adder
Bluelighter
- Joined
- Mar 28, 2006
- Messages
- 2,851
muvolution said:almost all opiates are "pro-drugs" in some sense of the word. Morphine to 3MAM, Oxymorphone to Noroxymorphone, Heroin to 6-MAM and Morphine, etc...
Alright but firstly morphine acts on opioid receptors with a good affinity itself so it's a good analgesic on its own while e.g. codeine while preserving some very little affinity is useless itself and needs metabolism to be effective as a medication.
And secondly I wouldn't put metabolism of morphine to morphine-3-glucuronide (I think you meant that and not 3-MAM) as a good outcome of morphine intake, this compound is inactive as an opioid and it's a convulsant. If you meant 3-MAM as a metabolite of heroin, it's also an example of a metabolite that brings little to nothing to overall feeling of drug intake.
Maybe calling e.g. codeine a prodrug is wrong? It definitely has an affinity to opioid receptors (Ki = 600nM but still) although it's very little. Prodrug is supposed to be an inactive compound that is metabolized to an active metabolite.8)