Drug intelligence / Profile preview

benzylfentanyl

Development stage
Discontinued
Modality
Small Molecules
01

Overview

Benzylfentanyl is a synthetic opioid and structural analog of fentanyl. It was originally placed on the US Schedule I controlled substances list in 1985 due to concerns about its potential for abuse as a designer drug, but was removed from the list in 2010 after studies showed it has minimal opioid activity. Benzylfentanyl binds to the mu opioid receptor with low affinity (Ki = 213 nM), making it approximately 200 times less potent than fentanyl itself, though still slightly more potent than codeine. Its mechanism of action is presumed to be similar to other opioids—agonism at the mu opioid receptor—but its weak binding results in negligible clinical or recreational effects. Benzylfentanyl has been used primarily as a chemical precursor in illicit synthesis of more potent fentanyls and is regulated as a List I chemical by the DEA[1][3][4][5].

Other names
N-benzylfentanylN-(1-benzylpiperidin-4-yl)-N-phenylpropionamiden-(1-benzylpiperidin-4-yl)-n-phenylpropanamide1474-02-8
02

Targets

MOR (Mu opioid receptor)

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