Drug intelligence / Profile preview

7-benzylidenenaltrexone

Development stage
Unknown
Modality
Small Molecules
01

Overview

7-Benzylidenenaltrexone (BNTX) is a small-molecule research compound and a selective delta-1 opioid receptor (DOR1) antagonist. It is a morphinan derivative of naltrexone, synthesized via the aldol condensation of naltrexone with benzaldehyde. BNTX exhibits high affinity for the delta-1 opioid receptor (Ki = 0.1 nM) with significantly lower affinity for the delta-2, mu, and kappa opioid receptors. It is widely utilized as a pharmacological tool in preclinical research to study opioid receptor subtypes, antinociception, and cardioprotection. Additionally, BNTX has demonstrated preclinical activity as a DOR1-independent immunosuppressant, reducing autoreactive B cells and improving lupus nephritis in mouse models, as well as reversing chloroquine resistance in Plasmodium chabaudi.

Other names
7-benzylidenenaltrexone maleate7(E)-BenzylidenenaltrexoneBNTX maleate
02

Targets

DOR (Opioid Receptor Delta 1)

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