Benjamin Neuenswander

2 papers in the library · publishing 2017

Papers

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The C-2 derivatives of salvinorin A, ethoxymethyl ether Sal B and β-tetrahydropyran Sal B, have anti-cocaine properties with minimal side effects.

Psychopharmacology August 1, 2017 Amy W M Ewald, Peter J Bosch, Aimee Culverhouse et al.

Kappa-opioid receptor (KOPr) agonists have pre-clinical anti-cocaine and analgesic effects. However, side effects including sedation, dysphoria, aversion, anxiety and depression limit their therapeutic development. The unique structure of salvinorin A has been used to develop longer acting KOPr agonists. We evaluate two novel C-2 analogues of salvinorin A, ethoxymethyl ether Sal B (EOM Sal B)...

DOI: 10.1007/s00213-017-4637-2 Full text Salvinorin a Anxiolytic Behavioural pharmacology Cocaine +5

Addressing Structural Flexibility at the A-Ring on Salvinorin A: Discovery of a Potent Kappa-Opioid Agonist with Enhanced Metabolic Stability.

Journal of Medicinal Chemistry May 11, 2017 Alexander M. Sherwood, Rachel Saylor Crowley, Kelly F Paton et al.

Previous structure-activity studies on the neoclerodane diterpenoid salvinorin A have demonstrated the importance of the acetoxy functionality on the A-ring in its activity as a κ-opioid receptor agonist. Few studies have focused on understanding the role of conformation in these interactions. Herein we describe the synthesis and evaluation of both flexible and conformationally restricted...

DOI: 10.1021/acs.jmedchem.7b00148 Full text