Drug intelligence / Profile preview

ro 64-6198

Development stage
Preclinical
Lead developer
Roche
Modality
Small Molecules
Administration
Systemic, Not Oral
01

Overview

**Ro 64-6198** is a potent, selective, systemically active, nonpeptide agonist of the **nociceptin receptor** (also known as the NOP receptor or ORL-1 receptor), with over 100-fold selectivity compared to traditional opioid receptors. It was developed by Hoffmann-La Roche for research purposes and demonstrates anxiolytic, antitussive, and some analgesic properties in preclinical models, with minimal abuse potential. It impairs short-term memory, counteracts stress-induced anorexia, and reduces self-administration and relapse in models of alcoholism and cocaine use. Ro 64-6198 has poor oral bioavailability, limiting clinical development, and does not generally produce classic opioid effects—such as respiratory depression or euphoria—seen with conventional opioids.

Other names
8-(2,3,3a,4,5,6-hexahydro-1H-phenalen-1-yl)-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one280783-56-4
02

Targets

NOP (Nociceptin/orphanin FQ peptide receptor)

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