Desmethylprodine

Desmethylprodine is a synthetic opioid developed in the 1940s by researchers at Hoffmann-La Roche. It is chemically related to pethidine (meperidine) and is a potent analgesic.

Chemistry

Desmethylprodine is a 4-phenylpiperidine derivative that is structurally similar to pethidine. The only difference is the absence of a methyl group on the nitrogen atom. This small change makes desmethylprodine approximately 30 times more potent than pethidine as an analgesic.

Pharmacology

Desmethylprodine acts primarily as a mu-opioid receptor agonist. The mu-opioid receptors are a class of opioid receptors with high affinity for enkephalins and beta-endorphin but low affinity for dynorphins. They are also the primary receptors responsible for the analgesic effects of opioids.

History

Desmethylprodine was first synthesized in 1947 by Hoffman-La Roche, which was looking for a non-addictive alternative to morphine. However, it was found to be highly addictive and was never marketed.

Legal status

Desmethylprodine is a Schedule I controlled substance in the United States, meaning it has a high potential for abuse and no accepted medical use. It is also controlled under international law by the Single Convention on Narcotic Drugs of 1961.

See also

• Opioid
• Pethidine
• Mu-opioid receptor