Methods for identifying and using low/non-addictive opioid...

Details Methods for identifying and using low/non-addictive opioid... Methods for identifying and using low/non-addictive opioid...

C - Chemistry, Metallurgy

12

Q

C12Q 1/02 (2006.01) A61K 31/00 (2006.01) A61K 31/485 (2006.01) C07D 489/12 (2006.01) G01N 33/94 (2006.01)

Patent

CA 2145207

The present invention relates to a method of using a bioassay consisting of an electrophysiological method and a cell cul- ture 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 ident- ified 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 dihydroetor- phine of the opioid alkaloid family as low- or non-addictive analgesics and for the treatment of opioid addiction. The present in- vention also relates to the preparation of dihydroetorphine hydrochloride (7a-[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.

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