Salvinorin A (1), a neoclerodane diterpene from the hallucinogenic mint Salvia divinorum, is the onlyknown non-nitrogenous and specific k-opioid agonist. Several structural congeners of 1 isolated fromSalvia splendens (2–8) together with a series of semisynthetic derivatives (9–24), some of which possessa pyrazoline structural moiety (9, 19–22), have been tested for affinity at human m, d, and k opioid receptors.None of these compounds showed high affinity binding to these receptors. However, 10 showedmodest affinity for k receptors suggesting that other natural neoclerodanes from different Salvia speciesmay possess opioid affinity.
|Numero di pagine||8|
|Stato di pubblicazione||Published - 2008|
All Science Journal Classification (ASJC) codes
- Drug Discovery
- Organic Chemistry
Savona, G., Fontana, G., Rothman, R. B., Prisinzano, T. E., Dersch, C. M., & Rodríguez, B. (2008). Synthetic studies of neoclerodane diterpenoids from Salvia splendens and evaluation of opioid receptor affinity. Tetrahedron, 64, 10041-10048.