Page last updated: 2024-08-21

pyrazines and as 3201

pyrazines has been researched along with as 3201 in 28 studies

Research

Studies (28)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's1 (3.57)18.2507
2000's17 (60.71)29.6817
2010's9 (32.14)24.3611
2020's1 (3.57)2.80

Authors

AuthorsStudies
Fujitani, B; Komiya, M; Kuromiya, A; Matsumoto, J; Murata, M; Negoro, T; Ono, Y; Suzuki, K; Ueda, S1
Fujiwara, I; Kurono, M; Yoshida, K1
Fujii, T; Kamataki, T; Terauchi, Y; Toide, K; Yamazaki, H1
Bril, V; Buchanan, RA2
Nakamura, J1
Hotta, N1
Fujii, A; Fujitani, B; Kurono, M; Murata, M; Negoro, T1
Giannoukakis, N3
Itogawa, A; Kurono, M; Noguchi, H; Sanjoba, M1
Fujiwara, Y; Hara, K; Kumagai, N; Mashiko, T; Shibasaki, M; Tanaka, D1
Kumagai, N; Mashiko, T; Shibasaki, M2
Bril, V; Kuromiya, A; Matsumoto, T; Ono, Y; Toyosawa, K; Ueda, Y1
Bril, V; Kuromiya, A; Kurono, M; Matsumoto, T; Nakamura, K; Ono, Y2
Bril, V; Buchanan, R; Hirose, T; Tomioka, S1
Dong, G; Osipov, M; Trost, BM1
Kakehashi, A; Kinoshita, N; Matsumoto, T; Ota, A; Shimmura, M; Takano, H; Tanaka, Y; Toyoda, F; Tsuji, J1
Arezzo, J; Bradshaw, KL; Bril, V; Gordon, RJ; Junor, RW; Nash, M; Polydefkis, M; Shaibani, A1
Kohara, N; Satoh, J; Sekiguchi, K; Yamaguchi, Y1
Atsumi, T; Ishizu, A; Kusunoki, Y; Miyoshi, A; Miyoshi, H; Nakamura, A; Nakazawa, D; Shida, H; Tomaru, U; Yamada, M1
Ishibashi, Y; Kato, H; Matsui, T; Matsumoto, T; Yamagishi, S1
Baba, M; Hamatani, T; Imai, T; Kohara, N; Komori, T; Naito, Y; Satoh, J; Sekiguchi, K; Yamaguchi, Y1
Kita, S; Tsuzaki, K; Yamamura, ET1
Fujita, T; Inoue, K; Ishii, D; Itou, M; Kakuyama, H; Takagaki, T; Uchida, N1

Reviews

6 review(s) available for pyrazines and as 3201

ArticleYear
[Role of polyol pathway in pathogenesis of diabetic microangiopathy].
    Nihon rinsho. Japanese journal of clinical medicine, 2005, Volume: 63 Suppl 6

    Topics: Aldehyde Reductase; Animals; Diabetic Angiopathies; Fructose; Glucose; Glycation End Products, Advanced; Humans; L-Iditol 2-Dehydrogenase; Oxidative Stress; Polymers; Polymorphism, Genetic; Protein Kinase C; Pyrazines; Sorbitol; Spiro Compounds

2005
[Progress on the drug therapy for diabetic microangiopathies: aldose reductase inhibitor].
    Nihon rinsho. Japanese journal of clinical medicine, 2005, Volume: 63 Suppl 6

    Topics: Aldehyde Reductase; Animals; Clinical Trials as Topic; Diabetic Angiopathies; Drug Design; Humans; Imidazolidines; Polymers; Polymorphism, Genetic; Pyrazines; Rhodanine; Spiro Compounds; Thiazolidines

2005
Drug evaluation: ranirestat--an aldose reductase inhibitor for the potential treatment of diabetic complications.
    Current opinion in investigational drugs (London, England : 2000), 2006, Volume: 7, Issue:10

    Topics: Aldehyde Reductase; Animals; Clinical Trials, Phase II as Topic; Clinical Trials, Phase III as Topic; Contraindications; Diabetes Complications; Drug Evaluation, Preclinical; Enzyme Inhibitors; Humans; Pyrazines; Spiro Compounds; Structure-Activity Relationship

2006
Ranirestat as a therapeutic aldose reductase inhibitor for diabetic complications.
    Expert opinion on investigational drugs, 2008, Volume: 17, Issue:4

    Topics: Aldehyde Reductase; Animals; Clinical Trials as Topic; Diabetes Complications; Diabetes Mellitus; Enzyme Inhibitors; Humans; Pyrazines; Sorbitol; Spiro Compounds; Treatment Outcome

2008
Inventing and understanding catalytic, enantioselective reactions.
    Current opinion in drug discovery & development, 2009, Volume: 12, Issue:6

    Topics: Aldehyde Reductase; Amination; Catalysis; Chemistry, Pharmaceutical; Dipeptidyl-Peptidase IV Inhibitors; Enzyme Inhibitors; Hydrogenation; Hypoglycemic Agents; Models, Chemical; Molecular Structure; Pyrazines; Sitagliptin Phosphate; Spiro Compounds; Stereoisomerism; Triazoles

2009
Evaluation of ranirestat for the treatment of diabetic neuropathy.
    Expert opinion on drug metabolism & toxicology, 2014, Volume: 10, Issue:7

    Topics: Aldehyde Reductase; Animals; Biomarkers; Clinical Trials as Topic; Diabetic Neuropathies; Drug Evaluation, Preclinical; Enzyme Inhibitors; Humans; Mice; Pyrazines; Rats; Reproducibility of Results; Spiro Compounds

2014

Trials

7 trial(s) available for pyrazines and as 3201

ArticleYear
Aldose reductase inhibition by AS-3201 in sural nerve from patients with diabetic sensorimotor polyneuropathy.
    Diabetes care, 2004, Volume: 27, Issue:10

    Topics: Adolescent; Adult; Aged; Aldehyde Reductase; Diabetes Mellitus, Type 1; Diabetes Mellitus, Type 2; Diabetic Neuropathies; Dose-Response Relationship, Drug; Double-Blind Method; Drug Administration Schedule; Electromyography; Female; Follow-Up Studies; Humans; Male; Middle Aged; Neural Conduction; Polyneuropathies; Probability; Pyrazines; Reference Values; Risk Assessment; Severity of Illness Index; Spiro Compounds; Sural Nerve; Treatment Outcome

2004
Long-term effects of ranirestat (AS-3201) on peripheral nerve function in patients with diabetic sensorimotor polyneuropathy.
    Diabetes care, 2006, Volume: 29, Issue:1

    Topics: Aldehyde Reductase; Blood Glucose; Diabetes Mellitus, Type 1; Diabetes Mellitus, Type 2; Diabetic Neuropathies; Double-Blind Method; Enzyme Inhibitors; Glycated Hemoglobin; Humans; Motor Neurons; Neural Conduction; Patient Selection; Peripheral Nerves; Peroneal Nerve; Placebos; Pyrazines; Spiro Compounds; Sural Nerve

2006
Ranirestat for the management of diabetic sensorimotor polyneuropathy.
    Diabetes care, 2009, Volume: 32, Issue:7

    Topics: Adolescent; Adult; Aged; Aldehyde Reductase; Diabetes Mellitus, Type 1; Diabetes Mellitus, Type 2; Diabetic Neuropathies; Dose-Response Relationship, Drug; Double-Blind Method; Humans; Median Nerve; Middle Aged; Motor Neurons; Neural Conduction; Placebos; Pyrazines; Sensory Thresholds; Spiro Compounds; Sural Nerve; Young Adult

2009
Safety and efficacy of ranirestat in patients with mild-to-moderate diabetic sensorimotor polyneuropathy.
    Journal of the peripheral nervous system : JPNS, 2015, Volume: 20, Issue:4

    Topics: Aged; Diabetic Neuropathies; Disease Progression; Double-Blind Method; Female; Humans; Male; Middle Aged; Neural Conduction; Polyneuropathies; Pyrazines; Quality of Life; Spiro Compounds; Treatment Outcome

2015
Effect of Ranirestat on Sensory and Motor Nerve Function in Japanese Patients with Diabetic Polyneuropathy: A Randomized Double-Blind Placebo-Controlled Study.
    Journal of diabetes research, 2016, Volume: 2016

    Topics: Administration, Oral; Aged; Aldehyde Reductase; Diabetes Mellitus, Type 1; Diabetes Mellitus, Type 2; Diabetic Neuropathies; Disease Progression; Double-Blind Method; Enzyme Inhibitors; Female; Humans; Japan; Kidney Function Tests; Liver Function Tests; Male; Middle Aged; Motor Neurons; Neural Conduction; Pyrazines; Sensory Receptor Cells; Severity of Illness Index; Spiro Compounds; Temperature

2016
Aldose reductase inhibitor ranirestat significantly improves nerve conduction velocity in diabetic polyneuropathy: A randomized double-blind placebo-controlled study in Japan.
    Journal of diabetes investigation, 2019, Volume: 10, Issue:2

    Topics: Adult; Aged; Aldehyde Reductase; Diabetic Neuropathies; Double-Blind Method; Enzyme Inhibitors; Female; Follow-Up Studies; Humans; Japan; Male; Middle Aged; Neural Conduction; Prognosis; Pyrazines; Quality of Life; Spiro Compounds; Young Adult

2019
Pharmacokinetics and Safety of Ranirestat in Patients With Hepatic Impairment.
    Journal of clinical pharmacology, 2020, Volume: 60, Issue:10

    Topics: Adult; Aged; Area Under Curve; Diabetic Neuropathies; Enzyme Inhibitors; Female; Healthy Volunteers; Humans; Liver Diseases; Male; Middle Aged; Protein Binding; Pyrazines; Spiro Compounds

2020

Other Studies

15 other study(ies) available for pyrazines and as 3201

ArticleYear
Novel, highly potent aldose reductase inhibitors: (R)-(-)-2-(4-bromo-2-fluorobenzyl)-1,2,3,4- tetrahydropyrrolo[1,2-a]pyrazine -4-spiro-3'-pyrrolidine-1,2',3,5'-tetrone (AS-3201) and its congeners.
    Journal of medicinal chemistry, 1998, Oct-08, Volume: 41, Issue:21

    Topics: Aldehyde Reductase; Animals; Crystallography, X-Ray; Diabetes Mellitus, Experimental; Enzyme Inhibitors; In Vitro Techniques; Lens, Crystalline; Male; Molecular Conformation; Pyrazines; Rats; Rats, Wistar; Sciatic Nerve; Sorbitol; Spiro Compounds; Stereoisomerism; Structure-Activity Relationship; Swine

1998
Stereospecific interaction of a novel spirosuccinimide type aldose reductase inhibitor, AS-3201, with aldose reductase.
    Biochemistry, 2001, Jul-27, Volume: 40, Issue:28

    Topics: Aldehyde Reductase; Binding Sites; Bromosuccinimide; Enzyme Inhibitors; Enzyme Stability; Fluorine; Holoenzymes; Humans; Hydrogen-Ion Concentration; Kinetics; Ligands; Models, Molecular; Nuclear Magnetic Resonance, Biomolecular; Pyrazines; Spectrometry, Fluorescence; Spiro Compounds; Stereoisomerism; Substrate Specificity; Succinimides; Temperature; Titrimetry

2001
Uridine diphosphate sugar-selective conjugation of an aldose reductase inhibitor (AS-3201) by UDP-glucuronosyltransferase 2B subfamily in human liver microsomes.
    Biochemical pharmacology, 2004, Apr-01, Volume: 67, Issue:7

    Topics: Aldehyde Reductase; Glucuronosyltransferase; Humans; Isoenzymes; Microsomes, Liver; Pyrazines; Recombinant Proteins; Spiro Compounds; Uridine Diphosphate Glucose

2004
Stereospecific recognition of a spirosuccinimide type aldose reductase inhibitor (AS-3201) by plasma proteins: a significant role of specific binding by serum albumin in the improved potency and stability.
    Biochemical pharmacology, 2006, Jan-12, Volume: 71, Issue:3

    Topics: Aldehyde Reductase; Animals; Binding, Competitive; Blood Proteins; Enzyme Inhibitors; Fatty Acids, Nonesterified; Humans; Hydrogen-Ion Concentration; Hydrolysis; In Vitro Techniques; Kinetics; Ligands; Molecular Structure; Nuclear Magnetic Resonance, Biomolecular; Organ Specificity; Protein Binding; Pyrazines; Rats; Serum Albumin; Spectrometry, Fluorescence; Spiro Compounds; Stereoisomerism; Temperature; Tissue Distribution

2006
Stability and hydrolysis kinetics of spirosuccinimide type inhibitors of aldose reductase in aqueous solution and retardation of their hydrolysis by the target enzyme.
    Journal of pharmaceutical sciences, 2008, Volume: 97, Issue:4

    Topics: Aldehyde Reductase; Diabetes Complications; Drug Stability; Enzyme Inhibitors; Hydrogen-Ion Concentration; Hydrolysis; Kinetics; Osmolar Concentration; Pyrazines; Solutions; Spiro Compounds

2008
En route to an efficient catalytic asymmetric synthesis of AS-3201.
    Journal of the American Chemical Society, 2007, Sep-19, Volume: 129, Issue:37

    Topics: Aldehyde Reductase; Amination; Catalysis; Hypoglycemic Agents; Molecular Structure; Pyrazines; Spiro Compounds

2007
An improved lanthanum catalyst system for asymmetric amination: toward a practical asymmetric synthesis of AS-3201 (Ranirestat).
    Organic letters, 2008, Jul-03, Volume: 10, Issue:13

    Topics: Amination; Catalysis; Lanthanum; Molecular Structure; Pyrazines; Spectrometry, Mass, Electrospray Ionization; Spiro Compounds; Stereoisomerism

2008
Long-term treatment with ranirestat (AS-3201), a potent aldose reductase inhibitor, suppresses diabetic neuropathy and cataract formation in rats.
    Journal of pharmacological sciences, 2008, Volume: 107, Issue:3

    Topics: Aldehyde Reductase; Animals; Cataract; Diabetic Neuropathies; Enzyme Inhibitors; Pyrazines; Rats; Spiro Compounds

2008
Ranirestat (AS-3201), a potent aldose reductase inhibitor, reduces sorbitol levels and improves motor nerve conduction velocity in streptozotocin-diabetic rats.
    Journal of pharmacological sciences, 2008, Volume: 107, Issue:3

    Topics: Aldehyde Reductase; Animals; Diabetes Mellitus; Diabetic Neuropathies; Enzyme Inhibitors; Male; Neural Conduction; Pyrazines; Rats; Rats, Wistar; Sorbitol; Spiro Compounds; Streptozocin

2008
Improvement of motor nerve conduction velocity in diabetic rats requires normalization of the polyol pathway metabolites flux.
    Journal of pharmacological sciences, 2009, Volume: 109, Issue:2

    Topics: Aldehyde Reductase; Animals; Diabetes Mellitus, Experimental; Erythrocytes; Fructose; In Vitro Techniques; Male; Neural Conduction; Pyrazines; Rats; Rats, Wistar; Sciatic Nerve; Sorbitol; Spiro Compounds

2009
A concise enantioselective synthesis of (-)-ranirestat.
    Organic letters, 2010, Mar-19, Volume: 12, Issue:6

    Topics: Aldehyde Reductase; Molecular Structure; Pyrazines; Spiro Compounds; Stereoisomerism

2010
Effect of ranirestat, a new aldose reductase inhibitor, on diabetic retinopathy in SDT rats.
    Journal of diabetes research, 2014, Volume: 2014

    Topics: Administration, Oral; Aldehyde Reductase; Animals; Blood Glucose; Body Weight; Diabetic Retinopathy; Disease Models, Animal; Drug Administration Schedule; Enzyme Inhibitors; Glial Fibrillary Acidic Protein; Glycated Hemoglobin; Male; Neuroprotective Agents; Pyrazines; Rats; Rats, Sprague-Dawley; Retina; Rhodanine; Spiro Compounds; Thiazolidines; Time Factors

2014
Circulating Neutrophil Extracellular Trap Levels in Well-Controlled Type 2 Diabetes and Pathway Involved in Their Formation Induced by High-Dose Glucose.
    Pathobiology : journal of immunopathology, molecular and cellular biology, 2016, Volume: 83, Issue:5

    Topics: Adult; Aged; Aged, 80 and over; Biomarkers; Case-Control Studies; Diabetes Mellitus, Type 2; Diabetic Angiopathies; DNA; Dose-Response Relationship, Drug; Extracellular Traps; Glucose; Humans; Hypoglycemic Agents; Middle Aged; Neutrophils; Peroxidase; Polymers; Pyrazines; Pyrroles; Quinazolines; Risk Factors; Spiro Compounds; Time Factors

2016
Ranirestat has a stronger inhibitory activity on aldose reductase and suppresses inflammatory reactions in high glucose-exposed endothelial cells.
    Diabetes & vascular disease research, 2016, Volume: 13, Issue:4

    Topics: Aldehyde Reductase; Anti-Inflammatory Agents; Cell Line, Tumor; Chromatography, Liquid; Dose-Response Relationship, Drug; Enzyme Inhibitors; Glucose; Human Umbilical Vein Endothelial Cells; Humans; Inflammation; Inflammation Mediators; Pyrazines; Reverse Transcriptase Polymerase Chain Reaction; Rhodanine; Sorbitol; Spiro Compounds; Superoxides; Tandem Mass Spectrometry; Thiazolidines; Vascular Cell Adhesion Molecule-1

2016
A novel method of producing the key intermediate ASI-2 of ranirestat using a porcine liver esterase (PLE) substitute enzyme.
    Bioscience, biotechnology, and biochemistry, 2019, Volume: 83, Issue:6

    Topics: Amino Acid Sequence; Animals; Bacillus thuringiensis; Bacterial Proteins; Base Sequence; Electrophoresis, Polyacrylamide Gel; Enzyme Inhibitors; Escherichia coli; Esterases; Hydrolysis; Liver; Pyrazines; Recombinant Proteins; Spiro Compounds; Swine

2019