Azidomorphine Explained

Azidomorphine^[1] is an opiate analogue that is a derivative of morphine, where the 7,8 double bond has been saturated and the 6-hydroxy group has been replaced by an azide group.^[2]

Azidomorphine binds with high affinity to the mu opioid receptor,^[3] and is around 40× more potent than morphine in vivo. It has similar effects to morphine, including analgesia, sedation, and respiratory depression. However, its addiction liability has been found to be slightly lower than that of morphine in animal studies.^{[4] [5]}

Notes and References

1. GB . 1396663 . Analgesic Compositions .
2. Knoll J, Fürst S, Kelemen K . The pharmacology of azidomorphine and azidocodeine . The Journal of Pharmacy and Pharmacology . 25 . 12 . 929–39 . December 1973 . 4150295 . 10.1111/j.2042-7158.1973.tb09982.x . 41506653 .
3. Horváth K, Wollemann M . Azidomorphine is an agonist of high-affinity opioid receptor binding sites . Neurochemical Research . 11 . 11 . 1565–9 . November 1986 . 2825053 . 10.1007/bf00965775 . 29580383 .
4. Knoll J . Azidomorphines: a new family of potent analgesics with low dependence capacity . Progress in Neuro-Psychopharmacology . 3 . 1–3 . 95–108 . 1979 . 45567 . 10.1016/0364-7722(79)90074-2 .
5. Hill RC, Roemer D, Buescher H . Investigations of the analgesic and morphine-like properties of azidomorphine . The Journal of Pharmacology and Experimental Therapeutics . 201 . 3 . 580–6 . June 1977 . 405472 .