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Narcotic antagonists in the benzomorphan series

Respiratory, cardiovascular and behavioral effects in dogs

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Summary

The behavioral, respiratory and cardiovascular effects of four analgesic antagonists derived from the benzomorphan nucleus have been described. In addition, the ability of these agents to reverse the respiratory, cardiovascular and behavioral depression produced by morphine and meperidine has been reported.

Two of the compounds, 2-allyl-5-ethyl-2′-hydroxy-9-methyl-6,7-benzomorphan (I) and 2-cyclopropylmethyl-2′-hydroxy-5,9-dimethyl-6,7-benzomorphan (IV) proved to be potent antagonists.

The other two, 2-(3,3-dimethylallyl)-2′-hydroxy-5,9-dimethyl-6,7-benzomorphan (II) and 2-(3,3-dimethylallyl)-5-ethyl-2′-hydroxy-9-methyl-6,7-benzomorphan (III), were found to be weak antagonists.

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References

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  5. Studies on the human addiction liability of 2′-hydroxy-5,9-dimethyl-2-(3,3-dimethylallyl)-6,7-benzomorphan (Win 20, 228): a weak narcotic antagonist. J. Pharmacol. exp. Ther. 143, 149 (1964).

  6. Harris, L. S., and A. K. Pierson: Some narcotic antagonists in the benzomorphan series. Addendum 1, Bull. Drug Addiction and Narcotics 1962.

  7. Some narcotic antagonists in the benzomorphan series. J. Pharmacol. exp. Ther. 143, 141 (1964).

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Dedicated to Professor Otto Krayer on his 65th birthday.

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Harris, L.S. Narcotic antagonists in the benzomorphan series. Naunyn-Schmiedebergs Arch 248, 426–436 (1964). https://doi.org/10.1007/BF00246889

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Keywords

  • Depression
  • Morphine
  • Cardiovascular Effect
  • Meperidine
  • Potent Antagonist