Pharmacological Profiles of a Novel Non-peptide Angiotensin II Type I Receptor Antagonist HR720 In Vitro and In Vivo
スポンサーリンク
概要
- 論文の詳細を見る
he pharmacological properties of 2-butyl-4-(methylthio)-1-[[2 [[[(propylamino)carbonyl] amino] sulfonyl](1, 1 biphenyl)-4-yl]methyl]-1<I>H</I>-imidazole-5-carboxylate (HR720), a novel non-peptide angiotensin (Ang) II type I (AT<SUB>1</SUB>) receptor antagonist, were characterized in both in vitro and in vivo systems. In vitro autoradiography using <SUP>125</SUP>I-[Sar<SUP>1<SUP>, IIe<SUP>8</SUP>]Ang II as a ligand revealed that HR720 competitively inhibited the specific binding of the ligand to the adrenal cortex. The IC<SUB>50</SUB> value for the adrenal cortex was 1.5 x 10<SUP>-8</SUP> M, and the IC<SUB>50</SUB> for medulla was 1.4 x 10<SUP>-6</SUP> M. Similar results were obtained in the adrenal cortex with CV-11974, a known potent AT<SUB>1</SUB>-receptor antagonist. Since AT1 receptors are known to predominate in the adrenal cortex and AT<SUB>2</SUB>-receptors in the adrenal medulla, it is considered that HR720 is highly selective for AT, receptors. HR720 inhibited the Ang II-induced contraction of isolated rabbit aortic strips and human gastroepiploic arteries in a noncompetitive manner, pD<SUB>2</SUB>=9.40 and 9.62 for rabbit aorta and human artery, respectively. With CV-11974, pD<SUB>2</SUB> values of 9.84 in isolated rabbit aorta and 10.00 in human artery were obtained. HR720 did not affect the norepinephrine-, serotonin or KCl-induced contraction even at a concentration of 1 x 10<SUP>-5</SUP> M. In anesthetized hamsters, HR720 induced a dose-dependent inhibition of the pressure response to Ang II. The potency of HR720 to antagonize the Ang II-induced pressure response was similar to that of CV-11974. These results demonstrate that HR720 is a potent and selective AT<SUB>1</SUB> -receptor antagonist.
- 社団法人 日本薬理学会の論文
- 1997-11-01
著者
-
Takai Shinji
Department Of Cardiology Kouseikai Takeda Hospital
-
OKA Yuko
Department of Cardiovascular and Respiratory Medicine, Shiga University of Medical Science
-
JIN Denan
Department of Pharmacology, Osaka Medical College
-
MIYAZAKI Mizuo
Department of Pharmacology, Osaka Medical College
-
SHIOTA Naotaka
Department of Pharmacology, Osaka Medical College
-
SONG Keifu
Department of Pharmacology, Osaka Medical Colleg
-
Takai Shinji
Department Of Pharmacology Osaka Medical College
-
Jin Denan
Department Of Pharmacology Osaka Medical College
-
Song Keifu
Department Of Pharmacology Osaka Medical Colleg
-
Shiota Naotaka
Department Of Pharmacology Osaka Medical Colleg
-
Okamoto Yukiko
Department Of Pharmacology Osaka Medical College
-
Oka Yuko
Department Of Cardiovascular And Respiratory Medicine Shiga University Of Medical Science
-
Miyazaki Mizuo
Department Of Pharmacoldgy Osaka Medical College
-
Takai Shinji
Department Of Animal Hygiene School Of Veterinary Medicine And Animal Sciences Kitasato University
関連論文
- Erythropoietin in Patients With Acute Coronary Syndrome and Its Cardioprotective Action After Percutaneous Coronary Intervention
- PJ-713 Seasonal Mortality Variation in Out-of-hospital Cardiac Arrest : Analysis from AMI-Kyoto Multi-Center Risk Study Database(PJ120,Cardiopulmonary and Critical Care/ACLS (H),Poster Session (Japanese),The 73rd Annual Scientific Meeting of The Japanese
- PJ-383 Predictors of In-Hospital Prognosis after Primary Percutaneous Coronary Intervention for Repeat Myocardial Infarction : Insights from the AMI-Kyoto Multi-Center Risk Study(PJ065,ACS/AMI (Clinical/Treatment) 3 (IHD),Poster Session (Japanese),The 73r
- PE-460 Prehospital Delay Time and the Rate of Ambulance User for Acute Myocardial Infarction were not Improved from 2000-2007 in Kyoto(PE077,ACS/AMI (Clinical/Diagnosis) 1 (IHD),Poster Session (English),The 73rd Annual Scientific Meeting of the Japanese C
- New Approaches to Blockade of the Renin–Angiotensin–Aldosterone System: Chymase as an Important Target to Prevent Organ Damage
- A case of Takayasu's arteritis and aortic regurgitation, which presented much difficulty in the diagnosing process because of complicated osteomyelitis and non-typical manifestations
- FRS-036 In-hospital Prognostic Value of Crude Peak Creatine Kinase Measurement after Primary Percutaneous Coronary Intervention for Acute Myocardial Infarction(FRS8,Novel Biomarkers and Pathophysiology of ACS (IHD),Featured Research Session (English),The
- Predictors of In-Hospital Outcome After Primary Percutaneous Coronary Intervention for Recurrent Myocardial Infarction
- Effects of Hospital Volume of Primary Percutaneous Coronary Interventions on Angiographic Results and In-Hospital Outcomes for Acute Myocardial Infarction
- OJ-204 Diminished Relation Between Hospital Volume of Primary PCI and In-Hospital Outcomes After AMI : Insights from the AMI-Kyoto Multi-Center Risk Study(Acute myocardial infarction, clinical (diagnosis / treatment)(04)(IHD),Oral Presentation (Japanese),
- Predictors of In-Hospital Prognosis After Primary Percutaneous Coronary Intervention for Acute Myocardial Infarction Requiring Mechanical Support Devices
- PJ-588 Rehabilitation after Angiogenic Cell Therapy for the Critical Limb Ischemia(PJ099,Exercise Test/Cardiac Rehabilitation 2 (H),Poster Session (Japanese),The 73rd Annual Scientific Meeting of The Japanese Circulation Society)
- PJ-461 Aerobic Exercise in the Postoperative Cardiac Rehabilitation did not Deteriorate Renal Function in the Patients with Renal Failure(PJ078,Kidney/Renal Circulation/CKD 4 (H),Poster Session (Japanese),The 73rd Annual Scientific Meeting of The Japanese
- OJ-023 Intermediate Fixed Coronary Stenosis at a Site of Ergonovine-Provoked Spasm as a Predictor of the Long-Term MACE of CSA Patients(OJ04,Angina Pectoris (Basic, Clinical) (IHD),Oral Presentation (Japanese),The 73rd Annual Scientific Meeting of The Jap
- Long-Term Angiotensin II Blockade May Improve Not Only Hyperglycemia but Also Age-Associated Cardiac Fibrosis
- PE-354 Aortic Valve Thickness Depends on Cardiac ACE Activity, not Blood Pressure in 1K-, 1K1C-, and 2K1C-Rabbit Models(PE060,Valvular Heart Disease (M),Poster Session (English),The 73rd Annual Scientific Meeting of The Japanese Circulation Society)
- PE-172 Introduction of Training Program in Basic Life Support can Improve the Survival after In-Hospital Cardiopulmonary Resuscitation(PE029,Cardiopulmonary and Critical Care/ACLS (H),Poster Session (English),The 73rd Annual Scientific Meeting of The Japa
- OE-244 Protruding Atheroma in the Thoracic Aorta Detected by Multislice Computed Tomography Can Predict the Major Vascular Events(OE42,CT/MRI (Coronary/Vascular) 2 (I),Oral Presentation (English),The 73rd Annual Scientific Meeting of The Japanese Circulat
- OE-235 Evidence of Plaque Neovascularization and Effects of Angiotensin Receptor Blocker in Cholesterol-Fed Monkey(OE40,Atherosclerosis, Basic 2 (IHD),Oral Presentation (English),The 73rd Annual Scientific Meeting of The Japanese Circulation Society)
- PE-441 Virtual Histology Assessment of Attenuation Image Detected With 40MHz Gray-scale IVUS
- OE-307 Imidapril Attenuates MMP-9 Level More Effectively than Losartan in Patients with Acute Myocardial Infarction Treated by Primary-Percutaneous Coronary Intervention(Acute myocardial infarction, clinical(diagnosis/treatment)(02)(IHD),Oral Presentation
- PE-341 The Longitudinal Calcification Length in Multi-slice Computed Tomography May be Available to Detect the Coronary Artery Stenosis(CT/DSA-5 (I) PE57,Poster Session (English),The 70th Anniversary Annual Scientific Meeting of the Japanese Circulation S
- PE-317 Angiotensin Receptor 1 Blocker Inhibits Atherosclerotic Changes of Aortic Valve by Preserving Endothelial Cells and Inhibiting Transformation into Osteoblast Phenotype(Vascular heart disease/Pericarditis/Cardiac tumor-2 (M) PE53,Poster Session (Eng
- Evidence for Abundant Presence of Chymase-Positive Mast Cells in the Kidneys of Patients with Immunoglobulin A Nephropathy : Effect of Combination Therapy with Prednisolone and Angiotensin II Receptor Blocker Valsartan
- Inhibition of Human Chymase by Suramin
- Angiotensin II Type 1 Receptor Antagonist, TCV-1 16, Prevents Neointima Formation in Injured Arteries in the Dog
- IS005 Vascular Smooth Muscle Cell(VSMC)-Specific Overexpression of Angiotensin type2(AT2)Receptor Causes Endothelium-dependent Vasodilation via bradykinin/NO/cGMP pathway
- Inhibition of the Angiotensin II Type 1 Receptor by TCV-116: Quantitation by In Vitro Autoradiography
- P218 INTERACTION OF VASCULAR SMOOTH MUSCLE CELLS(VSMC) WITH EXTRACELLULAR MATRIX(ECM) : EFFECTS OF THE PURIFIED HUMAN CHYMASE ON VSMC ATTACHMENT TO ECM
- Intermediate Fixed Coronary Artery Stenosis at the Site of Ergonovine-Provoked Spasm as a Predictor of Long-Term Major Adverse Cardiac Events of Patients With Coronary Spastic Angina
- PJ-232 Postconditioning and Early ST-Segment Resolution in Patients with Acute Myocardial Infarction and Its Cardioprotective Action after Mechanical Reperfusion Therapy(PJ039,Cardiac Function (Clinical) 2 (M),Poster Session (Japanese),The 73rd Annual Sci
- PJ-340 The Relationship between Progression of Coronary Artery Plaques and Plaque Composition : Virtual Histology Intravascular Ultrasound Analysis(Intravascular endoscopy/Intravascular ultrasound(06)(I),Poster Session(Japanese),The 72nd Annual Scientific
- PE-507 Long term outcome of contrast-induced nephropathy after coronary angiography in diabetes patient with chronic kidney disease(Coronary revascularization, PCI(15)(IHD),Poster Session(English),The 72nd Annual Scientific Meeting of the Japanese Circula
- Chymase inhibition attenuates tetrachloride-induced liver fibrosis in hamsters
- Chymase inhibitor prevents the nonalcoholic steatohepatitis in hamsters fed a methionine- and choline-deficient diet
- Significance of angiotensin II receptor blockers with high affinity to angiotensin II type 1 receptors for vascular protection in rats
- Anti-Atherosclerotic Effects of Dihomo-γ-Linolenic Acid in ApoE-Deficient Mice
- Chymase Inhibition Provides Pancreatic Islet Protection in Hamsters With Streptozotocin-Induced Diabetes
- Involvement of Vascular Angiotensin II-Forming Enzymes in the Progression of Aortic Abdominal Aneurysms in Angiotensin II-Infused ApoE-Deficient Mice
- Significance of chymase-dependent angiotensin II formation in the progression of human liver fibrosis
- Characterization of Recombinant Human Chymase Expressed in Escherichia coli
- OJ-062 Effect of Chymase Inhibition by NK-3201 on Hypoxia-Induced Left Ventricular Remodeling in Mice(Cardiovascular pharmacology, basic/clinical(02)(H),Oral Presentation(Japanese),The 72nd Annual Scientific Meeting of the Japanese Circulation Society)
- The Significance of Chymase in the Progression of Abdominal Aortic Aneurysms in Dogs
- OJ-199 Role of Chymase and MMPs in Angiotensin II-induced Abdominal Aortic Aneurysms(Atherosclerosis, basic-3, The 71st Annual Scientific Meeting of the Japanese Circulation Society)
- The Effects of Chymase on Matrix Metalloproteinase-2 Activation in Neointimal Hyperplasia after Balloon Injury in Dogs
- Tissue Angiotensin II Generating System by Angiotensin-Converting Enzyme and Chymase
- PJ-418 Effects of Chymase Inhibition on the Stenosis after Polytetrafluoroethylene Grafts Implantation(Restenosis, basic/clinical-5 (IHD) PJ71,Poster Session (Japanese),The 70th Anniversary Annual Scientific Meeting of the Japanese Circulation Society)
- PE-278 Chymase Inhibition Prevents the Progression of Abdominal Aortic Aneurysm in Dogs(Peripheral circulation-5 (H) PE47,Poster Session (English),The 70th Anniversary Annual Scientific Meeting of the Japanese Circulation Society)
- Chymase Inhibition Prevents Cardiac Fibrosis and Dysfunction after Myocardial Infarction in Rats
- Role of Chymase-Dependent Angiotensin II Formation in Regulating Blood Pressure in Spontaneously Hypertensive Rats
- The Effect of Chymase Inhibition on Arteriovenous Fistula Stenosis in Dogs (Peripheral Circulation/Vascular Disease 6 (H), The 69th Annual Scientific Meeting of the Japanese Circulation Society)
- A Potent Chymase Inhibitor, Suc-Val-Pro-Phe(p)(OPh)(2), Suppresses the Development of Abdominal Aortic Aneurysm in Dogs(Valvular Heart Disease/Pericarditis/Cardiac Tumor 2 (M), The 69th Annual Scientific Meeting of the Japanese Circulation Society)
- Effect of Chymase-Dependent Transforming Growth Factor β on Peritoneal Adhesion Formation in a Rat Model
- PJ-043 An Antiarrhythmic Effect of A Chymase Inhibitor After Myocardial Infarction(Acute Myocardial Infarction, Basic 2 (IHD) : PJ8)(Poster Session (Japanese))
- Impact of Chymase Inhibitor on Cardiac Function and Survival after Myocardial Infarction
- Oral Administration of a Specific Chymase Inhibitor, NK3201, Suppresses the Development of Aneurysmal Dilatation on Hamster Experimental Aneurysm Model
- Possible Roles of Angiotensin II-Forming Enzymes, Angiotensin Converting Enzyme and Chymase-like Enzyme, in the Human Aneurysmal Aorta
- Effect of Chymase Inhibitor on Vascular Proliferation
- Development of the Chymase Inhibitor as an Anti-Tissue-Remodeling Drug : Myocardial Infarction and Some Other Possibilities
- Recombinant Human Chymase Produced by Silkworm-Baculovirus Expression System : Its Application for a Chymase Detection Kit
- Oral Administration of a Novel Chymase Inhibitor, NK3201, Prevents Peritoneal Adhesion Formation in Hamsters
- Role of chymase in the development of aneurysmal formation; An experimental aneurysm model
- Possible Roles of Cardiac Chymase After Myocardial Infarction in Hamster Hearts
- PJ-743 A Comparison of Re-restenosis Results and Treatment Technique for Restenosis Lesion : Sirolimus-eluting Stent Versus Bare Metal Stent(Coronary revascularization, PCI-20, The 71st Annual Scientific Meeting of the Japanese Circulation Society)
- PJ-498 Assessment of cardiomyopathy with transient ballooning of the mid-base of the left ventricle. A new form of Takotsubo cardiomyopathy(Cardiomyopathy, basic/clinical-6 (M) PJ84,Poster Session (Japanese),The 70th Anniversary Annual Scientific Meeting
- PJ-423 Restenosis Following Sirolimus-eluting Stent Implantation for Ostial Lesions(Restenosis, basic/clinical-5 (IHD) PJ71,Poster Session (Japanese),The 70th Anniversary Annual Scientific Meeting of the Japanese Circulation Society)
- PJ-114 Assessment of the Latent Congestive Heart Failure in Patients with Arterial Fibrillation Using I-123 BMIPP Myocardial Images(Nuclear cardiology-8 (I) PJ19,Poster Session (Japanese),The 70th Anniversary Annual Scientific Meeting of the Japanese Circ
- OJ-170 Assessment of Lipid Pool of Coronary Artery Plague. -Gray Scale IVUS vs. Virtual Histology IVUS(Echo/Doppler-4 (I) OJ29,Oral Presentation (Japanese),The 70th Anniversary Annual Scientific Meeting of the Japanese Circulation Society)
- OJ-131 Assessment of Coronary Artery Plaque in ACS Patient Using Virtual Histology IVUS(Acute coronary syndrome, basic/clinical-2 (IHD) OJ22,Oral Presentation (Japanese),The 70th Anniversary Annual Scientific Meeting of the Japanese Circulation Society)
- OJ-099 Limitation of Sirolimus Eluting Stent for Recurrent In-stent Restenosis(Coronary revascularization, PCI-5 (IHD) OJ17,Oral Presentation (Japanese),The 70th Anniversary Annual Scientific Meeting of the Japanese Circulation Society)
- Potentiation by platelet-derived growth factor-BB of FGF-2-stimulated VEGF release in osteoblasts
- PJ-333 Impact of Clinical Path on Self Esteem to Modify Lifestyle in Patients Undergoing Cardiac Catheterization : Using Questionnaire about Lifestyle(PJ056,Preventive Medicine/Epidemiology/Education 2 (H),Poster Session (Japanese),The 73rd Annual Scienti
- PE-549 Different Acute Effect of Continuous Positive Airway Pressure on Morning Blood Pressure in Obstructive Sleep Apnea(Hypertension, clinical(06)(H),Poster Session(English),The 72nd Annual Scientific Meeting of the Japanese Circulation Society)
- Trans-Differentiation of Bone Marrow Monocyte-Lineage Cells to Endothelial-Like Cells and Reendothelialization on Injured Endothelium by MCP-1-Dependent Adhesion
- Coronary Microcirculation Disturbance in Takotsubo-like Transient Left Ventricular Dysfunction(Cardiomyopathy, Clinical 3 (M), The 69th Annual Scientific Meeting of the Japanese Circulation Society)
- PE-398 Nuclear Factor-κ B Activation Accelerates Cardiac Hypertrophy, Interstitial Fibrosis, and Oxidative Stress in Diabetic Rats Exposed to Intermittent Hypoxia(Chronic coronary heart disease/Remodeling-2, The 71st Annual Scientific Meeting of the Japan
- RELATIONSHIP AMONG ABNORMALITIES OF THE ULTRASONIC THREE-LAYERED APPEARANCE OF THE VENTRICULAR SEPTUM, MYOCARDIAL FATTY ACID METABOLISM AND PERFUSION IN PATIENTS WITH HYPERTROPHIC CARDIOMYOPATHY
- G-CSF Treatment Inhibits Neointimal Hyperplasia Associated with Endothelial Progenitor Cell Mobilization and Acceleration of Reendothelialization in Catorid Artery Injuty Model(Restenosis after Angioplasty, Basic/Clinical 5 (IHD), The 69th Annual Scientif
- Critical Role of Tyrosine Kinase PYK2 in eNOS Activation Revealed by Analysis of PYK2 Knockout Mice(Endothelium/NO 5 (H), The 69th Annual Scientific Meeting of the Japanese Circulation Society)
- OJ-417 Tyrosine Kinase PYK2 activates eNOS and subsequently regulates Vascular Tonus and Angiogenesis, revealed by its Knock-out Mice(Endothelium/NO 5 (H) : OJ51)(Oral Presentation (Japanese))
- eNOS Activation and Its Vascular Functions Critically Requires the Presence of Tyrosine Kinase PYK2
- OJ-028 G-CSF Treatment Inhibits Neointimal Formation after Arterial Injury through the Mobilization of Endothelial Progenitor Cell and Acceleration of Reendothelialization(Restenosis, basic/clinical-1 (IHD) OJ5,Oral Presentation (Japanese),The 70th Annive
- Inhibition of Vascular Angiotensin-Converting Enzyme by Telmisartan via the Peroxisome Proliferator-Activated Receptor γ Agonistic Property in Rats
- Inhibition of Matrix Metalloproteinase-9 Activity by Trandolapril after Middle Cerebral Artery Occlusion in Rats
- Predictors of nonoptimal coronary flow after primary percutaneous coronary intervention with stent implantation for acute myocardial infarction
- Erythropoietin Prevention Trial of Coronary Restenosis and Cardiac Remodeling After ST-Elevated Acute Myocardial Infarction (EPOC-AMI) : A Pilot, Randomized, Placebo-Controlled Study
- Influence of previous myocardial infarction site on in-hospital outcome after primary percutaneous coronary intervention for repeat myocardial infarction
- 我が国における子馬のロドコッカス・エクイ感染症の疫学調査--1992年から1998年の108症例
- Trandolapril Reduces Infarction Area after Middle Cerebral Artery Occlusion in Rats
- SOME EXPERIMENTS ON ASCENDING OF CORYNEBACTERIUM RENALE IN MICE FROM URINARY BLADDER INTO KIDNEYS
- Significance of Angiotensin II Receptor Blocker Lipophilicities and Their Protective Effect against Vascular Remodeling
- Combination therapy with irbesartan and efonidipine for attenuation of proteinuria in Dahl salt-sensitive rats
- Genotypic Characterization of Virulent Rhodococcus equi Isolated from the Environment of Hokkaido Native Horses in Hakodate, Hokkaido
- Comparative Effects of Candesartan and Amlodipine in a Monkey Atherosclerotic Model
- Pharmacological Profiles of a Novel Non-peptide Angiotensin II Type I Receptor Antagonist HR720 In Vitro and In Vivo
- Cloning and Characterization of the fur Gene From Moraxella bovis
- Expression of Virulence-Associated Antigens of Rhodococcus equi Is Regulated by Temperature and pH
- Rhodococcus qui Infection in Foals -Current Concepts and Implication for Future Research-
- Clinical manifestations and effects of primary percutaneous coronary intervention for patients with delayed pre-hospital time in acute myocardial infarction
- Irbesartan Prevents Metabolic Syndrome in Rats via Activation of Peroxisome Proliferator-Activated Receptor γ