title: Butorphanol: effects of a prototypical agonist-antagonist analgesic on kappa-opioid receptors.
abstract: The opioid analgesic, butorphanol (17-cyclobutylmethyl-3,14-dihydroxymorphinan) tartrate is a prototypical agonist-antagonist opioid analgesic agent whose potential for abuse has been the cause of litigation in the United States. With a published affinity for opioid receptors in vitro of 1:4:25 (mu:delta:kappa), the relative contribution of actions at each of these receptors to the in vivo actions of the drug are an issue of active investigation. A body of evidence has been developed which indicates that a substantial selective action of butorphanol on the kappa-opioid receptor mediates the development of tolerance to butorphanol and cross-tolerance to other opioid agonists; to the production of dependence upon butorphanol, particularly in the rodent; and to compensatory alterations in brain opioid receptor-effector systems. This perspective will identify the current state of understanding of the effects produced by butorphanol on brain opioid receptors, particularly on the kappa-opioid receptor subtype, and on the expression of phosphotyrosyl proteins following chronic treatment with butorphanol.
authors.affiliation: Department of Pharmacology & Toxicology, University of Mississippi Medical Center, Jackson, USA.
authors.forename: Stephen
authors.initials: S
authors.lastname: Commiskey
authors.forename: Lir-Wan
authors.initials: LW
authors.lastname: Fan
authors.forename: Ing K
authors.initials: IK
authors.lastname: Ho
authors.forename: Rob W
authors.initials: RW
authors.lastname: Rockhold
mesh_terms: D000701:Analgesics, Opioid / Q000494:pharmacology*; D000818:Animals; D002077:Butorphanol / Q000494:pharmacology*; D006801:Humans; D017473:Receptors, Opioid, kappa / Q000037:antagonists & inhibitors* / Q000502:physiology; D015398:Signal Transduction / Q000187:drug effects
chemical_list: D000701:Analgesics, Opioid; D017473:Receptors, Opioid, kappa; D002077:Butorphanol