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
スポンサーリンク
概要
- 論文の詳細を見る
3,7-Dimethyl-1-(5-oxo-hexyl)-xanthine (BL 191) and its major urinary metabolites were examined for the inhibitory effect on the cyclic 3', 5'-nucleotide phosphodiesterase (PDE) activity and for the stimulating effect on lipolysis in rat epididymal fat pads in vitro. In addition, the relationship between these effects of BL 191 and plasma level of free fatty acid (FFA) was investigated in rats. The addition of BL 191 at 2 mM to the incubation mixture inhibited the activity of PDE about 50% and evoked a lipolytic activity 1.5-fold, and BL 191 and theophylline exerted approximately the same effects on PDE and lipolysis. Furthermore, the PDE inhibition and lipolytic response evoked by metabolites I and II possessing an oxohexyl group at the side chain were slightly less than those by BL 191,and metabolites III and IV having a carboxyl group at the side chain had no effects on PDE activity and lipolysis. When BL 191 was given orally, plasma FFA level was elevated in the blood taken 30 min after the administration, increased linearly until 1 hr after the administration when the level was nearly 1.6 times higher than the basal level, and remained at this level till 2 hr after the administration. The above-described results suggested that BL 191 along with its metabolites I and II by the oral administration of BL 191 inhibited the PDE activity and secondarily stimulated the lipolytic activity within the living body.
- 公益社団法人日本薬学会の論文
- 1976-06-25
著者
-
小澤 光
Pharmaceutical Institute Tohoku University
-
坂口 孝
Pharmaceutical Laboratory, Hoechst Japan Limited
-
林 昌亮
ヘキストジャパン 医薬総研
-
坂口 孝
ヘキストジャパン
-
林 昌亮
ヘキストジャパン株式会社総合開発研究所
関連論文
- 尿路手術における組織接着剤(BI0.022)の応用 : 第1報イヌ腎切開術
- 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
- 尿路手術における組織接着剤の応用 : 第1報 イヌ腎切開術
- 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.
- Cefodizime sodium の急性毒性試験
- Cefodizime sodiumのウサギにおける腎毒性試験 : 単回および7日間連続静脈内投与試験
- Cefodizime sodiumのラット皮下投与による6ヵ月間慢性毒性試験および5週間回復試験
- Cefodizime sodiumのラット静脈内投与による1ヵ月間亜急性毒性試験および2週間回復試験
- 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
- 31. マウス胎仔肝の形態学的研究III肝内造血細胞の分裂方式について
- マウス胎仔肝の形態学的研究 : II.胎仔肝実質細胞と肝内造血細胞について
- マウス胎仔肝の形態学的研究
- 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.
- 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―
- Teratogenicity of Regular Insulin and Ultralente Insulin in Rats
- 13. SDラットおよびWistarラットにおけるultralente insulinの催奇形作用
- 100. ラットにおけるインスリン投与による母体血糖値の変動と眼奇形成立の関係
- Pentoxidfyllineのマウス脳内5-Hydroxytryptamineに及ぼす影響
- 創薬研究のための疾患モデル動物
- PropentofyllineとCaffeineの中枢作用に関する薬理学的比較