It was formerly marketed in the U.S. by Eli Lilly under the tradename Novrad (a reversal of Darvon) as an antitussive.

[1][2] Unlike many antitussives, it binds poorly to the sigma-1 receptor.

[3] The presence of two chiral centers in this molecule means that the compound can exist as any of four isomers.

Resolution of that isomer into its optical antipodes showed the d isomer to be the active analgesic; this is now denoted as propoxyphene.

The l isomer is almost devoid of analgesic activity; the compound does, however, show useful antitussive activity and is named levopropoxyphene.