Salvinorin A (1), a neoclerodane diterpene from the hallucinogenic mint Salvia divinorum, is the only known non-nitrogenous and specific κ-opioid agonist. Several structural congeners of 1 isolated from Salvia splendens (2-8) together with a series of semisynthetic derivatives (9-24), some of which possess a pyrazoline structural moiety (9, 19-22), have been tested for affinity at human μ, δ, and κ opioid receptors. None of these compounds showed high affinity binding to these receptors. However, 10 showed modest affinity for κ receptors suggesting that other natural neoclerodanes from different Salvia species may possess opioid affinity.
|Number of pages||8|
|State||Published - Oct 20 2008|
Bibliographical noteFunding Information:
This work was supported in part by funds from the Spanish ‘Comisión Interministerial de Ciencia y Tecnología’ (CICYT), grant No. CTQ2006-15279-C02-02, Italian ‘Università degli Studi di Palermo’, grant ‘Ex 60%-2005’, and R01DA018151 (to T.E.P.) from the National Institute on Drug Abuse. The content is the sole responsibility of the authors and does not necessarily represent the official views of the National Institute on Drug Abuse or the National Institutes of Health.
- Neoclerodane diterpenes
- Opioid receptors
- Salvia splendens
- Semisynthetic derivatives
ASJC Scopus subject areas
- Drug Discovery
- Organic Chemistry