European journal of medicinal chemistry
October 6, 2014
Prabhakar R Polepally, Krzysztof Huben, Eyal Vardy et al.
28 citations
The neoclerodane diterpenoid salvinorin A is a major secondary metabolite isolated from the psychoactive plant Salvia divinorum. Salvinorin A has been shown to have high affinity and selectivity for the κ-opioid receptor (KOR). To study the ligand-receptor interactions that occur between salvinorin A and the KOR, a new series of salvinorin A derivatives bearing potentially reactive Michael...
The Journal of biological chemistry
November 29, 2013
Eyal Vardy, Philip D Mosier, Kevin J Frankowski et al.
The crystal structures of opioid receptors provide a novel platform for inquiry into opioid receptor function. The molecular determinants for activation of the κ-opioid receptor (KOR) were studied using a combination of agonist docking, functional assays, and site-directed mutagenesis. Eighteen positions in the putative agonist binding site of KOR were selected and evaluated for their effects...
Bioorganic & Medicinal Chemistry Letters
May 15, 2013
Prabhakar R Polepally, Kate White, Eyal Vardy et al.
24 citations
Salvinorin A, the active ingredient of the hallucinogenic plant Salvia divinorum is the most potent known naturally occurring hallucinogen and is a selective κ-opioid receptor agonist. To better understand the ligand-receptor interactions, a series of dicarboxylic ester-type of salvinorin A derivatives were synthesized and evaluated for their binding affinity at κ-, δ- and μ-opioid receptors....
Science
March 22, 2013
Chong Wang, Yi Jiang, Jinming Ma et al.
522 citations
Dissecting Serotonin Receptors Serotonin receptors are the targets for many widely used drugs prescribed to treat ailments from depression to obesity and migraine headaches (see the Perspective by Palczewski and Kiser ). C. Wang et al. (p. 610 , published online 21 March) and Wacker et al. (p. 615 , published online 21 March) describe crystal structures of two members of the serotonin family of...
Science
March 21, 2013
Daniel Wacker, Chong Wang, Vsevolod Katritch et al.
689 citations
Dissecting Serotonin Receptors Serotonin receptors are the targets for many widely used drugs prescribed to treat ailments from depression to obesity and migraine headaches (see the Perspective by Palczewski and Kiser ). C. Wang et al. (p. 610 , published online 21 March) and Wacker et al. (p. 615 , published online 21 March) describe crystal structures of two members of the serotonin family of...
Planta Medica
August 1, 2011
JK Zjawiony, PR Polepally, B.l. Roth et al.
10 citations
Psychoactive natural products play an important role in the discovery and development of new drugs for the treatment of central nervous system (CNS) disorders. Our studies are focusing on identification of plant metabolites responsible for CNS activity and designing new ligands with high affinity to CNS receptors. Salvinorin A, the most potent naturally occurring hallucinogen isolated from the...