ChemInform Abstract: Synthesis of (1S,3aS)-8- (2,3,3a,4,5,6-Hexahydro-1H-phenalen-1-yl)-1-phenyl-1,3,8-triaza-spiro [4.5]decan-4-one, a Potent and Selective Orphanin FQ (OFQ) Receptor Agonist with Anxiolytic-Like Properties.
Abstract
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ChemInform Abstract
The synthesis of title compound (XII) and its diastereoisomers is achieved via a Stobbe-type condensation, an asymmetric hydrogenation, and a Strecker-reaction. Within this series full agonists of the opioid (μ, ϰ, δ) receptors are identified. The most selective compound (XII) is evaluated for its behavioral effects with specific attention for effects on emotional reactivity and anxiolytic-like properties in the elevated plus-maze test.