 2009-07-31 | Completed | ||
| Long-Term Safety Study of KW-6002 (Istradefylline) in the Treatment of Parkinson's Disease (Phase 3) [NCT00957203] | Phase 3 | 308 participants (Actual) | Interventional | 2009-10-31 | Completed | ||
| Istradefylline for Parkinson Disease Cognitive Impairment [NCT05333549] | Phase 2 | 10 participants (Anticipated) | Interventional | 2022-07-18 | Recruiting | ||
| A Double-Blind, Randomized, Placebo- and Active-Controlled Crossover Study to Evaluate the Abuse Potential of Istradefylline in Recreational Drug Users [NCT02609477] | Phase 1 | 42 participants (Actual) | Interventional | 2016-01-31 | Completed | ||
| A Long-Term, Multicenter, Open-Label, Safety Study With a Flexible Dose Range of KW-6002 as Treatment for Parkinson's Disease in Patients With Motor Response Complications on Levodopa/Carbidopa Therapy [NCT00955045] | Phase 2/Phase 3 | 0 participants | Interventional | 2002-08-31 | Completed | ||
| A Long-Term, Multicenter, Open-Label Safety Study With Oral 20 or 40 mg/d Doses of KW-6002 (Istradefylline) as Treatment for Parkinson's Disease in Patients With Motor Response Complications on Levodopa Therapy [NCT00203957] | Phase 3 | 10 participants (Actual) | Interventional | 2005-03-31 | Completed | ||
| Adenosine A2A Blockade With KW-6002 in Parkinson's Disease [NCT00006337] | Phase 2 | 16 participants | Interventional | 2000-10-31 | Completed | ||
| A Long-Term, Multicenter, Open-Label Safety Study With Oral 20 or 40 mg/d Doses of KW-6002 (Istradefylline) as Treatment for Parkinson's Disease in Patients With Motor Response Complications on Levodopa Therapy. [NCT00199368] | Phase 3 | 1,100 participants | Interventional | 2004-10-31 | Completed | ||
| A 12-week, Double Blind, Placebo-controlled, Randomized, Parallel Group, Multicenter, Fixed Dose Study to Evaluate the Efficacy and Safety of a 20 mg/d Oral Dose of KW-6002 (Istradefylline) as Treatment for Parkinson's Disease in Patients With Motor Respo [NCT00199407] | Phase 3 | 230 participants | Interventional | 2004-06-30 | Completed | ||
| A Phase 2, Double-blind, Placebo-controlled, Randomized, Parallel-Group, Multicenter Study to Evaluate the Efficacy and Safety of 40mg/Day KW-6002 (Istradefylline) in Subjects With Restless Legs Syndrome [NCT00199446] | Phase 2 | 160 participants | Interventional | 2005-07-31 | Completed | ||
| Placebo-controlled, Double-blind, Parallel Group, Fixed Dose Study of KW-6002 (Istradefylline) in the Treatment of Parkinson's Disease (Phase 2 Study) [NCT00455507] | Phase 2 | 363 participants (Actual) | Interventional | 2007-03-31 | Completed | ||
| A 12-Week, Double-Blind, Placebo-Controlled, Randomized, Multicenter Study of the Efficacy of Doses of 20 and 60 mg/Day Istradefylline as Treatment for Parkinson's Disease in Patients With Motor Response Complications on Levodopa/Carbidopa [NCT00456794] | Phase 2 | 325 participants | Interventional | 2002-03-31 | Completed | ||
| Placebo-Controlled , Crossover , Double-Blind Study of KW-6002(Istradefylline) in the Treatment of Parkinson's Disease. [Monotherapy] [NCT00250393] | Phase 2 | 64 participants | Interventional | 2005-11-30 | Completed | ||
| Effect of Istradefylline Treatment on Behavioral Measures of Apathy in Parkinson's Disease. [NCT05182151] | 8 participants (Anticipated) | Observational | 2022-07-29 | Active, not recruiting | |||
| A 12-Week, Double-Blind, Placebo-Controlled, Randomized, Multicenter Study of the Efficacy of 40 mg/Day KW-6002 as Treatment for Parkinson's Disease in Patients With Motor Response Complications on Levodopa/Carbidopa Therapy [NCT00456586] | Phase 2 | 180 participants | Interventional | 2002-04-30 | Completed | ||
| A 12-week, Double Blind, Placebo-controlled, Randomized, Parallel Group, Multicenter, Fixed Dose Study to Evaluate the Efficacy and Safety of 10, 20 and 40 mg/d Oral Dose of KW-6002 (Istradefylline) as Treatment for Parkinson's Disease in Patients With Mo [NCT00199420] | Phase 3 | 580 participants | Interventional | 2004-07-31 | Completed | ||
| An Open-Label Multicenter Study of the Continued Safety of Istradefylline (KW-6002) In Subjects With Parkinson's Disease Who Have Recently Completed One Year of Treatment With Istradefylline. [NCT00199381] | Phase 3 | 504 participants (Actual) | Interventional | 2005-10-31 | Terminated(stopped due to Additional long-term safety data no longer needed) | ||
| Placebo-Controlled , Double-Blind , Exploratory Study of KW-6002(Istradefylline) in the Treatment of Parkinson's Disease. [Adjunctive Therapy to Levodopa] [NCT00199355] | Phase 2 | 75 participants | Interventional | 2005-04-30 | Completed | ||
| A 16-week, Double-Blind, Placebo-Controlled, Randomised, Parallel-Group, Multicentre, International Study to Evaluate the Efficacy and Safety of 40 mg/Day KW-6002 (Istradefylline) and That of Entacapone Versus Placebo as Treatment for Parkinson's Disease [NCT00199394] | Phase 3 | 405 participants | Interventional | 2004-11-30 | Completed | ||
| A Phase 2, Double-blind, Placebo-controlled, Randomized, Parallel-Group, Multicenter Study to Evaluate the Efficacy and Safety of 40mg/Day KW-6002 (Istradefylline) as Monotherapy in Subjects With Parkinson's Disease [NCT00199433] | Phase 2 | 160 participants | Interventional | 2005-05-31 | Completed | ||
| A Phase 3, Long-term, Open-label Study of Istradefylline in Subjects With Moderate to Severe Parkinson's Disease [NCT02610231] | Phase 3 | 239 participants (Actual) | Interventional | 2015-12-31 | Completed | ||
| A Phase 3, 12-week, Double-Blind, Placebo-Controlled, Randomized, Multicenter Study to Evaluate the Efficacy of Oral Istradefylline 20 and 40 mg/Day as Treatment for Subjects With Moderate to Severe Parkinson's Disease [NCT01968031] | Phase 3 | 613 participants (Actual) | Interventional | 2013-10-31 | Completed | ||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||