Powerful new oral painkiller blocks signals without sedation or addiction

Scientists have shown the efficacy of a new non-opioid oral painkiller known as ADRIANA, the world's first selective alpha2B-adrenoceptor antagonist – a receptor subtype not previously targeted for analgesics. In clinical trials so far, it has provided powerful pain relief without sedation or risk of addiction.

Researchers at Japan's Kyoto University Scientists have developed an oral medication that targets the ?2B adrenoceptor, a little-studied brain receptor that scientists have found actually plays a major role in mechanical pain. This makes it the first-ever alpha2B-selective painkiller.

This receptor belongs in the adrenergic receptor family – alpha2A, alpha2B, alpha2C – but no approved drug has targeted alpha2B to inhibit the receptor with high precision. Existing drugs like dexmedetomidine target broad a2 receptors and in this example's case cause sedation and are not oral. This in itself makes this small-molecule drug candidate, also known as compound c545, a potentially new class of pain-relief drug.

"If successfully commercialized, ADRIANA would offer a new pain management option that does not rely on opioids, contributing significantly to the reduction of opioid use in clinical settings," said corresponding author Masatoshi Hagiwara, a specially-appointed professor at Kyoto University.

Image source: KyotoU / Hagiwara lab.