Identification of an achiral analogue of J-113397 as potent nociceptin/orphanin FQ receptor antagonist
Copyright policy )Identification of an achiral analogue of J-113397 as potent nociceptin/orphanin FQ receptor antagonist
To date, J-113397 represents the most potent and selective non peptide NOP receptor antagonist widely used in pharmacological studies. However, the synthesis, purification, and enantiomer separation of this molecule, which contains two chiral centers, is rather difficult and low-yielding. Here, we synthesized and tested a series of simplified J-113397 analogues to investigate the importance of the stereochemistry and the influence of the substituents at position 3 of the piperidine nucleus and on the nitrogen atom of the benzimidazolidinone nucleus. The compound coded as Trap-101, an achiral analogue of J-113397, combines a pharmacological profile similar to that of the parent compound with a practical, high-yielding preparation.
- University of Ferrara Italy
- University of Padua Italy
- University of Leicester United Kingdom
Male, Models, Molecular, Narcotic Antagonists, Guinea Pigs, Stereoisomerism, In Vitro Techniques, Nociceptin/orphanin FQ; NOP receptor; Non peptide antagonists; J-113397; Mouse vas deferens assay; Structure–activity study, Recombinant Proteins, Nociceptin Receptor, Mice, Vas Deferens, Piperidines, Guanosine 5'-O-(3-Thiotriphosphate), Receptors, Opioid, Animals, Humans, Benzimidazoles
Male, Models, Molecular, Narcotic Antagonists, Guinea Pigs, Stereoisomerism, In Vitro Techniques, Nociceptin/orphanin FQ; NOP receptor; Non peptide antagonists; J-113397; Mouse vas deferens assay; Structure–activity study, Recombinant Proteins, Nociceptin Receptor, Mice, Vas Deferens, Piperidines, Guanosine 5'-O-(3-Thiotriphosphate), Receptors, Opioid, Animals, Humans, Benzimidazoles
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