title: Comparison of [11C]diprenorphine and [11C]carfentanil in vivo binding to opiate receptors in man using a dual detector system.
abstract: A simple dual detector coincidence system was used to measure the binding of [11C]carfentanil and [11C]diprenorphine to opiate receptors in normal volunteers before and after the administration of naloxone. Total radioactivity without naloxone and the ratio of total/non-specific radioactivity was 2 times greater for [11C]diprenorphine than [11C]carfentanil. The dose of naloxone required to maximally block specific [11C]diprenorphine binding was 10 times that for [11C]carfentanil, indicating that [11C]diprenorphine labels opiate receptor subtypes in addition to mu opiate receptors.
authors.affiliation: Division of Nuclear Medicine, Johns Hopkins Medical Institutions, Baltimore, MD 21205-2179.
authors.forename: V L
authors.initials: VL
authors.lastname: Villemagne
authors.forename: J J
authors.initials: JJ
authors.lastname: Frost
authors.forename: R F
authors.initials: RF
authors.lastname: Dannals
authors.forename: J R
authors.initials: JR
authors.lastname: Lever
authors.forename: S
authors.initials: S
authors.lastname: Tanada
authors.forename: T K
authors.initials: TK
authors.lastname: Natarajan
authors.forename: A A
authors.initials: AA
authors.lastname: Wilson
authors.forename: H T
authors.initials: HT
authors.lastname: Ravert
authors.forename: H N
authors.initials: HN
authors.lastname: Wagner
mesh_terms: D000701:Analgesics, Opioid / Q000378:metabolism*; D001665:Binding Sites; D004174:Diprenorphine / Q000378:metabolism*; D004305:Dose-Response Relationship, Drug; D005283:Fentanyl / Q000031:analogs & derivatives* / Q000378:metabolism; D005720:Gamma Rays; D006801:Humans; D009270:Naloxone / Q000494:pharmacology; D011957:Receptors, Opioid / Q000378:metabolism*; D017450:Receptors, Opioid, mu / Q000378:metabolism
chemical_list: D000701:Analgesics, Opioid; D011957:Receptors, Opioid; D017450:Receptors, Opioid, mu; D004174:Diprenorphine; D009270:Naloxone; C017114:carfentanil; D005283:Fentanyl