METHODS FOR IDENTIFYING AND USING LOW/NON-ADDICTIVE OPIOID ANALGESICS

摘要

The present invention relates to a method of using a bioassay consisting of an electrophysiological method and a cell culture system of dorsal-root ganglion (DRG) neurons to screen and identify opioids with a high potential for use as "low- or non-addictive" analgesics. Another aspect of the invention relates to a specific group of opioid alkaloids and analogues thereof identified by the bioassay of the invention for the unique ability to activate only inhibitory, but not excitatory, opioid receptor function, for use as low- or non-addictive analgesics. Another aspect of the invention relates to the specific use of etorphine or dihydroetorphine of the opioid alkaloid family as low- or non-addictive analgesics and for the treatment of opioid addiction. The present invention also relates to the preparation of dihydroetorphine hydrochloride (7(alpha)-(1-(R)-hydroxy-1-methylbutyl)-6,14-endo-ethano-tetrahydrooripavine hydrochloride) and a pharmaceutical composition comprising the compound as an active ingredient in the form of a pharmaceutically acceptable salt.