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The irreversible narcotic antagonistic and reversible agonistic properties of the fumaramate methyl ester derivative of naltrexone |
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| Authors: | A. E. Takemori Dennis L. Larson P. S. Portoghese |
| Affiliation: | a Department of Pharmacology, Medical School (A.E.T.), University of Minnesota, Minneapolis, Minnesota 55455, U.S.A. b Department of Medicinal Chemistry, College of Pharmacy (P.S.P., D.L.L.), University of Minnesota, Minneapolis, Minnesota 55455, U.S.A. |
| Abstract: | The fumaramate methyl ester derivatives of naltrexone (β-FNA) and oxymorphone (β-FOA) were both found to be reversible agonists on the guinea pig ileal longitudinal muscle preparation. In addition, β-FNA possessed an irreversible antagonistic effect against morphine whereas β-FOA had no such capacity. Analysis by pA2 values revealed that β-FOa resembled pure agonists like morphine and enkephalin while β-FNA resembled the mixed agonist-antagonists like nalorphine and pentazocine. The antagonism by β-FNA was very selective in that it antagonized pure agonists but had little or no effect on the effects of either mixed agonists, ethylketocyclazocine or other non-opiate-type agonists like norepinephrine. |
| Keywords: | Fumaramate methyl ester derivative Guinea pig ileum Opioid receptor Oxymophone Naltrexone Agonist Antagonist Narcotic |
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