Buprenorphine is one of the Bentley compounds derived from an alkaloid of the plant Papaver somniferum (the opium poppy), known as thebaine.

Buprenorphine has an extremely high binding affinity at the µ- and κ-opioid receptor. It has partial agonist activity at the µ-opioid receptor, partial or full agonist activity at the ORL1/nociceptin and δ-opioid receptor, and competitive antagonist activity at the κ-opioid receptor.

Buprenorphine hydrochloride was first marketed in the 1980s by Reckitt & Colman (now Reckitt Benckiser) as an analgesic, generally available as Temgesic 0.2 mg sublingual tablets, and as Buprenex in a 0.3 mg/ml injectable formulation. In October 2002, the Food and Drug Administration (FDA) of the United States also approved Suboxone and Subutex, buprenorphine's high-dose sublingual tablet preparations indicated for detoxification and long-term replacement therapy in opioid dependency, and the drug is now used predominantly for this purpose.