The Therapeutic Efficacy of VP-343,a Selective Vasopressin V_2 Receptor Antagonist, in the Experimental SIADH Rat Model
スポンサーリンク
概要
- 論文の詳細を見る
The aim of this work is to investigate the therapeutic efficacy of VP-343 ((N-[4-[[2S, 3aR)-2-hydroxy-2,3,3a, 4-tetrahydropyrrolo[1,2-a]qunoxalin-5(1H)-yl]phenyl]-4'-methyl[1,1'-biphenyl]-2-carboxamide), a selective vasopressin V_2 receptor antagonist, using the experimental SIADH (syndrome of inappropriate secretion of antidiuretic hormone) rat model. In the model, which was accomplished by administering continuously 1-desamino-8-D-arginine vasopressin (DDAVP), serum sodium levels (S_<Na>) and serum osmolarity levels (S_<Osm>) significantly and remarkably decreased, which was accompanied with hyper-osmolarity of urine and oliguria. VP-343 increased rapidly and dose-dependently S_<Na> and S_<Osm>. VP-343 exhibited marked diuretic action and decreased urine osmolarity dose-dependently. In the SIADH rat model, all serum levels of chloride, calcium, creatinine, total cholesterol, and uric acid decreased when compared with normal levels. VP-343 increased all serum levels or chloride, calcium, and total cholesterol.These results indicate that VP-343 has efficacy to normalize the abnormalities in DDAVP-induced SIADH.
- 公益社団法人日本薬学会の論文
- 2000-11-01
著者
-
Ohtake Yosuke
Dep. Of Radiopharmacology Tohoku Pharmaceutical Univ.
-
Naito Akira
Sagami Research Laboratory Wakamoto Pharmaceutical Co. Ltd.
-
Koike Katsuo
東京薬科大学 内分泌分子薬理学
-
Koike K
Toho Univ. School Of Pharmaceutical Sci. Chiba Jpn
-
Koike Katsuo
Department Of Chemical Pharmacology Toho University Faculty Of Pharmaceutical Sciences
-
Shigenobu K
Department Of Pharmacology Toho University School Of Pharmaceutical Sciences
-
Tsuneoka Yayoi
Department of Pharmacology, Faculty of Pharmaceutical Sciences, Toho University
-
Naito A
Sagami Research Laboratory Wakamoto Pharmaceutical Co. Ltd.
-
Shigenobu Koki
Toho University School Of Pharmaceutical Sciences
-
KURASAWA Takashi
Sagami Research Laboratory, Wakamoto Pharmaceutical Co., Ltd.
-
OHTAKE Yasuhiro
Sagami Research Laboratory, Wakamoto Pharmaceutical Co., Ltd.
-
EZURE Yohji
Sagami Research Laboratory, Wakamoto Pharmaceutical Co., Ltd.
-
HASEGAWA Hisashi
Sagami Research Laboratory, Wakamoto Pharmaceutical Co., Ltd.
-
MATSUKAWA Hidehiko
Sagami Research Laboratory, Wakamoto Pharmaceutical Co., Ltd.
-
KOIKE Katsuo
Toho University School of Pharmaceutical Sciences
-
TSURIYA Yoshihiro
Sagami Reserch Laboratory, Wakamoto Pharmaceutical Co., Ltd.,
-
Koike K
Toho Univ. Chiba Jpn
-
Tanaka Yoshio
Dep. Of Chemical Pharmacology Fac. Of Pharmaceutical Sciences Toho Univ.
-
Hasegawa Hisashi
Sagami Research Laboratory Wakamoto Pharmaceutical Co. Ltd.
-
Toyoda Yoshihiro
Sagami Research Laboratory Wakamoto Pharmaceutical Co. Ltd.
-
Ezure Yohji
Sagami Research Laboratory Wakamoto Pharmaceutical Co. Ltd.
-
Hasegawa H
Department Of Pharmaceutical Technology Kobe Pharmaceutical University
-
Matsukawa Hidehiko
Sagami Research Laboratory Wakamoto Pharmaceutical Co. Ltd.
-
Tanaka Yoshio
Department Of Pharmacology Toho University Faculty Of Pharmaceutical Sciences
-
Ohtake Yasuhiro
Sagami Research Laboratory Wakamoto Pharmaceutical Co. Ltd.
-
Kurasawa Takashi
Sagami Research Laboratory Wakamoto Pharmaceutical Co. Ltd.
関連論文
- The Characteristics of Endothelin Receptor Subtypes on Muscle Contraction and Neuro-transmission in Rat Vas Deferens
- The Modified High-Density Survival Assay is the Useful Tool to Predict the Effectiveness of Fractionated Radiation Exposure
- Effect of T-type and L-type Ca^2+ Channel Blockade on Early Phase Ca^2+ Transients in Rat Atrial and Ventricular
- Relationship between Liver Injury and Transglutaminase Activities in Guinea Pigs and Rats(Pharmacology)
- Lack of Action Potential-Prolonging Effect of Terfenadine on Rabbit Myocardial Tissue Preparations(Pharmacology)
- The Effects of Several Vasopressin Receptor Antagonists on Normal Intraocular Pressure and the Intraocular Distribution of Vasopressin Receptor Subtypes
- New Aspects for the Treatment of Cardiac Diseases Based on the Diversity of Functional Controls on Cardiac Muscles : Diversity in the Excitation-Contraction Mechanisms of the Heart
- Species Difference in the Contribution of T-Type Calcium Current to Cardiac Pacemaking as Revealed by R(-)-Efonidipine
- Analysis of Arrhythmogenic Profile in a Canine Model of Chronic Atrioventricular Block by Comparing In Vitro Effects of the Class III Antiarrhythmic Drug Nifekalant on the Ventricular Action Potential Indices Between Normal Heart and Atrioventricular Bloc
- Muscarinic Receptor Subtypes Mediating Positive and Negative Inotropy in the Developing Chick Ventricle
- Atria Selective Prolongation by NIP-142, an Antiarrhythmic Agent, of Refractory Period and Action Potential Duration in Guinea Pig Myocardium
- MaxiK channel-triggered negative feedback system is preserved in the urinary bladder smooth muscle from streptozotocin-induced diabetic rats
- Histopathological Study of Kidney Abnormalities in an Experimental SIADH Rat Model and Its Application to the Evaluation of the Pharmacologic Profile of VP-343, a Selective Vasopressin V_2 Receptor Antagonist
- The Therapeutic Efficacy of VP-343,a Selective Vasopressin V_2 Receptor Antagonist, in the Experimental SIADH Rat Model
- The Effect of Blood Decrease on ^Ga Uptake by the Liver in Partially Hepatectomized Rats(Biopharmacy)
- Involvement of the Na^+/Ca^ Exchanger in the Automaticity of Guinea-Pig Pulmonary Vein Myocardium as Revealed by SEA0400
- The Effects of β-Adrenoceptor Agonists on KCI-induced Rhythmic Contraction in the Ureter of Guinea Pig
- Mechanism of Inhibition of Small Intestinal Motility by Restraint Stress Differs from That with Norepinephrine Treatment in Rats
- Activation of μ-Opioid Pathway Is Associated with the Canceling Effect of Footshock Stimulus on the Restraint Stress-Induced Inhibition of Small Intestinal Motility in Rats
- The R(-)-Enantiomer of Efonidipine Blocks T-type but Not L-type Calcium Current in Guinea Pig Ventricular Myocardium
- Effect of Cilnidipine on L- and T-type Calcium Currents in Guinea Pig Ventricle and Action Potential in Rabbit Sinoatrial Node
- Clinically relevant radioresistant cells efficiently repair DNA double-strand breaks induced by X-rays
- Gene Expression Profiles in Mouse Liver Cells after Exposure to Different Types of Radiation
- Inhibition of Agonist-Induced Positive Inotropy by a Selective Rho-Associated Kinase Inhibitor, Y-27632
- Pharmacological Evidence for Involvement of Phospholipase D, Protein Kinase C, and Sodium-Calcium Exchanger in α-Adrenoceptor-Mediated Negative Inotropy in Adult Mouse Ventricle
- Chronotropic Effects of Optical Isomers of Ephedrine and Methylephedrine in the Isolated Rat Right Atria and in Vitro Assessment of Direct and Indirect Actions on β_1-Arenoceptors
- Assessment of Antihistaminic and Antimuscarinic Effects of Optical Isomers of Ephedrine and Methylephedrine by Receptor Binding Assay in Guinea Pig Ileal Muscle
- Pharmacological Profile of VP-343,a Novel Selective Vasopressin V_2 Receptor Antagonist, in Rats
- Transferrin Is Not Involved in the Entry of^Ga into Hepatocytes from Regenerating Liver of Partially Hepatectomized Rats
- Neuroprotective Effect of the Novel Na^+/Ca^ Channel Blocker NS-7 on Rat Retinal Ganglion Cells
- The Uptake Mechanism of Gallium-67 into Hepatocytes Treated with Carbon Tetrachloride(Biochemistry)
- The Involvement of Transferrin in the Uptake of Iron-59 by Hepatocytes of Carbon Tetrachloride-Damaged Rats(Pharmacology)
- The Involvement of Polyamines as Substrates of Transglutaminase in Zonal Different Hepatocyte Proliferation after Partial Hepatectomy(Biochemistry/Molecular Biology)
- Uptake of Gallium-67 by the Hepatocytes during Liver Regeneration in Carbon Tetrachloride-Treated Mice(Biochemistry/Molecular Biology)
- Zonal Differences in DNA Synthesis and in Transglutaminase Activity between Perivenous versus Periportal Regions of Regenerating Rat Liver(Biochemistry/Molecular Biology)
- Role of BK Channels in Testosterone-Induced Relaxation of the Aorta in Spontaneously Hypertensive Rats(Pharmacology)
- Oxidative Stress Induced Lipocalin 2 Gene Expression : Addressing its Expression under the Harmful Conditions
- A POSSIBLE MECHANISM OF ACTION OF A BETA-ADRENERGIC PARTIAL AGONIST (CARTEOLOL) IN GUINEA PIG TAENIA CAECUM
- β-Adrenoceptors in the Detrusor of Guinea Pig Bladder
- Characteristics of Ca^ Oscillations in Ileal Longitudinal Muscle Cells of Guinea Pig
- Differences of Antagonism for a Selective α_-Adrenoceptor Antagonist BMY 7378 in the Rabbit Thoracic Aorta and Iliac Artery
- The β_2- and β_3-Adrenoceptor-Mediated Relaxation Induced by Isoprenaline and Salbutamol in Guinea Pig Taenia Caecum
- 平滑筋における薬物レセプターメカニズム : β-クロロエチルアミン親和性および非親和性レセプターメカニズム
- Signal Transduction Pathway Involved in β_3 - Adrenoceptor - Mediated Relaxation in Guinea Pig Taenia Caecum
- Effect of humulus lupulus on Gastric Secretion in a Rat Pylorus-Ligated Model(Pharmacology)
- Studies on the mechanisms underlying β-adrenoceptor-mediated relaxation of rat abdominal aorta
- Nitric Oxide (NO) Primarily Accounts for Endothelium-Dependent Component of β-Adrenoceptor-Activated Smooth Muscle Relaxation of Mouse Aorta in Response to Isoprenaline
- EFFECTS OF AGING ON ALPHA-1 AND-2 ADRENOCEPTOR MECHANISMS IN SMOOTH MUSCLES
- ALPHA_1-ADRENOCEPTOR MECHANISM AND AGING
- (+__-)-Pindolol Acts as a Partial Agonist at Atypical β-Adrenoceptors in the Guinea Pig Duodenum
- INTERACTIONS OF BEFUNOLOL, A BETA-ADRENERGIC PARTIAL AGONIST, AND ITS DERIVATIVES WITH HIGH AND LOW AFFINITY SITES IN BETA-ADRENOCEPTORS
- INTERACTION OF DYNORPHIN DERIVATIVE CONTAINING 3-NITRO-2-PYRIDINESULFENYL (Npys) GROUP WITH OPIOID RECEPTORS
- Comparison of the Inhibitory Effects of Docosahexaenoic Acid (DHA) on U46619-and Phenylephrine-Induced Contractions in Guinea-Pig Aorta(Pharmacology)
- Free ^Ga enters into the hepatocytes of carbon tetrachloride-treated rats
- Further Evidence that (±)-Carteolol-induced Relaxation is Mediated by β_2-Adrenoceptors but not by β_3-Adrenoceptors in the Guinea Pig Taenia Caecum
- MaxiK channel roles in blood vessel relaxations induced by endothelium-derived relaxing factors and their molecular mechanisms
- β1-Subunit of MaxiK Channel in Smooth Muscle : a Key Molecule Which Tunes Muscle Mechanical Activity
- β_1-Adrenoceptor-mediated relaxation with isoprenaline and the role of MaxiK channels in guinea-pig esophageal smooth muscle
- MaxiK Channel Mediates β_2-Adrenoceptor-activated Relaxation to Isoprenaline through cAMP-dependent and -independent Mechanisms in Guinea-pig Tracheal Smooth Muscle
- The β_3-Adrenoceptor-Mediated Relaxation Induced by Dopamine in Guinea Pig Taenia Caecum
- Development of an Experimental System for Evaluation of Stress Effect on Ethyl Alcohol Metabolism Using Radiorespirometric Analysis in Rat (Pharmacology)
- Effects of a New Positive Inotropic Agent with a Vasodilatory Action, 5-Methyl-6-(4-pyridyl)-2H-1,4-thiazin-3 (4H)-one (ZSY-27), on Calcium-Movement and Mechanical Response in Rabbit Thoracic Aorta
- Zonal differences in gallium-67 uptakes between perivenous versus periportal regions of rat liver following carbon tetrachloride treatment
- Antioxidative Action of the β-Adrenoceptor Antagonist Bopindolol and Its Metabolite 18-502
- Electromyographic Study of the Elbow Flexors and Extensors in a Motion of Forearm Pronation/Supination while Maintaining Elbow Flexion in Humans
- Electromyographic (EMG) Study of the Elbow Flexors during Supination and Pronation of the Forearm
- Functional Contribution of Voltage-Dependent and Ca^2+-Activated K^+ (BK_ca) Channels to the Relaxation of Guinea-Pig Aorta in Response to Natriuretic Peptides
- Structure-Activity Relationship Studies of (±)- Terbutaline and (±)-Fenoterol on β_3-Adrenoceptors in the Guinea Pig Gastric Fundus
- INHIBITION OF Ca-MOVEMENT AND MECHANICAL MOVEMENT IN RABBIT TAENIA COLI BY A SMOOTH MUSCLE RELAXANT (SULOCTIDIL)
- EFFECTS OF SMOOTH MUSCLE RELAXANT (ASPAMINOL) ON Ca-UPTAKE BY MITOCHONDRIAL AND MICROSOMAL FRACTIONS FROM RAT UTERUS
- EFFECTS OF NONSPECIFIC SMOOTH MUSCLE RELAXANTS ON CALCIUM-UPTAKE BY MICROSOMAL FRACTION AND THEIR INHIBITORY ACTION IN RABBIT TAENIA COLI
- POSSIBLE MECHANISMS OF STIMULATORY ACTION OF PAPAVERINE ON CALCIUM-UPTAKE BY RAT UTERINE MICROSOMAL FRACTION
- Adrenaline produces the relaxation of guinea-pig airway smooth muscle primarily through the mediation of β_2-adrenoceptors
- Phospholipase C Inhibitors Suppress Spontaneous Mechanical Activity of Guinea Pig Urinary Bladder Smooth Muscle(Pharmacology)
- The β_2- and β_3-Adrenoceptor-Mediated Relaxation Induced by Fenoterol in Guinea Pig Taenia Caecum
- The Entering of Indium-111 and Iron-59 into the Hepatocytes from Partially Hepatectomized Rats Differ from That of Gallium-67(Biochemistry/Molecular Biology)
- Effect of Restraint and Footshock Stress and Norepinephrine Treatment on Gastric Emptying in Rats
- The β_3-Adrenoceptor-Mediated Relaxation Induced by Epinephrine in Guinea Pig Taenia Caecum
- Partial Agonistic Effects of Carteolol on Atypical β-Adrenoceptors in the Guinea Pig Gastric Fundus
- H2 Receptor-Mediated Positive Inotropic Effect of Histamine in Neonatal Guinea-Pig Left Atria
- RELATIONSHIP BETWEEN INTRINSIC ACTIVITY OF β-ADRENOCEPTOR AGONIST AND AMOUNT OF SPARE RECEPTORS IN GUINEA PIG TAENIA CAECUM
- PHARMACOLOGICAL PROPERTIES OF ACETYLCHOLINE RECEPTOR IN MOLLUSCAN SMOOTH MUSCLE
- INTERACTIONS OF SOME PARTIAL AGONISTS WITH BETAADRENOCEPTOR IN GUINEA-PIG TAENIA CAECUM
- Effects of aging on α_1-adrenoceptor mechanisms in the isolated mouse aortic preparation
- α_1-Adrenoceptors in the Guinea Pig Thoracic Aorta
- Update on Angiogenic Potential of Neural Stem Cells
- A DIFFERENCE IN PHARMACOLOGICAL ACTION OF R (+) AND S (-) ISOMERS OF BEFUNOLOL, BETA-ADRENOCEPTOR BLOCKER
- INTERACTION OF THE PARTIAL AGONISTS WITH BETA-ADRENOCEPTOR IN GUINEA-PIG TAENIA CAECUM
- BETA-ADRENOCEPTOR MECHANISMS IN GUINEA PIG TAENIA CAECUM
- A difference in alpha-adrenoceptor mechanisms in vasa deferential isolated from young and old rats.
- Variation in Sensitivity of .ALPHA.1-Adrenoceptor Stimulants and .ALPHA.1-Adrenoceptor Mechanisms in Rabbit Arteries.
- A Difference in Receptor Mechanisms for Muscarinic Full and Partial Agonists.
- Effect of ageing on .ALPHA.1A-adrenoceptor mechanisms in rabbit isolated bronchial preparations.
- INTERACTIONS OF R (+)- AND S (-)-ISOMERS OF BETA-ADRENERGIC PARTIAL AGONISTS, BEFUNOLOL AND CARTEOLOL, WITH BETAADRENOCEPTORS
- Characterization of Subtype of Propylbenzilylcholine Mustard (PrBCM)-Sensitive and-Resistant Muscarinic Cholinoceptors in Guinea Pig Ileal Muscle.
- Involvement of .BETA.3-Adrenoceptor in the Relaxation Response in Guinea Pig Taenia Caecum.
- A possible mechanism in interaction of a partial agonist with .BETA.-adrenoceptor in guinea-pig taenia caecum: Effects of Gpp(NH)p on its two different binding sites.
- Evidence for release of prostaglandin F2.ALPHA. in contractile response of guinea pig trachea to norepinephrine.
- Effect of aging on the response of guinea pig trachea to isoprenaline.
- Update on Angiogenic Potential of Neural Stem Cells