Binding of 1-(2-Ethoxyethyl)-2-(hexahydro-4-methyl-1,4-diazepin-1-yl) benzimidazole Difumarate (KG-2413) to Serum or Plasma Proteins in Man, Guinea Pig and Rat
スポンサーリンク
概要
- 論文の詳細を見る
Human, guinea pig and rat sera or plasma protein binding of 1-(2-ethoxyethyl)-2-(hexahydro-4-methyl-1,4-diazepin-1-yl) benzimidazole difumarate (KG-2413) were investigated by equilibrium dialysis. There were pronounced interspecies differences in binding affinity and binding capacity which were the highest in guinea pig and human species, respectively. In humans, the binding index (n_1P_1/Kd_1) of isolated α_1-acid glycoprotein (α_1-AG) was seven times higher than that of isolated albumin, and the dissociation constant for human serum at the high affinity binding site was comparable to that for α_1-AG. These facts suggested that the free base of KG-2413 was mainly bound to α_1-AG in human serum. The contribution of albumin to the binding of KG-2413 in guinea pig and rat plasma may be relatively small. The interspecies differences in KG-2413 binding observed in this study may be due to species differences in the binding affinity and/or capacity of α_1-AG.
- 社団法人日本薬学会の論文
著者
-
WATANABE Jun
Department of Cardiovascular Medicine, Tohoku University Graduate School of Medicine
-
Awata N
Kanebo Ltd. Osaka Jpn
-
AWATA Norio
Pharmaceuticals Research Center, Kanebo, Ltd.,
-
Awata Norio
Product R & D Laboratories Pharmaceuticals Research Center
-
Awata Norio
Pharmaceuticals Research Center Kanebo Ltd.
-
Hamada T
National Inst. Agrobiological Resources Tsukuba Jpn
-
Sakai T
Pharmaceuticals Research Center Kanebo Ltd. :department Of Biopharmaceutics Faculty Of Pharmaceutica
-
Sakai Takanori
Product R & D Laboratories Pharmaceuticals Research Center
-
Watanabe J
Department Of Pharmaceutics College Of Pharmacy Nihon University
-
Hamada T
Pharmacology And Molecular Biology Research Laboratories Sankyo Co. Ltd.
-
SAKAI Takeshi
Kobe Pharmaceutical University
-
Sakai T
Kobe Pharmaceutical University
-
Watanabe Jun
Department Of Anatomy & Cell Science Kansai Medical University
関連論文
- Incidence and Characteristics of Ventricular Fibrillation in Bystander-witnessed Out-of-hospital Cardiac Arrest with Cardiac Etiology in the City of Sendai, Japan
- Estimated Incidence of Ventricular Tachycardia/Fibrillation (VT/VF) in out-of Hospital Cardiac Arrest (OHCA) with Cardiac Etiologies (Preventive Medicine/Epidemiology/Education/Health Policy 5 (H), The 69th Annual Scientific Meeting of the Japanese Circul
- Incidence of Ventricular Fibrillation in out-of Hospital Cardiac Arrest (OHCA) Depends on Age and Time of Day (Preventive Medicine/Epidemiology/Education/Health Policy 5 (H), The 69th Annual Scientific Meeting of the Japanese Circulation Society)
- Poor Prognosis of Japanese Patients With Chronic Heart Failure Following Myocardial Infarction : Comparison With Nonischemic Cardiomyopathy
- Analysis of Chronic Heart Failure Registry in the Tohoku District : Third Year Follow-up
- Characterization of antioxidant protection of cultured neural progenitor cells (NPC) against methylmercury (MeHg) toxicity
- Estimated Incidence of Ventricular Tachycardia/Fibrillation (VT/VF) in out-of Hospital Cardiac Arrest (OHCA) with Cardiac Etiologies (Preventive Medicine/Epidemiology/Education/Health Policy 5 (H), The 69th Annual Scientific Meeting of the Japanese Circul
- Circadian variation of vascular endotherial function - correalation with neurohormonal agents
- Binding of 1-(2-Ethoxyethyl)-2-(hexahydro-4-methyl-1,4-diazepin-1-yl) benzimidazole Difumarate (KG-2413) to Serum or Plasma Proteins in Man, Guinea Pig and Rat
- Utility of extracorporeal traction with nylon thread for easier vesicourethral anastomosis in laparoscopic prostatectomy
- Diabetes mellitus accelerates left ventricular diastolic dysfunction through activation of the renin-angiotensin system in hypertensive rats
- PJ-171 Pravastatin Ameliorates Hypoxia-Induced Pulmonary Arterial Hypertension Through Down-regulation of Stromal Cell-Derived Factor-1 in Mice(Pulmonary circulation(03)(H),Poster Session(Japanese),The 72nd Annual Scientific Meeting of the Japanese Circul
- Prognostic Importance of Chronic Kidney Disease in Japanese Patients With Chronic Heart Failure : Implications of the CHART Study
- PE-483 Prognostic Impact of Central Sleep Apnea in Patients with Chronic Heart Failure(Heart failure, clinical-9 (M) PE81,Poster Session (English),The 70th Anniversary Annual Scientific Meeting of the Japanese Circulation Society)
- OJ-385 End-tidal Carbon Dioxide Predicts the Responsiveness of Patients with Chronic Heart Failure Associated with Central Sleep Apnea to Oxygen Therapy(Heart failure, clinical-6 (M) OJ65,Oral Presentation (Japanese),The 70th Anniversary Annual Scientific
- OJ-247 Chronic Hypoxia Mobilizes Smooth Muscle Progenitors in Mice(Vascular smooth muscles-1 (H) OJ42,Oral Presentation (Japanese),The 70th Anniversary Annual Scientific Meeting of the Japanese Circulation Society)
- OJ-103 Therapeutic Importance of Angiotensin-Converting Enzyme Inhibitor and/or Angiotensin Receptor Blocker in Patients with Diastolic Heart Failure(Heart failure, clinical-4 (M) OJ18,Oral Presentation (Japanese),The 70th Anniversary Annual Scientific Me
- OE-168 Hemoglobin Level Predicts Sudden Death in Patients with Diastolic Heart Failure(Heart failure, clinical-1 (M) OE28,Oral Presentation (English),The 70th Anniversary Annual Scientific Meeting of the Japanese Circulation Society)
- 1 Accumulated Risks and Non-Optimum Medical Treatment in Japanese Older Patients with Chronic Heart Failure : Results from the CHART Study(Characteristics and Management Strategies of Chronic Heart Failure in the Japanese,Symposium 12 (SY12) (M),The 70th
- Portopulmonary Hypertension : Hemodynamics, Pulmonary Angiography, and Configuration of the Heart
- Monophasic Action Potential Duration at the Crista Terminalis in Patients With Sinus Node Disease
- Effect of Nifekalant, a Class III Anti-Arrhythmic Agent, on Ca^ Waves in Rat Intact Trabeculae
- Inotropic Effect of Nifekalant on Monocrotaline-indeced Hypertrophied and Failing Rat Hearts (Cardiovascular Pharmacology, Basic/Clinical 3 (H), The 69th Annual Scientific Meeting of the Japanese Circulation Society)
- Pravastatin Ameliorate Hypoxia-Induced Pulmonary Hypertension by Suppression of Matrix Metalloproteinase-9 (Pulmonary Circulation 4 (H), The 69th Annual Scientific Meeting of the Japanese Circulation Society)
- Characteristics and Risks of Cardiac Events in Elderly Patients with Symptomatic Chronic Heart Failure : Implications from the CHART Study (Heart Failure, Clinical 12 (M), The 69th Annual Scientific Meeting of the Japanese Circulation Society)
- Local Ca^ Overload Causes Cardiac Nonuniformity and Initiates Ca^ Waves : Role of Ca^ Dissociated from Myofilaments (Excitation-contraction Coupling/Ion Channel 2 (A), The 69th Annual Scientific Meeting of the Japanese Circulation Society)
- Similarity of Delta-like Wave of Idiopathic Left Ventricular Tachyarrhythmia Arising from Mitral Annulus to Full-preexcited Delta Wave of WPW syndrome (Arrhythmia, Diagnosis/Pathophysiology/EPS 8 (A), The 69th Annual Scientific Meeting of the Japanese Cir
- Micropapillary bladder cancer
- Effects of sextant transrectal prostate biopsy plus additional far lateral cores in improving cancer detection rates in men with large prostate glands
- Effect of Maleylated Bovine Serum Albumin on the Disposition of Fractionated Heparin in Rats
- Uptake of FH by Two Types of Scavenger-Like Receptors in Rat Liver Parenchymal Cells in Primary Culture
- Uptake of Fractionated Heparin by Two Types of Scavenger Receptors in Isolated Rat Kupffer Cells
- Kinetic Characterization of Binding and Internalization of Fractionated [^3H]Heparin in Rat Liver Parenchymal Cells in Primary Culture
- Macromolecule-Macromolecule Interaction in Drug Distribution. V. Effects of Plasma Proteins on Uptake of Fractionated [^3H]Heparin in Isolated Rat Kupffer Cells
- Molecular Weight Dependency in the Uptake of Fractionated [^3H]Heparin in Isolated Rat Kupffer Cells
- Uptake Mechanism of Fractionated [^3H]Heparin in Isolated Rat Kupffer Cells : Involvement of Scavenger Receptors
- Macromolecule-Macromolecule Interaction in Drug Distribution. IV. Molecular Weight Dependency in the Interaction of Fractionated [^3H] Heparin with Plasma Proteins
- Inter-organ Relation between Salivary Gland and Kidney in Lithium Excretion. II. Salivary, Renal and Systemic Clearances of Lithium under Continuous Stimulation of Salivation in Water Loaded Dogs
- Investigation on Interaction of Fractionated ^3H-Heparin with Plasma Proteins by Gel Filtration Chromatography
- OE-089 Absence of Cardiac Involvement in Asymptomatic Patients with Pulmonary Sarcoidosis by Myocardial Delayed Enhanced MRI(X-ray/CT/MRI/DSA 1 (I) : OE11)(Oral Presentation (English))
- p53 and chemosensitivity in bladder cancer
- High throughput comparative genomic hybridization array analysis of multifocal urothelial cancers
- Oxidative Stress Evaluated by Urinary Excretion of 8-iso-Prostaglandin F_ Predicts Cardiac Death in Patients with Dilated Cardiomyopathy(Cardiomyopathy, Clinical 6 (M), The 69th Annual Scientific Meeting of the Japanese Circulation Society)
- Efficacy of Acute Inhalation of Nitric Oxide in Patients With Primary Pulmonary Hypertension Using Chronic Use of Continuous Epoprostenol Infusion
- PJ-572 Paroxysmal Atrial Fibrillation after Lung Surgery. : The Relation Between the Incidence of Paroxysmal Atrial Fibrillation and the Type of Lobectomy.(Arrhythmia, Basic and Diagnosis/Pathophysiology/EPS (A) : PJ96)(Poster Session (Japanese))
- Incidence and Characteristics of Pulmonary Thromboembolism in Japan 2000
- Coexisting clear cell adenocarcinoma and squamous cell carcinoma arising from ovarian endometriosis
- Androgen-Producing Ovarian Tumors : A Clinicopathological Study of 3 Cases
- Right Ventricular Systolic Function and the Manner of Transformation of the Right Ventricle in Patients With Dilated Cardiomyopathy
- Effects of Tachycardia on Regional Wall Motion in Acute Ischemic Canine Heart
- OE-249 Effects of changes in Coronary perfusion on Subendocardial contractility Assessed with the novel high-resolution Doppler method(Echo/Doppler 11 (I) : OE31)(Oral Presentation (English))
- Varieties of Right Ventricular Diastolic Function in Patients with Non-Obstructive Hypertrophic Cardiomyopathy
- Post-Endsystolic Active Shortening in the Non-Ischemic Region Impairs Left Ventricular Pressure Fall in Acute Ischemic Heart
- Unique Histopathological Features of a Familial Dilated Cardiomyopathy with Conduction Defect Caused by a Lamin A/C Gene Mutation
- Transglycosylation Activity of β-N-Acetylhexosaminidase from Penixillium pxalicum and Its Application to Synthesis of a Drug Carrier
- The Expression of Erythropoietin-receptor on Stem Cells might Play Crucial Roles in the Protection of Cardiac Muscle under Ischemic-or Hypoxic-condition(Myocardial Ischemia-reperfusion, Basic 2 (IHD), The 69th Annual Scientific Meeting of the Japanese Cir
- Mobilization and Accumulation of VEGFR2^+ Progenitor Cells around Pulmonary Vasculature in Patients with Primary Pulmonary Hypertension(Angiogenesis 5 (M), The 69th Annual Scientific Meeting of the Japanese Circulation Society)
- The Erythropoietin-Erythropoietin Receptor System is Crucial for Mobilization of Endothelial Progenitor Cells in Hypoxia-Induced Pulmonary Hypertension(Angiogenesis 3 (M), The 69th Annual Scientific Meeting of the Japanese Circulation Society)
- Circulating VEGFR2^+ Progenitor Cells Have Sub-populations Which Differentiate into Several Vascular Lineages in the Development of Hypoxia-induced Pulmonary Hypertension(Angiogenesis 3 (M), The 69th Annual Scientific Meeting of the Japanese Circulation S
- OJ-269 Pravastatin Reduce the Numbers and Adhesiveness of Circulating Flk-1 Positive Cells and Ameliorate Hypoxia-Induced Pulmonary Hypertension(Angiogenesis 2 (M) : OJ31)(Oral Presentation (Japanese))
- OE-214 Bone Marrow-Derived Progenitor Cells Contribute To the Pulmonary Arterial Remodeling in Hypoxia-Induced Pulmonary Hypertension(Angiogenesis 1 (M) : OE26)(Oral Presentation (English))
- FRS-040 Unique Arrhythmogenesis of a Familial Dilated Cardiomyopathy with Conduction Defect Caused by a Lamin A/C Gene Mutation(Arrhythmia-Clinical : Advances in Diagnosis and Management (A) : FRS5)(Featured Research Session (English))
- Adult Bone Marrow Cells with Transdifferentiation Potential for Cadiomyocytes Possess the Early Vascular Progenitor Properties and Activatable Cardiomyocyte Differentiation Systems
- Comparison of the Efficacy of Reperfusion Therapies for Early Mortality From Acute Myocardial Infarction in Japan : Registry of Miyagi Study Group for AMI (MsAMI)
- Observation of Electrical Conduction of Right Atrium Related with the Crista Terminalis and Sinus Venosa Region in Patients with AFL(Arrhythmia, Non-pharmacological Therapy 3 (A), The 69th Annual Scientific Meeting of the Japanese Circulation Society)
- Two Ttypes of Origin Refractory to Ablate from Endocardium of Idiopathic Left Ventricular Tachyarrhythmia from the Mitral Annulus(Arrhythmia, Non-pharmacological Therapy 5 (A), The 69th Annual Scientific Meeting of the Japanese Circulation Society)
- Expression of the von Willebrand Factor in Atrial Endocardium is Increased in Atrial Fibrillation Depending on the Extent of Structural Remodeling
- EFFECT OF PITUITARY ADENYLATE-CYCLASE ACTIVATING POLYPEPTIDES (PACAP) ON ADULT NEURAL STEM CELLS
- Identification of the Substrate Interaction Region of the Chitin-Binding Domain of Streptomyces griseus Chitinase C
- Myocardial phosphoinositide turnover can be assessed by positron emission tomography with C-11-labelled diacylglycerol in patients with myocardial infarction
- II-B-23 Study of development of enteric nerve network structure in the embrionic ret intestine using confocal laser scanning microscopy(THE 45TH ANNUAL MEETING OF THE JAPAN SOCIETY OF HISTOCHEMISTRY AND CYTOCHEMISTRY)
- P3-15 Relationship between proliferation of endoplasmic reticulum and induction of CYP2B1/2 in liver lobules of phenobarbital-treated rats
- THE EXISTENCE OF MULTI-ENDOCRINE CELLULAR ANTIGEN (MECA) IN THE ACTH-PRODUCING CELLS OF THE GERBIL ADENOHYPOPHYSIS : CONFOCAL LASER SCANNING MICROSCOPIC ANALYSIS
- P-30 The induction and regulation of CYP1A1 expression induced by 3 methylcholanthrene treatment on cultured hepatoma cell lines.
- A-4 A sensitive and quantitative immunohistochemical method with chemiluminescence
- Leiomyosarcoma of the spermatic cord
- Should Increasing the Dose or Adding AT1 Receptor Blocker Follow the Early Initiation of ACE Inhibitor in Acute Myocardial Infarction?
- Isolation and Identification of Acetyl-CoA Carboxylase Inhibitors from Green Tea (Camellia sinensis)
- Isolation and Activity of N-p-Coumaroyltyramine, an α-Glucosidase Inhibitor in Welsh Onion (Allium fistulosum)
- Isolation and Identification of α-Glucosidase Inhibitors from Tochu-cha (Eucommia Ulmoides)
- Clinical characterization of familial dilated cardiomyopathy with conduction defect caused by a novel lamin A/C gene mutation
- Identification of a single cell-derived bone marrow cell line with transdifferentiation potential for cardiomyocytes
- Up-regulation and nuclear localization of β-catenin in endometrial carcinoma in response to progesterone therapy
- Clinical Evaluation of Plasmapheresis for Hepatic Disorders
- Plasmapheresis in the Tokai University Medical Center, 1983-1989
- Central Sleep Apnea Predicts the Prognosis of Patients with Chronic Heart Failure Independent of Brain Natriuretic Peptide(Heart Failure, Clinical 11 (M), The 69th Annual Scientific Meeting of the Japanese Circulation Society)
- Qualitative and Quantitative Assessment of Modified In Situ Reverse Transcription-Polymerase Chain Reaction (In Situ RT-PCR) Method
- Effect of Combination Therapy with Amiodarone and Beta-blocker in Patients with Congestive Heart Failure
- One-Dimensional Heisenberg Ferromagnetic Susceptibility Just at the Percolation Threshold for K_2Cu_xZn_F_4
- Amplification of Immunostaining Intensity by the Peroxidase-Antiperoxidase, Avidin-Biotin-Peroxidase Complex or Catalyzed Signal Amplification Method Gives Erroneous Antigen Content in Sections
- Changes in the Density of Cytochrome P-450 2B1/2 Molecules in the Membrane of Endoplasmic Reticulum in Perivenular, Midzonal and Periportal Hepatocytes of Rats after Administration of Phenobarbital
- B-32 Effect of rifampicin on carbon tetrachloride-induced DNA fragmentation in hepatocytes of mice
- PACAP INDUCES DIFFERENTIATION OF MOUSE EMBRIONIC NEURAL STEM CELLS INTO ASTROCYTES IN VITRO AND IN VIVO
- Warfarin-Intractable, Intraatrial Thrombogenesis in A 52-Year-Old Woman with Mitral Stenosis and Chronic Atrial Fibrillation
- Increased synthesis of von Willebrand factor in the endocardial endothelium as a prothrombotic alteration in atrial fibrillation involving structural remodeling
- Quantitative Investigation of the Effect of Sensory Nerve Anesthesia with 9% Lidocaine Ointment on Healthy Subjects by Use of the Neuroselective Current Perception Threshold
- Dissolution Tests for Self-Setting Calcium Phosphate Cement-Containing Nifedipine
- Isolation and Cultivation of a Novel Ice Nucleation-active Strain of Xanthomonas campestris
- Investigation on the Influx Transport Mechanism of Pentazocine at the Blood-Brain Barrier in Rats Using the Carotid Injection Technique(Biopharmacy)
- Pharmacokinetic/Pharmacodynamic Relationship of Eptazocine, a Narcotic-Antagonist Analgesic, in Rats