Antispasmodic Action of 1-Diethylaminoethyl-3-(p-methoxybenzyl)-2-quinoxalone (P 201-1) and Its Inhibitory Effect on Cyclic 3', 5'-Nucleotide Phosphodiesterase (PDE) Activity

スポンサーリンク

概要

• 論文の詳細を見る

• The action on various smooth muscle of 1-diethylaminoethyl-3-(p-methoxybenzyl)-2-quinoxalone (P 201-1) and its inhibitory effect on the phosphodiesterase (PDE) activity in the supernate prepared from the rat ileum, cerebral cortex, and liver were investigated by comparison with those of papaverine. P 201-1 had more potent antispasmodic action on the isolated guinea pig ileum, gastric smooth muscle and uterus of the rat, rabbit ileum and so on than papaverine, and showed little influence upon the autonomic nervous system. P 201-1 inhibited the PDE activity in the supernate prepared from the rat ileum, cerebral cortex, and liver. The Ki values of P 201-1 for the supernate of the ileum, cerebral cortex, and liver were 1370,700,and 650 μM, respectively, and the values were 5-10 times those of papaverine. The inhilitory effect of P 201-1 on PDE from the rat ileum or cerebral cortex was competitive and that from the liver noncompetitive, and the type of inhibition of P 201-1 was different from that of papaverine in each tissue. When the influence of Mg^<2+> concentration on the inhibitory effect of P 201-1 was examined, the liver PDE inhibition of P 201-1 occurred in a different way from the ileum or cerebral cortex PDE inhibition, and completely disappeared at high concentration of Mg^<2+> (10 mM).

• 公益社団法人日本薬学会の論文
• 1975-04-25

著者

• 小澤 光

  Pharmaceutical Institute Tohoku University

• 林 昌亮

  Department of Biological Science, Pharmaceutical Laboratory, Hoechst Japan Limited

• 林 昌亮

  Department Of Biological Science Pharmaceutical Laboratory Hoechst Japan Limited

関連論文

• General Pharmacological Actions of N-Acetoacetyl-3-hydroxytyrosine
• Ganglion Blocking Activity of Amidinothiocholine Derivatives
• Effects of Hexylguanidine on Cardiovascular System and Blood Glucose
• Cocaine-like Action of Hexylguanidine on Smooth Muscle Preparations
• Antagonistic Phenomena between Crystalline Tetrodotoxin and Guanidines on Sympathetic Nervous Systems
• Structure-activity Relationship of Alkylguanidines on Smooth Muscle Organs
• Biochemical Studies on Quinone Derivatives. II. Effects of Naturally Occurring Benzoquinone Derivatives on the Respiration of Intact Rat Liver Mitochondria.
• Biochemical Studies on Quinone Derivatives. I. Effects of Naturally Occurring Benzoquinone Derivatives on Mitochondrial Preparations
• Studies on 3,7-Dimethyl-1-(5-oxo-hexyl)-xanthine (BL 191). III. Effects of BL 191 and Its Metabolites on Cyclic 3', 5'-Nucleotide Phosphodiesterase and Lipolytic Activities
• Antispasmodic Action of 1-Diethylaminoethyl-3-(p-methoxybenzyl)-2-quinoxalone (P 201-1) and Its Inhibitory Effect on Cyclic 3', 5'-Nucleotide Phosphodiesterase (PDE) Activity
• Pharmacokinetic Investigation of 17α-Desoxymethasone (A 41 304) in Rats
• Studies on 3,7-Dimethyl-1-(5-oxo-hexyl)-xanthine (BL 191). I. Cyclic 3', 5'-Nucleotide Phosphodiesterase (PDE) and the Inhibitory Effect of BL 191 on PDE in Rat Brain and Heart
• A Simple Method for Evaluating Analgesic Efficacy of Non-Steroidal Anti-Inflammatory Drugs
• Syntheses and Activities of Bioquinone Substances. I. Total Syntheses of Rhodoquinones
• Copper DL-Methionine, a New Anthelmintic for Swine Lung Worm. The Action of Copper DL-Methionine on Lung Worms.
• Activation of Adenyl Cyclase and Adenosine 3', 5'-Monophosphate Phosphodiesterase in Rat Brain Synaptosomes
• The Stimulation of Synaptosomal Adenyl Cyclase Activity by the Supernatant from Rat Brain Cerebral Cortex
• Endogenous Inhibitor (s) in Rat Liver of Dopamine β-Hydroxylase
• Pharmacological Studies of Troponoids. IV. Antipyretic Analgesic, and Anti-inflammatory Activities of Aminotroponoids
• Pharmacological Studies on Guanethidine Derivatives. IV. Adrenergic Neurone Blocking Action of 2,3,4,5-Tetrahydro-1H-2-benzazepine-2-carboxamidine Sulfate.
• Studies on 3,7-Dimethyl-1-(5-oxo-hexyl)-xanthine (BL 191). II. Effect of BL 191 on Lipolysis in Rat Epididymal Adipose Tissue
• Biochemical Studies on Benzoquinone Derivatives. III. Effects of Dihydroxythymoquinone on Rat Liver Mitochondria in the Electron Transport System.
• The Adrenergic Neurone Blocking Action of [2-(Methylphenylamino)-ethyl] guanidine Sulfate. II.
• Studies on Proteases in Submaxillary Gland. I. Fractionation and General Characteristics of Rat Submaxillary Proteases.
• Pharmacological Properties of Heterocyclic Amidine Derivatives. II. Pharmacological Studies of Phenylguanylpiperazine Derivatives
• Dopamineの摘出ラット左心房標本に対する作用
• Lithium塩の薬理学的研究(第3報)　―塩化リチウム(LiCl)の循環系および平滑筋におよぼす一般薬理作用―

もっと見る 閉じる

スポンサーリンク