Synthesis and Biological Evaluation of New Salvinorin B-Sulfonate Ester Ligands to Opioid Receptors

• Published in: Planta Medica
• Main Authors: Polepally, PR, Roth, BL, White, K, Vardy, E, Zjawiony, JK
• Format: Conference Proceeding
• Language: English
• Published: 22.03.2013
• ISSN: 0032-0943; 1439-0221
• DOI: 10.1055/s-0033-1336486

Salvinorin A, a major metabolite isolated from the leaves of Salvia divinorum , is a neoclerodane diterpenoid with a strong hallucinogenic activity. It has been shown to have high affinity and selectivity for kappa opioid receptor (KOR) [1]. Salvinorin A represents an attractive lead compound for drug development due to its strong effects on human mood and low toxicity. Over the past decade numerous derivatives and analogues of salvinorin A were synthesized showing a broad range of KOR affinities [2]. To better understand the ligand-KOR interactions, we synthesized a series of new salvinorin B-sulfonate ester ligands and evaluated them for binding affinity to k , µ and δ-opioid receptors. Acknowledgements: This work was supported by the NIH Grant R01 DA017204 and the NIMH Psychoactive Drug Screening Program (PDSP), University of North Carolina at Chapel Hill, NC 27599. References : [1] Roth BL, et al. (2002) Proceedings of the National Academy of Sciences, 99: 11934 – 11939. [2] Cunningham CW, et al. (2011) Pharmacol Rev, 63: 316 – 347.