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1 Department of Pharmacology, Sterling-Winthrop Research Institute, Rensselaer, New York
Four members of a new series of analgesic antagonists in the 6,7-benzomorphan series have been described.
A quantitative method for the assessment of analgesic-antagonistic potency in the rat has been outlined. Using this method 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), were found to be potent antagonists. The other two, 2-(3,3-dimethylallyl 2-(3,3-di-methylallyl)-2'-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.
Compound IV was also found to have important central muscle-relaxant, anticonvulsant, and tranquilizing properties.
Again, a separation appears to have been made between analgesic activity and addiction liability.
Submitted on May 9, 1963
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