Comparative neuropharmacology of structurally distinct non-fentanyl opioids that are appearing on recreational drug markets worldwide

Original research
par
Vandeputte, Marthe M. et al

Date de publication

2023

Géographie

International

Langue de la ressource

English

Texte disponible en version intégrale

Non

Open Access / OK to Reproduce

Non

Évalué par des pairs

Yes

L’objectif

Here, we examined the neuropharmacology of structurally distinct non-fentanyl NSOs, including U-47700, isotonitazene, brorphine, and N-desethyl isotonitazene, as compared to morphine and fentanyl.

Constatations/points à retenir

Receptor binding results revealed high MOR selectivity for all compounds, with MOR affinities comparable to those of morphine and fentanyl (i.e., nM). All drugs acted as full-efficacy MOR agonists in the cyclic AMP assay, but nitazene analogs had greater functional potencies (i.e., pM) compared to the other drugs (i.e., nM). When administered to rats, all compounds induced opioid-like antinociception, catalepsy, and body temperature changes, but nitazenes were the most potent. Similar to fentanyl, the nitazenes had faster onset and decline of in vivo effects when compared to morphine.

La conception ou méthodologie de recherche

In vitro and in vivo testing

Mots clés

Drug checking
Illegal drugs