Drug intelligence / Profile preview

dihydroetorphine

Development stage
Unknown
Lead developer
McFarlan-Smith
Modality
Small Molecules
Administration
Sublingual, Oral, Transdermal
01

Overview

Dihydroetorphine is a semi-synthetic opioid analgesic developed in the 1960s by K. W. Bentley at McFarlan-Smith. It is a derivative of etorphine and is used mainly in China for severe pain management. Dihydroetorphine is extraordinarily potent—between 1000 and 12 000 times more potent than morphine—and acts as a full agonist at μ-opioid receptors while also binding to δ-opioid and κ-opioid receptors[1][2][8]. Its primary clinical use is sublingual administration due to poor oral bioavailability; transdermal patches have also been developed for sustained delivery[2][5]. The drug produces strong analgesia with relatively mild side effects compared to other opioids but can cause typical opioid adverse effects such as dizziness, sedation, nausea, constipation and respiratory depression[1][2]. Tolerance and dependence can develop with repeated use.

Other names
18,19-dihydroetorphinedihydroetorphine hydrochlorideTetrahydro-7alpha-(1-hydroxy-1-methylbutyl)-6,14-endo-ethanooripavine7,8-Dihydro-7alpha-(1-(R)-hydroxy-1-methylbutyl)-6,14-endo-ethanotetrahydrooripavine6,14-Ethenomorphinan-7-methanol, 4,5-epoxy–18,19-dihydro–3-hydroxy–6-methoxy-alpha,17-dimethyl-alpha-propyl-, (5alpha,7alpha(R))
02

Targets

DOR (Opioid Receptor Delta 1)KOR (Kappa opioid receptor)MOR (Mu opioid receptor)

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