A New Potent Analgetic Antagonist

  title={A New Potent Analgetic Antagonist},
  author={M. Gordon and J. Lafferty and D. H. Tedeschi and N. B. Eddy and E. May},
THE discovery of a new potent analgetic with a reduced liability to addiction1 in the benzomorphan series, namely, 2′-hydroxy-5,9-dimethyl-2-phenylethyl-6,7-benzomorphan2 (I), has suggested further work in the series. 2′-Hydxoxy-5,9-dimethyl-2-allyl-6,7-benzomorphan (III) is a potent antagonist of phenazocine, morphine, meperidine, and other analgetic agents. This compound is of special interest in that combinations of phenazocine and III in ratios of 5 : 1 to 100 : 1 retain analgetic activity… Expand
Narcotic Antagonists as Analgesics
Studies of addiction liability with Win 20,228 in monkeys suggest that this compound will not support morphine addiction, and preliminary clinical trials indicate that Win 19,362 is about twice as potent as morphine as an analgesic but, like nalorphine, is capable of producing severe psychic side effects. Expand
Structure-Activity Relationships
The importance of this finding lies in the fact that the narcotic-antagonist analgesics have a much lessened abuse potential and do not produce a typical morphine-like physical dependence. Expand
Antinociceptive studies of the optical isomers of N-allylnormetazocine (SKF 10,047).
  • M. Aceto, E. May
  • Chemistry, Medicine
  • European journal of pharmacology
  • 1983
The results suggest that morphine and NANM are acting at different sites, and different alpha 2-adrenoceptors appear to be involved. Expand
Antagonists, Dualists, and Kappa Agonists
The aim of this chapter is to bring together data on opioid ligands that (1) antagonize the actions of morphine and its surrogates, (2) possess both agonist and antagonist properties, and (3) possessExpand
Potential long acting opiate antagonists: preparation, pharmacological activity, and opiate-receptor binding of N-substituted 2'-hydroxy-5-methyl-9 alpha-propyl-6,7-benzomorphans.
A homologous series of N-substituted 2'-hydroxy-5-methyl-9 alpha-propyl-6,7-benzomorphans (hydrogen to octyl inclusive, allyl, and cyclopropylmethyl) was prepared and the N-pentyl and N-hexyl derivatives do not have the analgesic potency of the parent N-methyl compound; instead, they are narcotic antagonists with a long duration of action. Expand
Historical introduction and review of chemistry.
A historical introduction and review of the chemistry of the agonist-antagonist analgesics is presented and structure-activity relationships are summarized relating changes in N-alkylation to the production of narcotic antagonist activity over all of the structural types of opioids. Expand
Structural and conformational relationships between the enkephalins and the opiates
The significance of the finding that both of these small peptides contain a tyrosine residue at the amino terminal position for the conformational relationship between the enkephalins and opiates is considered. Expand
Chemistry of Nonpeptide Opioids
During the past three decades interest in nonpeptide opioids has been rekindled in part by the introduction of a clinically acceptable analgesic of the mixed agoinst-antagonist type with reducedExpand
The enkephalins and opiates: structure‐activity relations
The X‐ray structures of 9 ‘opiate’ drugs which exhibit a range of pharmacological activity have been examined in detail leading to the theory that one of the reasons why the enkephalins and relatedExpand
Comparison of the Behavioral Pharmacology of Phencyclidine to Related Compounds
A comparison of the behavioral pharmacol ogy of PCP to related compounds and several compounds with PCP-l i ke is presented. Expand