HOMOBENZOMORPHAN COMPOUNDS WITH A POTENT NARCOTIC ANTAGONIST PROPERTY

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概要

• 論文の詳細を見る

• In consequence of testing antagonistic activity on morphine-induced analgesia and respiratory depression of the, 2-hydroxy-6, 10-dimethy-7, 8-homobenzomorphans, it was found that the order of antagonistic activity is <I>N</I>-cyclopropylmethyl (trans isomer TA-414 and cis isomer TA-576)><I>N</I>-allyl (trans isomer TA-412)><I>N</I>-dimethylallyl (trans isomer TA-413 and cis isomer TA-415) with respect to the influence of replacing antagonistic substitution on the tertiary nitrogen. The properties of TA-414 and TA-576 in this regard were higher than those of nalorphine but slightly less than levallorphan. Moreover, the narcotic antagonist action of TA-414 was of long duration, comparable to that of nalorphine. On the other hand, TA-414 was entirely lacking an agonistic (analgesic) activity even at large doses, while TA-576 equalled nalorphine and pentazocine in the potency of agonistic activity in mice. Conclusively, TA-414 appears to fall under the category of a pure antagonist such as naloxone.

• 社団法人 日本薬理学会の論文

著者

• TAKEDA MIKIO

  Organic Chemistry Research Laboratory, Tanabe Seiyaku Co., Ltd.

• NURIMOTO Seiichi

  Safety Research Laboratory, Tanabe Seiyaku Co. Ltd.

• SUZUKI Shogo

  Safety Research Laboratory, Tanabe Seiyaku Co. Ltd.

• HAYASHI Goro

  Safety Research Laboratory, Tanabe Seiyaku Co. Ltd.

• TAKEDA Mikio

  Organic Chemistry Research Laboratory, Tanabe Seiyaku Co. Ltd.

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• HOMOBENZOMORPHAN COMPOUNDS WITH A POTENT NARCOTIC ANTAGONIST PROPERTY

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