ETONITAZENE

Investigational

Details

Stereochemistry	ACHIRAL
Molecular Formula	C22H28N4O3
Molecular Weight	396.4827
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

CCOC1=CC=C(CC2=NC3=C(C=CC(=C3)[N+]([O-])=O)N2CCN(CC)CC)C=C1

InChI

InChIKey=PXDBZSCGSQSKST-UHFFFAOYSA-N

InChI=1S/C22H28N4O3/c1-4-24(5-2)13-14-25-21-12-9-18(26(27)28)16-20(21)23-22(25)15-17-7-10-19(11-8-17)29-6-3/h7-12,16H,4-6,13-15H2,1-3H3

HIDE SMILES / InChI

Molecular Formula	C22H28N4O3
Molecular Weight	396.4827
Charge	0
Count	MOL RATIO 1 MOL RATIO (average)

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description

Etonitazene is a potent and selective mu-opioid agonist. It was developed in CIBA. Administration of etonitazene may induce respiratory depression, and therefor etonitazene is not used in humans. Etonitazene is explicitly listed as an illegal drug under UN convention and is illegal throughout the world.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Mu opioid receptor 221	Agonist 2,678		0.5 nM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Pain 614	Primary		Preclinical	Unknown

PubMed

Show entries

Title	Date	PubMed
Effects of etonitazene upon respiratory neurons.	1967 Jan 15	4961975
Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.	1998 Mar	9686407

Showing 1 to 2 of 2 entries

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Patents

Sample Use Guides

In Vivo Use Guide

In rat tail-withdrawal assay, etonitazene was administered subcutaneously. ED50 was 0.38 mg/kg.

Route of Administration: Other

In Vitro Use Guide

Binding of etonitazene to mu-opioid receptors from the membrane fraction of rat brains (minus cerebellum) was studied using [3H]DAMGO as a radioligand. Etonitazene binds to mu-opioid receptors with Ki of 0.5 nM.