Drug intelligence / Profile preview

MCOPPB

Development stage
Preclinical
Lead developer
Tokyo University of Science
Modality
Small Molecules
Administration
Oral
01

Overview

MCOPPB is a potent, non-peptide small molecule that acts as a selective agonist for the nociceptin receptor (NOP, also known as the opioid receptor-like 1 or ORL-1). Originally developed for its potential anxiolytic effects, MCOPPB has demonstrated the ability to reduce anxiety in animal models without the sedative or motor-impairing side effects typically associated with benzodiazepines. Recent research utilizing high-content morphological profiling (Cell Painting) has identified an additional, previously overlooked mechanism: MCOPPB acts as an inhibitor of autophagy. It appears to disrupt autophagosome-lysosome fusion, leading to the accumulation of p62/SQSTM1 and LC3 markers. This dual activity suggests that while MCOPPB is a valuable tool for studying NOP receptor signaling, it also possesses off-target effects that may have therapeutic relevance in oncology, where autophagy inhibition is a recognized strategy for sensitizing tumors to stress and therapy.

Other names
1-[1-(1-methylcyclooctyl)-4-piperidinyl]-1,3-dihydro-2H-benzimidazol-2-one1-[1-(1-methylcyclooctyl)piperidin-4-yl]-3H-benzimidazol-2-one
02

Targets

NOP (Nociceptin/orphanin FQ peptide receptor)

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