Researchers Synthesize Potential Natural Alternative to Opioid Analgesics

Synthetic conolidine could offer an equally effective alternative to morphine without the associated side effects.

Scientists have isolated a product from the bark of the tropical flowering plant Tabernaemontana divaricata that may lead to the development of “an effective alternative to commonly prescribed narcotic pain treatments.”

Researchers at the Scripps Research Institute have found a way to synthesize “meaningful quantities of the rare natural product conolidine,” a naturally occurring compound that is “a potent analgesic as effective as morphine in alleviating inflammatory and acute pain, with few, if any, side effects.”

Conolidine belongs to the class of opioid analgesics known as C5-nor stemmadenines. Pharmacological assessment revealed that synthetic conolidine effectively suppressed acute pain and inflammatory-derived pain, passed through the blood-brain barrier, and remained present in test subjects’ bloodstreams in high concentrations for several hours after administration.

However, Scripps Florida Associate Professor Laura Bohn said in a statement that although the analgesic properties of synthetic conolidine are “encouraging,” the mechanism of action of this compound remains a mystery. “After pursuing more than 50 probable cellular targets, we are still left without a primary mechanism,” she said.

Another challenge confronting researchers’ efforts to better understand this compound and more fully develop it for therapeutic applications is that fact that is has very low affinity to known opiate receptors

Results from this study were published in the article “Synthesis of Conolidine: A Potent Non-opioid Analgesic for Tonic and Persistent Pain” in the June 2011 issue of Nature Chemistry.