Journal of Pharmacology and Experimental Therapeutics
March 2008
Yulin Wang, Yong Chen, Wei Xu et al.
Salvinorin (Sal) A is a naturally occurring, selective kappa opioid receptor (KOPR) agonist with a short duration of action in vivo. Pharmacological properties of a C(2) derivative, 2-methoxymethyl (MOM)-Sal B, were characterized. MOM-Sal B bound to KOPR with high selectivity and displayed approximately 3-fold higher affinity than U50,488H...
Bioorganic & Medicinal Chemistry Letters
November 1, 2006
David Y W Lee, Minsheng He, Lee-Yuan Liu-Chen et al.
Salvinorin A, a compound isolated from the plant Salvia divinorum, is a potent and highly selective agonist for the kappa opioid receptor. For exploration of its structure and activity relationships, further modifications, such as reduction at the C(4) position, have been studied and a series of salvinorin A derivatives were prepared. These C(4)-modified salvinorin A analogues were screened for...
Bioorganic & Medicinal Chemistry Letters
September 1, 2006
Cécile Béguin, Michele R Richards, Jian-Guo Li et al.
kappa-opioid receptor ligands have raised interest for their apparent effects on mood. The potent and selective kappa-agonist salvinorin A has short-lasting (15min) depressive-like effects in rats in behavioral models used to study mood disorders. Two series of salvinorin derivatives modified at C(2) and C(18), respectively, were synthesized and their kappa-opioid receptor affinities,...
Bioorganic & Medicinal Chemistry
October 1, 2005
David Y W Lee, Zhongze Ma, Lee-Yuan Liu-Chen et al.
Bioactivity-guided fractionation of the leaves of Salvia divinorum has resulted in the isolation of three new neoclerodane diterpenoids: divinatorin D (1), divinatorin E (2), and salvinorin G (3), together with 10 known terpenoids, divinatorin C (4), hardwickiic acid (5), salvinorin-A (6), -B (7), -C (8), -D (9), -E (10), and -F (11), presqualene alcohol (12), and (E)-phytol (13). The...
Bioorganic & Medicinal Chemistry Letters
October 1, 2005
David Y W Lee, Minsheng He, Leelakrishna Kondaveti et al.
Salvinorin A is the most potent naturally occurring opioid agonist with a high selectivity and affinity for kappa-opioid receptor. To explore its structure-activity relationships, modifications at the C(4) position have been studied and a series of salvinorin A derivatives were prepared. These C(4)-modified salvinorin A analogues were screened for binding and functional activities at the human...