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Synthesis and in vitro characterization of new salvinorin a analogs incorporating natural amino acids

โœ Scribed by Fichna, Jakub; Lewellyn, Kevin; Yan, Feng; Roth, Bryan L.; Zjawiony, Jordan K.


Book ID
121769069
Publisher
Elsevier
Year
2011
Tongue
English
Weight
90 KB
Volume
63
Category
Article
ISSN
1734-1140

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Synthesis and biological evaluation of n
โœ Jakub Fichna; Kevin Lewellyn; Feng Yan; Bryan L. Roth; Jordan K. Zjawiony ๐Ÿ“‚ Article ๐Ÿ“… 2011 ๐Ÿ› Elsevier Science ๐ŸŒ English โš– 258 KB

The synthesis and in vitro evaluation of a new series of salvinorin A analogues substituted at the C(2) position with natural amino acids is reported. Compound 12, containing Val, displayed high affinity and full agonist activity at the kappa-opioid receptor. Analogues with bulky and/or aromatic res