PHARMACOLOGY OF dl-5-METHYL-8-(2-HYDROXY-3-t-BUTYLAMINOPROPOXY) COUMARIN HYDROCHLORIDE (CS-359), A NEW β-ADRENERGIC BLOCKING AGENT
スポンサーリンク
概要
- 論文の詳細を見る
β-Adrenergic blocking activity and other pharmacological properties of CS-359, 5-methyl-8-(2-hydroxy-3-t-butylaminopropoxy) coumarin were compared with those of propranolol. CS-359 inhibited the positive chronotropic and the smooth muscle relaxing responses to isoproterenol. The cardiac effect of stellate ganglion stimulation in anesthetized dogs was also abolished. CS-359 given orally to conscious dogs inhibited the positive chronotropic response to isoproterenol given i.v. The β-adrenergic blocking activity of this compound was 2 to 3 times more potent than that of propranolol, both of which were devoid of any intrinsic stimulant activity. Aconitine and ouabain-induced arrhythmias in anesthetized dogs were protected by CS-359. As to local anesthetic action on frog sciatic nerve and guinea-pig cornea, CS-359 had one-tenth the activity of propranolol. Concerning percent reduction of the maximum rate of rise of action potential recorded intracellularly from the ventricular muscle fiber, CS-359 was 3 times less potent than propranolol. It reduced heart rate but had only minor effects on the blood pressure and respiration in anesthetized dogs. These data suggest that CS-359 is a more specific β-adrenergic blocking agent with a greater potency and a less cardiac depression than propranolol.
- 社団法人 日本薬理学会の論文
著者
-
KOIKE HIROYUKI
Central Research Laboratories, Sankyo Co., Ltd.
-
Oshima Takeshi
Department Of Otolaryngology Tohoku University School Of Medicine
-
KUMAKURA Seiji
Central Research Laboratories, Sankyo Co., Ltd.
-
Nakayama Koichi
Department Of Cellular And Molecular Pharmacology Graduate School Of Pharmaceutical Sciences Univers
-
Koike Hiroyuki
Central Research Laboratories Sankyo Co. Ltd.
-
NAKAYAMA Koichi
Department of Pharmacology, Tohoku University School of Medicine
関連論文
- A novel KCNQ4 one-base deletion in a large pedigree with hearing loss : implication for the genotype-phenotype correlation
- Involvement of Cyclooxygenase-2 in Synergistic Effect of Cyclic Stretching and Eicosapentaenoic Acid on Adipocyte Differentiation
- Expression of Xeroderma Pigmentosum Group G (XPG) in Sporadic Breast Carcinoma
- Long-Term Follow-up of Obstructive Sleep Apnea Syndrome Following Surgery in Children and Adults
- A Case Report of Sinonasal Teratocarcinosarcoma
- Stable Expression of the Motor Protein Prestin in Chinese Hamster Ovary Cells(Bioengineering)
- Role of Na^+/Ca^ Exchanger-Mediated Ca^ Entry in Pressure-Induced Myogenic Constriction in Rat Posterior Cerebral Arteries
- (+)-[^3H] Isradipine and [^3H] Glyburide Bindings to Heart and Lung Membranes From Rats With Monocrotaline-Induced Pulmonary Hypertension
- A Case Report of Salivary Duct Carcinoma
- A Case of Basal Cell Adenocarcinoma of the Parotid Gland
- A Case of Leiomyosarcoma of the Sphenoid Sinus
- Surgical Criteria for Obstructive Sleep Apnea Syndrome Based on Localization of Upper Airway Collapse during Sleep : A Preliminary Study
- A Press-Through-Pack in the Larynx
- Effects of Long-Term Low-Dose Macrolide Administration on Neutrophil Recruitment and IL-8 in the Nasal Discharge of Chronic Sinusitis Patients
- Comparison of Complications between Endoscopic Sinus Surgery and Caldwell-Luc Operation
- ANTIHYPERTENSIVE ACTIVITY OF BUCUMOLOL, A β-ADRENERGIC BLOCKING AGENT, IN SPONTANEOUSLY HYPERTENSIVE RATS
- Masked Patulous Eustachian Tube : An Important Diagnostic Precaution Before Middle Ear Surgery
- Inhibition of Untransformed Prostaglandin H2 Production and Stretch-Induced Contraction of Rabbit Pulmonary Arteries by Indoxam, a Selective Secretory Phospholipase A2 Inhibitor
- Contractile Potentiation by Endothelin-1 Involves Protein Kinase C-δ Activity in the Porcine Coronary Artery
- Impedance Cardiography for the Assessment of Cardiac Function During Exercise : SYMPOSIUM ON EXERCISE TESTINGS OF HEART DISEASE
- Glibenclamide-Sensitive Hypotension Produced by Helodermin Assessed in the Rat
- Flow-Dependent Regulation of Nitric Oxide Formation in the Isolated Canine Mesenteric Arterial Bed
- Flow Regulates Vasodilator Responses to Acetylcholine in the Isolated Canine Mesenteric Arterial Bed
- Differential involvement of α_1-adrenoceptors in vasoconstrictor responses to cooling in mouse plantar arteries in vitro and in vivo
- Role of Na+/Ca2+ Exchanger–Mediated Ca2+ Entry in Pressure-Induced Myogenic Constriction in Rat Posterior Cerebral Arteries
- Distinct Roles of Protein Kinase C Isoforms in Myogenic Constriction of Rat Posterior Cerebral Arteries
- Evidence for Protein Kinase C-Mediated Activation of Rho-Kinasein a Porcine Model of Coronary Artery Spasm
- ^Mg (d,p)^Mg Reactions at 3.1 and 3.5 MeV
- Involvement of Different Activator Ca^ in the Rate-Dependent Stretch-Induced Contractions of Canine Basilar Artery
- Facilitation of L-type Ca^ Currents by Fluid Flow in Rabbit Cerebral Artery Myocytes
- Functional Studies on Blockade by Neosurugatoxin of Nicotinic Receptors in Nitroxidergic and Sensory Nerve Terminals and Intramural Ganglionic Cells
- Effects of Beta Blockers on Cardiac Function and Myocardial Oxygen Consumption in the Isolated Supported Heart Preparation of the Dog
- Sensorineural Hearing Loss Associated with Byler Disease
- Two Cases of Plunging Ranula Managed by the Intraoral Approach
- Isobaric Analogue Resonances in ^Al Studied with the ^Mg (p, p) and ^Mg (p, γ) Reactions
- Effects of DX-9065a, an Inhibitor of Factor Xa, on Ellagic Acid-Induced Plantar Skin Thrombosis Assessed in Tetrodotoxin- and N^ω -Nitro-L-Arginine- Treated Rats
- ANTIARRHYTHMIC ACTIVITY OF DEXTRO- AND LEVO-ISOMERS OF 5-METHYL-8-(2-HYDROXY-3-T-BUTYLAMINO-PROPOXY) COUMARIN HYDROCHLORIDE (BUCUMOLOL), A β-ADRENERGIC BLOCKING AGENT, ON ACONITINE-INDUCED ATRIAL AND OUABAIN-INDUCED VENTRICULAR ARRHYTHMIAS IN DOGS
- PHARMACOLOGY OF dl-5-METHYL-8-(2-HYDROXY-3-t-BUTYLAMINOPROPOXY) COUMARIN HYDROCHLORIDE (CS-359), A NEW β-ADRENERGIC BLOCKING AGENT
- EFFECTS OF ANISOTROPINE METHYLBROMIDE (VALPIN®) AND ITS MIXTURE WITH SULPYRINE ON VOCALIZATION RESPONSE AND SPASM OF INTESTINE INDUCED BY ACETYLCHOLINE IN DOGS
- Two Distinct Effects of cGMP on Cytosolic Ca^ Concentration of Rat Pancreatic β-Cells
- SELECTIVE ABOLITION OF Ca-DEPENDENT RESPONSES OF SMOOTH AND CARDIAC MUSCLES BY FLUNARIZINE
- ROLE OF CALCIUM IONS AND ENDOTHELIUM IN THE STRETCH-INDUCED CONTRACTILE ACTIVATION OF VASCULAR TISSUES
- Inhibition of Untransformed Prostaglandin H_2 Production and Stretch-Induced Contraction of Rabbit Pulmonary Arteries by Indoxam, a Selective Secretory Phospholipase A_2 Inhibitor
- Correct Diagnosis of Warthin Tumor in the Parotid Gland with Dynamic MRI
- Role of Secretory Phospholipase A2 in Rhythmic Contraction of Pulmonary Arteries of Rats With Monocrotaline-Induced Pulmonary Arterial Hypertension
- Role of Secretory Phospholipase A_2 in Rhythmic Contraction of Pulmonary Arteries of Rats With Monocrotaline-Induced Pulmonary Arterial Hypertension
- ANTIARRHYTHMIC POTENCY OF N-PROPYL AJMALINE WITH UNTOWARD RESPONSE OF VENTRICULAR FIBRILLATION IN EXCESS DOSE