Binding Characteristics of α_1-Adrenoceptors in Bovine Prostate Using a Radioligand Binding Assay
スポンサーリンク
概要
- 論文の詳細を見る
Binding characteristics of α_1-adrenoceptors in the bovine prostate were examined using a radioligand binding assay. [^3H] Bunazosin was used as a radioligand. The optimal incubation conditions for the radioligand binding assay were determined : incubation time (30 min), protein concentration (0.2 mg/tube) and temperature (30℃). Scatchard plots for α_1-adrenoceptors in bovine prostates were linear and the K_d and B_<max> values were 0.61 nM and 49.8 fmol/mg protein, respectively. The pK_i value of terazosin was significantly higher than those of prazosin, bunazosin or phentolamine in the bovine prostate. Since this radioligand binding assay using [^3H] bunazosin demonstrated the presence of α_1-adrenoceptors in bovine prostates, this method is useful for the assessment of α_1-blockers of new chemicals synthesized for the treatment of the benign prostatic hyperplasia.
- 公益社団法人日本薬学会の論文
著者
-
Nagatomo T
Dep. Of Pharmacology Fac. Of Pharmaceutical Sciences Niigata Univ. Of Pharmacy And Applied Life Scie
-
TSUCHIHASHI HIROSHI
Department of Surgery, Department of Medicine, Shiga University of Medical Science
-
MARUYAMA Keiko
Department of Pharmacology, Niigata College of Pharmacy
-
Kinami Junji
Department Of Pharmacology Niigata College Of Pharmacy
-
Maruyama Keiko
Department Of Pharmacology Niigata College Of Pharmacy
-
Maruyama Keiko
Department Of Neurology Suwa Red Cross Hospital
-
NAGATOMO Takefumi
Department of Pharmacology, Niigata College of Pharmacy
-
Nagatomo Takafumi
Department Of Pharmacology Faculty Of Pharmaceutical Sciences Niigata University Of Pharmacy And App
-
Tsuchihashi Hiroshi
新潟薬科大学 薬理
-
Tsuchihashi Hiroshi
Department Of Pharmacology Niigata College Of Pharmacy
-
Namikawa Tomoko
Biological Res. Dep. Sawai Pharmaceutical Co. Ltd.
-
Maruyama Keiko
Department Of Clinical Laboratory Science Kanazawa University Graduate School Kanazawa University
関連論文
- 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
- Assessment of Binding Affinity to 5-Hydroxytryptamine 2A (5-HT_) Receptor and Inverse Agonist Activity of Naftidrofuryl : Comparison With Those of Sarpogrelate
- Pharmacological Differences between Liu-Jun-Zi-Tang, a Traditional Chinese Herbal Medicine, and Domperidone on Isolated Guinea-Pig Ileum(Pharmacology)
- Actions of Liu-Jun-Zi-Tang, a Traditional Chinese Herbal Medicine, on Exogenous and Endogenous Opioid Systems in Isolated Guinea Pig Ileum
- 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
- Inverse Agonist Activity of Sarpogrelate, a Selective 5-HT_-Receptor Antagonist, at the Constitutively Active Human 5-HT_ Receptor
- Assessment of Affinities and Dissociation Potencies of Several 5-HT_2 Antagonists to and from M_2 Muscarinic Receptor in Rat Heart Membranes(Pharmacology)
- Molecular modeling of the interaction of sarpogrelate and human 5-HT_, 5-HT_ and 5-HT_ receptor subtypes
- Chronic Myocarditis and Angiotensin-II Receptor Antagonist (TCV-116)
- Changes in α_1-and β_1-Adrenergic Receptors and Calcium Ion Binding Sites in the Fetal Myocardium of Spontaneously Hypertensive Rats (SHR)
- Internalization of Constitutively Active N111G Mutant of AT1 Receptor Induced by Angiotensin II–Receptor Antagonists Candesartan, Losartan, and Telmisartan: Comparison With Valsartan
- Mutational Analysis of the α_-Adrenergic Receptor Binding Pocket of Antagonists by Radioligand Binding Assay(Pharmacology)
- Amino Acids of the Human α_-Adrenergic Receptor Involved in Antagonist Binding
- Asp125 and Thr130 in Transmembrane Domain 3 Are Major Sites of α_-Adrenergic Receptor Antagonist Binding(Pharmacology)
- Differential Inhibition by Oxygen Radicals of Vasoactive Amines-Induced Contractions in the Porcine Coronary Artery(Pharmacology)
- Beta-Blockers Show Inverse Agonism to a Novel Constitutively Active Mutant of β_1-Adrenoceptor
- 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
- Identification of Amino Acid Residues Important for Sarpogrelate Binding to the Human 5-Hydroxytryptamine_ Serotonin Receptor
- Site-Directed Mutagenesis of the Serotonin 5-Hydroxytryptamine_ Receptor : Identification of Amino Acids Responsible for Sarpogrelate Binding(Pharmacology)
- Effects of Sarpogrelate, a Novel 5-HT_2 Antagonist, on 5-HT-Induced Endothelium-Dependent Relaxations in Porcine Coronary Artery
- Assessment of Affinity and Dissociation Ability of a Newly Synthesized 5-HT_2 Antagonist, AT-1015: Comparison With Other 5-HT_2 Antagonists
- Binding Affinity of a Newly Synthesized 5-HT_2 Antagonist, AT-1015(N-[2-[4-(5H-Dibenzo[a, d]cyclohepten-5-ylidene)-piperidino]ethyl]-1-formyl-4-piperidinecarboxamide Monohydrochloride Monohydrate), in the Rabbit Platelet Membrane
- Abnormal fatty acid matabolism in patients with coronary vasospasm
- Identification of a Key Amino Acid of the Human 5-HT2B Serotonin Receptor Important for Sarpogrelate Binding
- Postprandial Hyperglycemia After a Gastrectomy and the Prediabetic State : A Comparison Between a Distal and Total Gastrectomy
- SIMVASTATIN REDUCES INSULIN-LIKE GROWTH FACTOR-1 SIGNALING IN DIFFERENTIATING C2C12 MOUSE MYOBLAST CELLS IN AN HMG-CoA REDUCTASE INHIBITION-INDEPENDENT MANNER
- Assessment of β_2- and β_3-Adrenoceptors in Rat White Adipose Tissues by Radioligand Binding Assay
- Effects of Chronic Administration of Bopindolol on the Binding Characteristics of Cardiac α_-, α_-, β_1- and β_2-Adrenoceptor Subtypes in Cardiac Muscles of Spontaneously Hypertensive Rats (SHR)
- Anti-obesity and Anti-diabetic Activities of a New β_3 Adrenergic Receptor Agonist, (S)-(Z)-[4-[[1-[2-[(2-Hydroxy-3-phenoxypropyl)]amino]athyl]-1-propenyl]phenoxy] Acetic Acid Ethanedioic Acid (SWR-0342SA), in KK-A^y Mice
- Molecular Characterization of Pharmacological Properties and Selectivity of SWR-0315NA for β_3-Adrenoceptors (Pharmacology)
- Structure-activity relationship studies of phenoxypropanolamine derivatives for β_3-adrenergic activity
- β-Adrenoceptors: Three-Dimensional Structures and Binding Sites for Ligands
- 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
- Affinity for [^3H]Iloprost Binding Sites and cAMP Synthesis Activityof a 3-Oxa-methano Prostaglandin I_1Analog, SM-10906,in Human Platelets and Endothelial Cells
- Slow Dissociation of Long-Acting Ca^ Antagonist Amlodipine from ^3H-PN200-110 Binding Sites in Membranes of Rat Hearts and Brains
- Multiple Brain Tumors of Diffuse Large B Cell Lymphoma in a Patient with Waldenstrom's Macroglobulinemia/Lymphoplasmacytic Lymphoma : PCR and DNA Sequence Analysis Show Evidence of Differences in Clonality of the Two B Cell Malignancies
- cAMP-Independent Chloride Secretion Activated by a Vasoactive Intestinal Peptide in a Monolayer Culture of Human Bronchinal Epithelial Cells
- Beta-blocking Potency and Selectivity of Bopindolol and Its Two Metabolites for β_1-and β_2-Adrenergic Receptors as Assessed by Radioligand Binding Assay
- Binding Characteristics of [^3H] Ketanserin for Serotonin-2 Receptor in the Rabbit Platelet
- Binding Characteristics of α_1-Adrenoceptors in Bovine Prostate Using a Radioligand Binding Assay
- MCI-9042 : High Affinity for Serotonergic Receptors as Assessed by Radioligand Binding Assay
- Three Binding Sites of ^I-Iodocyanopindolol, i.e. β_1,β_2-Adrenergic and 5HT_-Serotonergic Receptors in Rat Brain Determined by the Displacement and Scatchard Analysis
- Binding Characteristics of ^I-Iodocyanopindolol to β-Adrenergic Receptors : Biphasic Scatchard Plts. II. : Effects of Selective Antagonists(Pharmacological)
- Studies on the Metabolic Fate of Lamivudine (III): Absorption, Metabolism and Excretion of Lamivudine in Dogs
- Studies on the Metabolic Fate of Lamivudine (II): Tissue Distribution, Transfer into Fetus and Milk, Plasma Protein Binding and Distribution to Erythrocytes of Lamivudine in Rats
- Studies on the Metabolic Fate of Lamivudine (I): Absorption, Metabolism and Excretion of Lamivudine in Rats
- Edaravone Improves the Survival of Rats Subjected to Hemorrhagic Shock Without Resuscitation
- Bone fracture in physically disabled children attending schools for handicapped children in Japan
- BINDING ASSAY OF ALPHA-1 ADRENOCEPTOR SUBTYPES : RELATIONSHIP BETWEEN BIPHASIC SCATCHARD PLOT AND DISPLACEMENT CURVE
- Alpha-blocking Potencies of Antihypertensive Agents (Prazosin, Terazosin, Bunazosin, SGB-1534 and Ketanserin) Having with Quinazoline or Quinazolinedione as Assessed by Radioligand Binding Assay Methods in Rat Brain
- BINDING CHARACTERISTICS OF 3H-DIHYDROALPRENOLOL TO β-ADRENOCEPTORS OF RAT HEART TREATED WITH NEURAMINIDASE
- Multiple Sclerosis with Open-Ring Enhancement in the Cerebrum and Spinal Cord
- Engineered Mutation of Some Important Amino Acids in Angiotensin II Type 1 (AT_1) Receptor Increases the Binding Affinity of AT_1-Receptor Antagonists
- Internalization of Constitutively Active N111G Mutant of AT_1 Receptor Induced by Angiotensin II-Receptor Antagonists Candesartan, Losartan, and Telmisartan : Comparison With Valsartan
- EFFECTS OF NEURAMINIDASE AND DEOXYRIBONUCLEASE ON THE β-ADRENERGIC RECEPTORS IN RAT HEART
- Effect of Site-directed Mutagenesis in Some Important Amino Acids of AT_1 Receptor on the Binding Affinity of the Agonist and Antagonists
- Selectivity of Valsartan to the Human Angiotensin II Type One Receptors as Assessed by Binding Affinity, Functional Activity and Molecular Modeling
- Pharmacological and Molecular Studies for the Regulation of β_1-Adrenergic Receptors that Reveals Activation and Inactivation
- Two case reports of inherited antithrombin deficiency : a novel frameshift mutation and a large deletion including all seven exons detected using two methods
- Nipradilol Displays a Unique Pharmacological Profile of Affinities for the Different α1-Adrenoceptor Subtypes
- Assessment of Ca2+-Antagonistic Effects of SM-6586 and Its Isomers, Novel 1, 4-Dihydropyridine Derivatives, by Radioligand Binding Assay
- Comparison of α1-Adrenoceptors between Rat Brain and Spleen
- Characteristics of 125I-lodocyanopindolol Binding to β-Adrenergic and Serotonin-1B Receptors of Rat Brain: Selectivity of β-Adrenergic Agents
- Mechanism of Inverse Agonist Action of Sarpogrelate at the Constitutively Active Mutant of Human 5-HT2A Receptor Revealed by Molecular Modeling
- Influence of polymeric effectors on binding of 3H-dihydroalprenolol to .BETA.-adrenergic receptor of rat brain.
- Beneficial effects of diltiazem on the ischemic derangements of the myocardial metabolism assessed by 31P-NMR in the isolated perfused rat heart.
- Binding characteristics of 3H-CGP12177 to .BETA.-adrenoceptors in rat myocardial membranes.
- Beta-Blockers Show Inverse Agonism to a Novel Constitutively Active Mutant of .BETA.1-Adrenoceptor
- Selectivity of bunitrolol for .BETA.1- and .BETA.2-adrenergic receptors and 5HT1B-receptors: Assessment by biphasic scatchard plots and biphasic displacement curve analysis with 125I-iodocyanopindolol and 3H-CGP12177.
- Effects of bunitrolol on adrenergic and serotonergic receptors.
- Binding characteristics of 3H-dihydroalprenolol to .BETA.-adrenergic receptors of rat brain: Influence of lectins.
- Beta-receptor blocking potencies of the three newly synthesized .BETA.-adrenergic antagonists (S-596,K-351,N-696) as assessed with the radioligand binding assay method in rat cardiac muscle membrane treated with neuraminidase.
- Binding characteristics of 3H-dihydroalprenolol to .BETA.-adrenergic receptors of rat brain: Influence of exo- and endoglycosidases and glycopeptidase.
- Displacement by .ALPHA.-adrenergic agonists and antagonists of 3H-prazosin bound to the .ALPHA.-adrenoceptors of the dog aorta and the rat brain.
- Effects of deoxyribonuclease I and neuraminidase treatments on the specific binding of 3H-prazosin and 3H-quinuclidinyl benzilate (3H-QNB) to .ALPHA.-adrenergic and muscarinic receptors in rat myocardial membranes.
- The increase in .BETA.-adrenergic receptors in lymphocytes following treatment with xamoterol.
- Calcium Channel Blocking Properties of SM-6586 in Rat Heart and Brain as Assessed by Radioligand Binding Assay.
- Alpha-1 Adrenoceptor Subtypes in Canine Aorta.