The Preparative and Pharmacological Studies of levo and dextro 9-Aza-des-N-morphinan (2,3,4,4a-Tetrahydro-1H, 6H-5,10b-propanophenanthridin-9-ol).

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概要

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• The analgesic effect was found in levo-isomer (DH-15) of 2,3,4,4a-tetrahydro-1H, 6H-5,10b-propanophenanthridin-9-ol, but not in dextro-isomer (DH-14). The analgesic effect of DH-15 was some what stronger than morphine, synergistic to morphine and antagonized by Levallorphane. The acute toxicity of DH-15 was far stronger than that of morphine. The pharmacological effects of DH-15 on the body temperature of mice and rats, barbiturate anaesthesia in mice, purpil of mice and gastrointestinal propulsion in mice were similar to that of morphine, but less active except barbiturate anaesthesia. DH-14 showed little effects. The contraction or increase of tonus in the isolated or in situ intestine of rabbits by the low dosis of DH-14 and DH-15 were observed.

• 社団法人日本薬学会の論文
• 1963-04-25

著者

• 藤村 一

  Kyoto Pharmaceutical University

• 杉本 典夫

  Osaka Research Laboratory Tanabe Seiyaku Co. Ltd.

• 林 五朗

  Osaka Research Laboratory, Tanabe Seiyaku Co., Ltd.

• 武田 幹男

  Osaka Research Laboratory, Tanabe Seiyaku Co., Ltd.

• 釘田 博至

  Osaka Research Laboratory, Tanabe Seiyaku Co., Ltd.

• 藤村 一

  Institute for Chemical Research, Kyoto University

• 杉本 典夫

  Osaka Research Laboratory Gohei Tanabe & Co. Ltd.

• 釘田 博至

  Osaka Research Laboratory Gohei Tanabe & Co. Ltd.

• 杉本 典夫

  Osaka Research Laboratory, Tanabe Seiyaku Co., Ltd.

関連論文

• Synthesis and Analgetic Activity of Sulfur-Containing Morphinans and Related Compounds
• The Preparative and Pharmacological Studies of levo and dextro 9-Aza-des-N-morphinan (2,3,4,4a-Tetrahydro-1H, 6H-5,10b-propanophenanthridin-9-ol).
• Expectorant Effect and Clinical Efficacy of 1-Methyl-3-(di-2-thienylmethylene)piperidine Citrate (AT-327)
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• Studies on the Syntheses of Hydrogenated Quinolines and Isoquinolines as Analgesics. XIV. Synthesis of 6-Hydroxy-4a, 10-trimethylene-1,2,3,4,4a, 9,10,10a-octahydrophenanthridine (Supplement).
• Studies on the Syntheses of Hydrogenated Quinolines and Isoquinolines as Analgesics. XIII. Synthesis of 3-Hydroxy-N-methyl-6-aza-des-N-morphinan (N-Methyl-9-hydroxy-5,10b-trimethylene-1,2,3,4,4a, 5,6,10b-octahydrobenzo [h] isoquinoline).
• Studies on the Syntheses of Hydrogenated Quinolines and Isoquinolines as Analgesics. XII. Synthesis of N-Methyl-7-aza-des-N-morphinan (3-Methyl-5,10b-trimethylene-1,2,3,4,4a, 5,6,10b-octahydrobenzo [f] isoquinoline).
• Studies on the Syntheses of Hydrogenated Quinolines and Isoquinolines as Analgesics. XI. Synthesis of N-Methyl-6-aza-des-N-morphinan (2-Methyl-5,10b-trimethylene-1,2,3,4,4a, 5,6,10b-octahydrobenzo [h] isoquinoline).
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