Abstract
Removal of the carbonyl oxygen of himbacine furnishes a molecule which binds with 20-fold and 4-fold lower affinity at the M 2 and M 1 receptor sites, respectively. Thus, the carbonyl oxygen constitutes an important pharmacophoric element responsible for some of the M 2 selectivity of himbacine. Other modifications of the C-ring of the tricyclic portion of himbacine were examined and tested for potency at M 1 and M 2 sites, and the data confirm that M 2 selectivity is optimal with a closed heterocyclic ring and with the presence of a proximal carbonyl oxygen.
Published Version
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