Detection and Determination of Pharmacologically Active Benzodiazepines in Rat Brain after the Administration of 2-o-Chlorobenzoyl-4-chloro-N-methyl-N'-glycylglycinanilide, using a Combination of High-Pressure Liquid Chromatography and Radioreceptorassay
スポンサーリンク
概要
- 論文の詳細を見る
In the present work we attempted to detect and quantitate central nervous system (CNS)-active benzodiazepines in rat brain after administration of a peptido-aminobenzophenone. The results can be summarized as follows. 1. Radioreceptorassay (RRA) using ^3H-diazepam as the labeled ligand and ratbrain crude synaptosomes was a simple, reliable and sensitive assay method for benzodiazepines. 2. A benzene extract of a rat brain homogenate prepared 15 min after i.p. administration of 2-o-chlorobenzoyl-4-chloro-N-methyl-N'-glycylglycinanilide (1) was subjected to high pressure liquid chromatography (HPLC). By RRA analysis of the eluted fractions, four benzodiazepines having high affinity for benzodiazepine receptors were detected. 3. Changes in the levels of each benzodiazepine in rat brains after i.p. administration of 1 were determined by a combination of HPLC and RRA. The levels can account for the CNS activities of 1. 1 itself could not be detected throughout the experiments. These results strongly indicate that 1 exerts its CNS activities through conversion into CNS-active benzodiazepines in vivo.
- 社団法人日本薬学会の論文
- 1980-05-25
著者
-
藤本 正文
Shionogi Research Laboratories, Shionogi & Co., Ltd.,
-
藤本 正文
Shionogi Research Laboratories Shionogi & Co. Ltd.
-
月野木 祐二
Shionogi Research Laboratory, Shionogi & Co., Ltd.
-
岡林 直
Shionogi Research Laboratories Shionogi And Co. Ltd.
-
元瀬 勝己
Shionogi Research Laboratory, Shionogi and Co., Ltd.
-
来間 和男
Shionogi Research Laboratory, Shionogi and Co., Ltd.
-
小中 隆盛
Shionogi Research Laboratory, Shionogi and Co., Ltd.
-
元瀬 勝己
Shionogi Research Laboratory Shionogi And Co. Ltd.
-
小中 隆盛
Shionogi Research Laboratory Shionogi And Co. Ltd.
-
来間 和男
Shionogi Research Laboratory Shionogi And Co. Ltd.
-
月野木 祐二
Shionogi Research Laboratory Shionogi And Co. Ltd.
関連論文
- Synthesis and Evaluation of Novel Pyrazolo[1,5-a]pyrimidine Derivatives as Nonpeptide Angiotensin II Receptor Antagonists
- Synthesis and Evaluation of Novel Nonpeptide Angiotensin II Receptor Antagonists : Imidazo[4,5-c]pyridine Derivatives with an Aromatic Substituent
- Peptido-aminobenzophenones-Novel Open-ring Derivatives of 1,4-Benzodiazepines
- Good Correlations between Brain Levels of Benzodiazepines determined by Radioreceptorassay and Central Nervous System Activity
- Detection and Determination of Pharmacologically Active Benzodiazepines in Rat Brain after the Administration of 2-o-Chlorobenzoyl-4-chloro-N-methyl-N'-glycylglycinanilide, using a Combination of High-Pressure Liquid Chromatography and Radioreceptorassay
- Interaction of Peptido-aminobenzophenones with Benzodiazepine Receptors
- Mutagenic Activity of 4-Nitroquinoline 1-Oxide and 4-Hydroxyaminoquinoline 1-Oxide on Bacteria
- Colorimetric Determination of 4-Hydroxyaminoquinoline 1-Oxide and 4-Aminoquinoline 1-Oxide.
- Mutagenic Activity of 4-Hydroxyaminoquinoline 1-Oxide.
- Reduction of 4-Nitroquinoline 1-Oxide by Microorganisms.
- Mutagenic Activity of 4-Hydroxyaminoquinoline 1-Oxide
- On the Action of Substituted Azaindolizines on Microorganisms. III. Action of Aminated Azaindolizines on Lactic Acid Bacteria.
- Action of Subsituted Azaindolizines on Microorganisms. II. Action of Halogenated Azaindolizines on Escherichia coli.
- Action of Substituted Azaindolizines on Microorganisms. I. Action on Lactic Acid Bacteria.
- Occurrence of Nucleotides in the Culture Fluid of Microorganisms. II. The Nucleotides in the Broth of Brevibacterium liquefaciens novo sp.
- Occurrence of Nucleotides in the Culture Fluid of Microorganisms. I. Screening of Purine-excreting Bacteria with Purine Auxotrophs of Escherichia coli.
- Occurrence of Nucleotides in the Culture Fluid of a Microorganism