Potentiation of Barbiturate-Induced Narcosis by N,N'-(or N,S-) Diallyl-Substituted Derivatives of Phenobarbital, Amobarbital and Thiopental in Mice(Pharmacological)

スポンサーリンク

概要

• 論文の詳細を見る

• N-(or S-) Allyl derivatives of phenobarbital (PheB), amobarbital (AB) and thiopental (TP) were prepared, and their pharmacological activities (hypnotic activity and anticonvulsant activity against pentylenetetrazol-induced seizures) were investigated in mice. N-Monoallyl-substituted derivatives (MAPheB, MAAB and MATP) of PheB, AB and TP exhibited hypnotic and anticonvulsant activities. W,S-Diallylthiopental (N,S-DATP) possessed hypnotic activity, but failed to show anticonvulsant activity even at a dose of 250 mg/kg (i.p.). N,N'-Diallyl-substituted derivatives (DAPheB, DAAB and DATP) were devoid of not only the hypnotic activity, but also-the anticonvulsant activity. The interactions of these allyl derivatives with various barbiturates were then studied in order to characterize whether the allyl compounds have antagonistic or potentiating properties. MAPheB, DAPheB, MAAB and DAAB showed dose-dependent potentiation of the sleep induced by the corresponding mother compounds. All the allyl compounds tested prolonged the pentobarbital-induced sleeping time more than 7-to 19-fold as compared with the control. MAAB markedly prolonged the PheB-induced sleeping time by 25-fold, but it did not potentiate the barbital-induced sleep. These results indicate that N-(or S-) allyl derivatives of PheB, AB and TP interact differently with the barbiturates.

• 公益社団法人日本薬学会の論文
• 1987-02-25

著者

• 渡辺 和人

  Department of Hygienic Chemistry, Faculty of Pharmaceutical Sciences, Hokuriku University

• 山本 郁男

  Department of Hygienic Chemistry, Faculty of Pharmaceutical Sciences, Hokuriku University

• 木村 敏行

  Department of Hygienic Chemistry, Faculty of Pharmaceutical Sciences, Hokuriku University

• HO Ing

  University of Mississippi Medical Center

• HO Ing

  Department of Pharmacology and Toxicology, University of Mississippi Medical Center

• 舘岡 裕二

  Shinshin Chemical Industry Co. Ltd.

• Ho Ing

  ミシシッピ大学医学部薬毒理学教室

• Ho Ing

  Department Of Pharmacology & Toxicology University Of Mississippi Medical Center

• Tateoka Yuji

  Department Of Hygienic Chemistry Faculty Of Pharmaceutical Sciences Hokuriku University

• 舘岡 裕二

  Department of Hygienic Chemistry, School of Pharmacy, Hokuriku University

• 舘岡 裕二

  Department Of Hygienic Chemistry Faculty Of Pharmaceutical Sciences Hokuriku University

関連論文

• Involvement of CYP2C in the Metabolism of Cannabinoids by Human Hepatic Microsomes from an Old Woman
• 新規催眠物質N^3-Phenacyluridineの活性代謝物を用いた新規ウリジン受容体の発見とその作用メカニズムの解析並びに創薬への応用研究
• 抹消組織におけるウリジン誘導体の結合活性 - 心臓における部位特異性
• Synthesis and Hypnotic and Anti-Human Immunodeficiency Virus-1 Activities of N^3-Substituted 2'-Deoxy-2'-fluorouridines
• Formation of p-Hydroxycocaine from Cocaine by Hepatic Microsomes of Animals and Its Pharmacological Effects in Mice
• 3,4,5-Trimethoxyphenylacetaldehyde, an Intermediate Metabolite of Mescaline, Is a Substrate for Microsomal Aldehyde Oxygenase in the Mouse Liver
• Formation of Carbon Monoxide during Mouse Hepatic Microsomal Oxidative Metabolism of Cannabidiol ; Identification and Determination
• Synthesis and Pharmacological Effects in Mice of Halogenated Cannabinol Derivatives
• In Vitro Metabolic Formation of a New Metabolite, 6β-Hydroxymethyl-Δ^9-tetrahydrocannabinol from Cannabidiol through an Epoxide Intermediate and Its Pharmacological Effects on Mice
• Synthesis of N^3-Substituted Uridine and Related Pyrimidine Nucleosides and Their Antinociceptive Effects in Mice
• Possible Existence of a Novel Receptor for Uridine Analogues in the Central Nervous System Using Two Isomers, N^3-(S)-(+)-and N^3-(R)-(-)-α-Hydroxy-β-phenethyluridines
• Hypnotic Action of N^3-Substituted Arabinofuranosyluracils on Mice
• Cross-Reactivity of Various Tetrahydrocannabinol Metabolites with a Monoclonal Antibody against Tetrahydrocannabinolic Acid
• Synthesis and Central Nervous System Depressant Effects of N^3-Substituted 2', 3'-O-Isopropylideneuridines
• Pharmacologica Efects in Mice of Anandamide and Its Related Fatty Acid Ethanolamides, and Enhancement of Cataleptogenic Effect of Anandamide by Phenylmethylsulfonyl Fluoride
• Synthesis and Sedative-Hypnotic Effects of N^3-Allyl-and N^1-Allyl-5,6-substituted 2-Thiouracil Derivatives in Mice
• Cytochrome P450 Isozymes Catalyzing the Hepatic Microsomal Oxidation of 9-Anthraldehyde to 9-Anthracene Carboxylic Acid in Adult Male Rats
• Comparison of Pharmacological Effects of Tetrahydrocannabinols and Their 11-Hydroxy-Metabolites in Mice
• In Vivo and in Vitro Metabolism of Cannabidiol Monomethyl Ether and Cannabidiol Dimethyl Ether in the Guinea Pig : : On the Formation Mechanism of Cannabielsoin-Type Metabolite from Cannabidiol
• Pharmacological Activities in the Mouse of Δ^9-Tetrahydrocannabinol Metabolites Oxidized at the 8-Position
• 大麻主成分Δ^9-Tetrahydrocannabinol(Δ^9-THC)およびCannabidiol(CBD)のPentobarbital睡眠および肝薬物代謝酵素系に及ぼす影響-マウスにおける性差
• Synthesis of 8α, 9α- and 8β, 9β-Epoxyhexahydrocannabinols
• Suppression of Liver Microsomal Drug-Metabolizing Enzyme Activities in Adult Female Rats Pretreated with Cannabidiol
• Compertitive Inhibition of Δ^8-Tetrahydrocannabinol and Its Active Metabolites for Cannabinoid Receptor Binding
• The Potent Depressant Effects of N^3-Phenacyluridine in Mice
• Preparation and Pharmacological Evaluation of N^3-Substituted Thymidine Derivatives as Central Deprassants
• ウラシル誘導体の合成及びマウスにおける中枢抑制作用新鎮静・催眠薬の開発に関する研究(第2報)
• Central Nervous System Depressant Effects of N^3-Substituted Derivatives of Deoxyuridine in Mice
• STRUCTURE-ACTIVITY RELATIONSHIP OF URIDINE DERIVATIVES FOR HYPNOTIC ACTIVITY
• Potentiating Effects of N^1,N^3-Diallyluracil, N^1,N^3-Diallylthymine and N^1,N^3-Diallyl-6-methyluracil on Pentobarbital-Induced Sleep and Diazepam-Induced Motor Incoordination(Pharmacological,Chemical)
• Potentiation of Barbiturate-Induced Narcosis by N,N'-(or N,S-) Diallyl-Substituted Derivatives of Phenobarbital, Amobarbital and Thiopental in Mice(Pharmacological)
• N^3-BENZYLURIDINE EXERTS HYPNOTIC ACTIVITY IN MICE
• EXCITATORY AMINO ACIDS AND LEAD-INDUCED NEUROTOXICITY
• ROLES OF μ-OPIOID RECEPTORS IN DEVELOPMENT OF TOLERANCE TO DIISOPROPYLFLUOROPHOSPHATE (DFP)
• DIFFERENTIAL MODULATION OF MUSCARINIC RECEPTORS IN THE RAT BRAIN BY REPEATED EXPOSURE TO METHYL PARATHION
• MECHANISM OF TOLERANCE DEVELOPMENT TO PENTOBARBITAL IN RELATION TO GABA-ERGIC NEURONAL AND DISPOSITIONAL FUNCTIONS IN MICE
• MECHANISM OF TOLERANCE DEVELOPMENT TO PHENCYCLIDINE IN RELATION TO GABA-ERGIC NEURONAL AND DISPOSITIONAL FUNCTIONS IN MICE
• Nonspecific Effects of the Selective κ-Opioid Receptor Agonist U-50, 488H on Dopamine Uptake and Release in PC12 Cells
• Butorphanol : Effects of a Prototypical Agonist-Antagonist Analgesic on κ-Opioid Receptors
• The Role of Glutamate in Physical Dependence on Opioids
• Metabolic Reaction of Tolualdehydes by Microsomal Aldehyde Oxygenase (MALDO) in Lung (Proceedings of the 19th Symposium on Toxicology and Environmental Health)
• Effects of Barbiturates on GABA System: Comparison to Alcohol and Benzodiazepines.

もっと見る 閉じる

スポンサーリンク