Natural products (NPs) play an important role in drug discovery, serving as either a source or inspiration for approximately half of all approved small-molecule drugs. Although a large number of these drugs are naturally occurring substances, derivatives of NPs are often necessary to improve their pharmacokinetic properties. Perhaps the best examples of NP derivatives that have been developed into drugs are the many morphine-derived opioids prescribed for the treatment of pain. Opioid receptors, the site of action of morphine and related compounds, have also been implicated in other CNS disorders such as Parkinson's disease, depression and drug abuse. This talk will outline our recent progress in developing novel treatments for CNS disorders by targeting opioid receptors. In particular, our efforts to develop drug abuse medications through a better understanding of the chemistry and pharmacology of salvinorin A will be described.

Natural products as leads for CNS drug discovery

247th National Meeting (2014)

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