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Identification of an Achiral Analogue of J-113397 as Potent nociceptin/orphanin FQ Receptor Antagonist

Identification of an Achiral Analogue of J-113397 as Potent nociceptin/orphanin FQ Receptor Antagonist

Claudio Trapella, Remo Guerrini, Laura Piccagli, Girolamo Calo', Giacomo Carra', Barbara Spagnolo, Samantha Rubini, Giulia Fanton, Christopher Hebbes, John McDonald, David G Lambert, Domenico Regoli, Severo Salvadori

Bioorg Med Chem. 2006 Feb 1;14(3):692-704.

PMID: 16202610

Abstract:

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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP256640456	J-113397		256640-45-6	Price

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