Abstract
The antagonist potencies of methylnaloxone and naloxone were measured for morphine in the isolated guinea pig ileum by the pA 2 method and a potency ratio determined. A second potency ratio was determined by comparing the concentration of each antagonist required to produce abstinence-like contractures of ileal tissues from morphine-treated guinea pigs. If the latter response required penetration of the cell membrane lipid bilayer, one would expect methylnaloxone, a quaternary amine, to be significantly less potent than naloxone. Comparison of potency ratios for methylnaloxone and naloxone did not support this hypothesis.
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