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Synthetic studies of neoclerodane diterpenoids from Salvia splendens and evaluation of opioid receptor affinity |
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| Authors: | Gianfranco Fontana,Benjamí n Rodrí guez,Christina M. Dersch,Thomas E. Prisinzano |
| Affiliation: | a Dipartimento di Chimica Organica ‘E. Paternò’, Università degli Studi di Palermo, Parco d'Orleans 2, I-90128 Palermo, Italy b Instituto de Química Orgánica, Consejo Superior de Investigaciones Científicas (CSIC), Juan de la Cierva 3, E-28006 Madrid, Spain c Clinical Psychopharmacology Section, IRP, NIDA, NIH, DHHS, Baltimore, MD 21224, USA d Department of Medicinal Chemistry, The University of Kansas, Lawrence, KS 66045, USA |
| 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. |
| Keywords: | Salvia splendens Opioid receptors Neoclerodane diterpenes Semisynthetic derivatives |
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