1971Folia Pharmacologica JaponicaOpen access

Analgesic effect of 2-methylaminomethyl 2, 3-dihydrobenzofuran (EPS-4032)

Tosiharu OHGOH, Akifumi Kitahara, Masatoshi Fujimoto, Kohhei Miyao

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Abstract

2-Methylaminomethyl 2, 3-dihydrobenzofuran (EPS-4032) revealed relatively potent analgesic effect on various method in mice. Its effect was roughly equivalent to codein and as 5 times potent as aminopyrine. Morphine analgesia was apparently antagonized by levallorphan, while EPS-4032 analgesia was markedly potentiated by it, as well as aminopyrine. In the animals pretreated with reserpine or tetrabenazine, EPS-4032 and morphine failed to produced analgesic action. However, this antagonism was disappeared by administration of 1-DOPA after tetrabenazine. Analgesic effect of EPS-4030 was significantly intencified with pretreatment of nialamide and SKF-525A, but apparently reduced by pretreatment of phenobarbital. Also slight developement of tolerance was observed by repeated administration of EPS-4032 on mice.

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2-Methylaminomethyl 2, 3-dihydrobenzofuran (EPS-4032) revealed relatively potent analgesic effect on various method in mice. Its effect was roughly equivalent to codein and as 5 times potent as aminopyrine. Morphine analgesia was apparently antagonized by levallorphan, while EPS-4032 analgesia was markedly potentiated by it, as well as aminopyrine. In the animals pretreated with reserpine or tetrabenazine, EPS-4032 and morphine failed to produced analgesic action. However, this antagonism was disappeared by administration of 1-DOPA after tetrabenazine. Analgesic effect of EPS-4030 was significantly intencified with pretreatment of nialamide and SKF-525A, but apparently reduced by pretreatment of phenobarbital. Also slight developement of tolerance was observed by repeated administration of EPS-4032 on mice.

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Available abstract

2-Methylaminomethyl 2, 3-dihydrobenzofuran (EPS-4032) revealed relatively potent analgesic effect on various method in mice. Its effect was roughly equivalent to codein and as 5 times potent as aminopyrine. Morphine analgesia was apparently antagonized by levallorphan, while EPS-4032 analgesia was markedly potentiated by it, as well as aminopyrine. In the animals pretreated with reserpine or tetrabenazine, EPS-4032 and morphine failed to produced analgesic action. However, this antagonism was disappeared by administration of 1-DOPA after tetrabenazine. Analgesic effect of EPS-4030 was significantly intencified with pretreatment of nialamide and SKF-525A, but apparently reduced by pretreatment of phenobarbital. Also slight developement of tolerance was observed by repeated administration of EPS-4032 on mice.

Key concepts: Tetrabenazine, Reserpine, Pharmacology, Analgesic, Nialamide, Chemistry, Morphine, Medicine

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