Partial opioids. Medications for the treatment of pain and drug abuse.
Pentazocine and cyclazocine are two benzomorphans that were synthesized by the late Sydney Archer in 1962. These benzomorphans were synthesized as part of an effort to develop analgesics with little or no abuse potential. Pentazocine is used as an analgesic, often in individuals who have sever pain or in those who have drug-abuse problems. Cyclazocine is a low-liability analgesic and potential therapeutic for the treatment of drug abuse. The risk of drug dependence is lower with the benzomorphans, which usually act as partial agonists at the mu opioid receptor and as kappa agonists. In an attempt to synthesize analogs of cyclazocine with increased bioavailability and varying kappa agonist and partial mu agonist properties, a series of 8-amino derivatives of cyclazocine were synthesized. These compounds were characterized in radioligand binding assays for their affinity and selectivity for the mu, delta, and kappa opioid receptors. Mouse antinociceptive tests were used to characterize the agonist and antagonist properties of each compound at the mu, delta and kappa receptors.
Department of Pharmacology and Physiology, University of Rochester, School of Medicine and Dentistry, New York 14642-8711, USA. jean_bidlackj@urmc.rochester.edu
J M
JM
Bidlack
J P
JP
McLaughlin
M P
MP
Wentland
D000700:Analgesics / Q000627:therapeutic use*; D000818:Animals; D003496:Cyclazocine / Q000031:analogs & derivatives / Q000627:therapeutic use*; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D010146:Pain / Q000188:drug therapy*; D010423:Pentazocine / Q000627:therapeutic use*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D019966:Substance-Related Disorders / Q000188:drug therapy*
D000700:Analgesics; D003496:Cyclazocine; D010423:Pentazocine