6533b7d4fe1ef96bd1262a61
RESEARCH PRODUCT
Synthetic studies of neoclerodane diterpenoids from Salvia splendens and evaluation of opioid receptor affinity
Giuseppe SavonaChristina M. DerschThomas E. PrisinzanoRichard B. RothmanGianfranco FontanaBenjamín Rodríguezsubject
AgonistbiologyChemistrymedicine.drug_classStereochemistryOrganic ChemistryPyrazolineSalviabiology.organism_classificationBiochemistryArticleSalvinorin Achemistry.chemical_compoundOpioid receptorClerodanes opioid receptors salviaDrug DiscoverySalvia divinorummedicineDiterpeneReceptordescription
Abstract 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.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2008-12-20 |