Assessment of Binding Affinity to 5-Hydroxytryptamine 2A (5-HT_<2A>) Receptor and Inverse Agonist Activity of Naftidrofuryl : Comparison With Those of Sarpogrelate
スポンサーリンク
概要
- 論文の詳細を見る
Naftidrofuryl is a peripheral vasodilator that has been clinically used in the treatment of intermittent claudication and dementia. It has 5-hydroxytryptamine 2 (5-HT2) antiserotonergic activity and selectively binds with the 5-HT2 receptor. The purpose of the present study is to assess the binding affinity and functional potency of naftidrofuryl to the 5-HT2A receptor, to find out the inverse agonist activity of this compound at a constitutively active mutant of 5-HT2A receptor, and finally to compare the findings with those of sarpogrelate. The investigation showed that the binding affinity (pKi) of naftidrofuryl was decreased 25- or 50-fold compared to sarpogrelate in the wild-type 5-HT2A receptor or Cys322Lys mutant receptor, respectively. Moreover, the functional potency (pKb) of naftidrofuryl was much lower compared to sarpogrelate at the 5-HT2A receptor. In addition, inverse agonist activity of naftidrofuryl was lower compared with sarpogrelate at the constitutively active mutant receptor. Thus, the data of the present study would be very important for the clarification of interaction sites of naftidrofuryl to 5-HT2A receptors and also may help to understand the mechanism of inverse agonist activity at the constitutively active mutant receptor.
- 2009-08-20
著者
-
Nakamura Takashi
Department of Cardiology, Saiseikai Shigaken Hospital
-
BHUIYAN Mohiuddin
Department of Pharmacology, Niigata University of Pharmacy and Applied Life Sciences
-
HOSSAIN Murad
Department of Pharmacology, Niigata University of Pharmacy and Applied Life Sciences
-
NAGATOMO Takafumi
Department of Pharmacology, Niigata University of Pharmacy and Applied Life Sciences
-
長友 孝文
新潟薬科大学薬学部薬理学教室
-
ALY Saida
Department of Pharmacology, Faculty of Pharmaceutical Sciences, Niigata University of Pharmacy and A
-
Bhuiyan Mohiuddin
Dep. Of Pharmacology Fac. Of Pharmaceutical Sciences Niigata Univ. Of Pharmacy And Applied Life Scie
-
Aly Saida
Department Of Pharmacology Faculty Of Pharmaceutical Sciences Niigata University Of Pharmacy And App
-
Aly Saida
Department Of Pharmacology Faculty Of Medicine Assiut University
-
Nagatomo T
Dep. Of Pharmacology Fac. Of Pharmaceutical Sciences Niigata Univ. Of Pharmacy And Applied Life Scie
-
Nagatomo Takafumi
Department Of Pharmacology Faculty Of Pharmaceutical Sciences Niigata University Of Pharmacy And App
-
Bhuiyan Mohiuddin
Department Of Pharmacology Faculty Of Pharmaceutical Sciences Niigata University Of Pharmacy And App
-
Hossain Murad
Department Of Pharmacology Faculty Of Pharmaceutical Sciences Niigata University Of Pharmacy And App
-
Nakamura Takashi
Department Of Cardiology Saiseikai Shiga Hospital
関連論文
- Erythropoietin Prevention Trial of Coronary Restenosis and Cardiac Remodeling After ST-Elevated Acute Myocardial Infarction (EPOC-AMI) : – A Pilot, Randomized, Placebo-Controlled Study –
- 1P113 Backbone NMR assignment and hydrogen exchange of goat α-lactalbumin(3. Protein folding and misfolding (1),Poster Session,Abstract,Meeting Program of EABS & BSJ 2006)
- 1P101 The role of Ca^ in the folding of goat α-Lactalbumin(3. Protein folding and misfolding (I),Poster Session,Abstract,Meeting Program of EABS & BSJ 2006)
- Engineered Mutation of Some Important Amino Acids in Angiotensin II Type 1 (AT1) Receptor Increases the Binding Affinity of AT1-Receptor Antagonists
- Constitutively Active Mutant N111G of Angiotensin II Type 1 (AT_1) Receptor Induces Homologous Internalization Through Mediation of AT_1-Receptor Antagonist
- Coulomb Excitation of ^24Si
- Coulomb Dissociation of ^23Al
- Coulomb Excitation of ^Si
- Coulomb Dissociation of ^Al
- Assessment of Binding Affinity to 5-Hydroxytryptamine 2A (5-HT_) Receptor and Inverse Agonist Activity of Naftidrofuryl : Comparison With Those of Sarpogrelate
- Evaluation of a commercial PET tomograph-based system for the quantitative assessment of rCBF, rOEF and rCMRO_2 by using sequential administration of ^O-labeled compounds
- Identification of New Isotopes ^Pd and ^Pd Produced by In-Flight Fission of 345 MeV/nucleon ^U : First Results from the RIKEN RI Beam Factory(Nuclear physics)
- Inelastic Scattering of ^12Be with ^4He
- Inelastic Scattering of ^Be with ^4He
- Study of the ^7Be (p,γ)^8B Reaction with the Coulomb Dissociation Method
- The Design and Performance of Multiwire Proportional Chambers for High Flux Beam Monitoring
- Development of a New High-Speed Measuring System to Analyze the Dental Cast Form
- Long-term survivorship analysis of hip arthroplasty with vitallium mold cup
- Mutation of Important Amino Acid Residue of Asp104Lys in Human β_1-Adrenergic Receptor Triggers Functional and Constitutive Inactivation(Pharmacology)
- Identification of a Key Amino Acid of the Human 5-HT_ Serotonin Receptor Important for Sarpogrelate Binding
- Selectivity of Sarpogrelate to the Recombinant Human 5-HT_ Receptors as Assessed by Molecular Pharmacology and Molecular Modeling
- Non-Contact Evaluation for Articular Cartilage Using Ultrasound
- Calibration of a DBF Receiving Array Antenna by Using a Reference Sequence for Systems in Power-Limited Channels
- Prevalence of Coronary Artery Disease in Japanese Patients With Cerebral Infarction : Impact of Metabolic Syndrome and Intracranial Large Artery Atherosclerosis
- PJ-223 Behavioral Monitoring in Life-style Intervention Can Predict Cardiovascular Events Independently of Major Biological Risk Factors in High-risk Hypertensive Patients(Hypertension, clinical-9 (H) PJ38,Poster Session (Japanese),The 70th Anniversary An
- Severe erosive arthropathy requiring surgical treatments in systemic lupus erythematosus
- Development of General-Purpose Particle and Heavy Ion Transport Monte Carlo Code
- A Field-Theoretic Model of Macroscopic Quantum Nucleation
- MECHANISM OF CIRCULATORY COLLAPSE IN RATS WITH SPONTANEOUSLYOCCURING HYPERTRORHIC CARDIOMYOPATHY
- Peptic ulcer recurrence during maintenance therapy with H^2-receptor antagonist following first-line therapy with proton pump inhibitor
- Internalization of Constitutively Active N111G Mutant of AT1 Receptor Induced by Angiotensin II–Receptor Antagonists Candesartan, Losartan, and Telmisartan: Comparison With Valsartan
- Amino Acids of the Human α_-Adrenergic Receptor Involved in Antagonist Binding
- Pharmacological and Molecular Characterization of Novel SWR-Compounds for β-Adrenergic Receptors as assessed by Molecular Modeling, Site-Directed Mutagenesis, Binding Affinity and Functional Activity
- Assessment of Affinity and Dissociation Ability of a Newly Synthesized 5-HT_2 Antagonist, AT-1015: Comparison With Other 5-HT_2 Antagonists
- DPJ-050 Comprehensive Cardiac Rehabilitation Improves Clinical Outcome in Patients with Acute Coronary Syndrome after Implantation of Drug-eluting Stents(DPJ09,Exercise Test/Cardiac Rehabilitation (H),Digital Poster Session (Japanese),The 73rd Annual Scie
- PJ-117 Combination of Carotid Arterial Wall Thickness and Stiffness Parameters Improves Prediction of Target Organ Damage in Patients with Essential Hypertension(Hypertension, Clinical 2 (H) : PJ20)(Poster Session (Japanese))
- Validation of the Japanese version of the Roland-Morris Disability Questionnaire
- IMMUNOELECTRON MICROSCOPIC LOCALIZATION OF HUMAN T-CELL LEUKEMIA VIRUS TYPE-I ANTIGENS (Immuno-Histochemistry and Cytochemistry)
- Identification of a Key Amino Acid of the Human 5-HT2B Serotonin Receptor Important for Sarpogrelate Binding
- Isolated Left Ventricular Noncompaction Was not a Very Rare Disorder in an Adult Population
- Habitual Walking Improves Distensibility of Central Artery in Patients with Essential Hypertension : Relation to Blood Pressure Reduction and Energy Metabolism
- Energy Spectrum of Ultra High Energy γ-Rays from Supernova
- Time Variation of Ultra High Energy γ-Ray from SN1987A
- Response Function Measurements of the Self-TOF Neutron Detector for Neutrons up to 800 MeV
- The Recovery of the Walking Ability of Patients at Early Stages after Total Hip Arthroplasty from the Perspective of the Displacement of the Center of Gravity
- Neuroprotection and Enhanced Recovery With Edaravone After Acute Spinal Cord Injury in Rats
- Expression Profile of Amylolytic Genes in Aspergillus nidulans
- β-Adrenoceptors: Three-Dimensional Structures and Binding Sites for Ligands
- An Off-Axis Jet Model for GRB 980425 and Low Energy Gamma-Ray Bursts(Poster)
- Erythropoietin Prevention Trial of Coronary Restenosis and Cardiac Remodeling After ST-Elevated Acute Myocardial Infarction (EPOC-AMI) : A Pilot, Randomized, Placebo-Controlled Study
- Pharmacological Tests in 100 Patients with Intractable Pain
- Raw Materials for Low-Activation Concrete Neutron Shields
- Correlation between Tritium and ^Eu Induced in Various Types of Concrete by Thermal Neutron Irradiation
- Design and Implementation of a Community-based Limb Salvage Program for ESRD Patients
- Inhibitory Effects of a Newly Synthesized 5-HT_2 Receptor Antagonist, AT-1015 (N-[2-[4-(5H-Dibenzo[a, d]cyclohepten-5-ylidene)piperidino]-ethyl]-1-formyl-4-piperidinecarboxamide Monohydrochloride Monohydrate), on Contraction and Relaxation of Pig Coronary
- Comparative Analyses of Fatty Acid Compositions in Rice Grain Glycerolipids among Three Cultivars with Different Chilling Susceptibilities
- Preparation of and Immunoelectron Microscopy with a Monoclonal Antibody to the Structural Protein of a Retrovirus Produced in a Human Lymphoblastoid Cell Line
- Characterization of the Complex between α_2-Macroglobulin and a Serine Proteinase from Bacillus natto(Biological Chemistry)
- The Long-Term Effect of Eicosapentaenoic Acid on Serum Levels of Lipoprotein (a) and Lipids in Patients with Vascular Disease
- Interaction of π-Electrons in the Acetylene Molecule
- Cross-sectional analysis of the surface ceramic layer developed on Ti metal by NaOH-heat treatment and soaking in SBF
- Tackler's bony spur in sumo wrestlers : a report of two cases
- Gravitational Radiation from a Particle with Orbital Angular Momentum Plunging into a Kerr Black Hole : Astrophysics and Relativity
- General Relativistic Collapse to Black Holes and Gravitational Waves from Black Holes
- Gravitational Radiation from a Particle Scattered by a Kerr Black Hole : Astrophysics and Relativity
- X-Rays and γ-Rays from a Non-Spherical Patchy Supernova Ejecta : Astrophysics and Relativity
- O-C2 Angle as a Predictor of Dyspnea and/or Dysphagia After Occipitocervical Fusion
- Atlantoaxial Transarticular Screw Fixation With Posterior Wiring Using Polyethylene Cable : Facet Fusion Despite Posterior Graft Resorption in Rheumatoid Patients
- Vertebral Artery Injury During Cervical Spine Surgery : A Survey of More than 5600 Operations
- Pneumoretroperitoneum, Pneumomediastinum, Pneumopericardium, and Subcutaneous Emphysema Complicating Sigmoidoscopy : Report of a Case
- (重イオン慣性核融合の新しい展開)
- Natural course of desmoid-type fibromatosis
- Elevation of lipid peroxide level and production of hydroxy lipids in cultured Hepa-T1 cells by oxidative stressors
- Fracture Resistance of Inlay-retained Fixed Partial Dentures Reinforced with Fiberreinforced Composite
- In Vitro Study on Marginal and Internal Fit of CAD/CAM All-Ceramic Crowns
- Application of a Dental CAD/CAM System to the Production of All-ceramic Crowns
- Collective Instabilities of Self-Gravitating Systems. III : Disk-Halo System
- Collective Instabilities of Self-Gravitating Systems. II : Instabilities Due to Temperature Anisotropy
- Collective Instabilities of Self-Gravitating Systems : Infinite Homogeneous Case
- The Clinical Risk of Vertebral Artery Injury From Cervical Pedicle Screws Inserted in Degenerative Vertebrae
- Transpedicular Screw Placement Evaluated by Axial Computed Tomography of the Cervical Pedicle
- Atlantoaxial Transarticular Screw Fixation for a High-Riding Vertebral Artery
- Cervical disc herniation causing localized ipsilateral popliteal pain
- Pseudoaneurysm of the Deep Circumflex Iliac Artery : A Rare Complication at an Anterior Iliac Bone Graft Donor Site
- Sclerotherapy for Varicose Veins of the Lower Legs in Patients with Dysplasminogenemia
- Remarkable Stereochemical Features of Ene Reaction of 2-(Alkylthio)crotyl Silyl Ethers. Proposal of a Six-Membered Chair-like Transition State
- Hyaluronan inhibits IL-1β-stimulated collagenase production via down-regulation of phosphorylated p38 in SW-1353 human chondrosarcoma cells
- Lack of increase in postoperative complications with low-dose methotrexate therapy in patients with rheumatoid arthritis undergoing elective orthopedic surgery
- Requirement of mitogen-activated protein kinase for collagenase production by the fibronectin fragment in human articular chondrocytes in culture
- Metabolic balance of streams draining urban and agricultural watersheds in central Japan
- The Coagulofibrinolytic State of Patients with Primary Varicose Veins of the Lower Legs
- Electrophoretic Deposition Behavior of Ceria-stabilized Zirconia/Alumina Powder
- Synthesis and Characterization of Novel Phosphido-Bridged Bimetallic Complexes of Molybdenum and Tungsten
- Preparation of Monodispersed Cu Nanoparticles by Microwave-Assisted Alcohol Reduction
- A Null Test of the Cosmological Constant
- Apatite formation on surface titanate layer with different Na content on Ti metal
- Preparation of bioactive Ti and its alloys via electrochemical treatment in sulfuric acid solution
- Superior mesenteric arterial embolism : treatment by trans-catheter thrombo-aspiration
- Energy, Momentum and Angular Momentum of Gravitational Waves Induced by a Particle Plunging into a Schwarzschild Black Hole
- Gravitational Waves from a Particle Scattered by a Schwarzschild Black Hole : Astrophysics and Relativity