Comparison of [11C]diprenorphine and [11C]carfentanil in vivo binding to opiate receptors in man using a dual detector system.
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.
Villemagne
V L
VL
Division of Nuclear Medicine, Johns Hopkins Medical Institutions, Baltimore, MD 21205-2179.
Frost
J J
JJ
Dannals
R F
RF
Lever
J R
JR
Tanada
S
S
Natarajan
T K
TK
Wilson
A A
AA
Ravert
H T
HT
Wagner
H N
HN
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
D000701:Analgesics, Opioid; D011957:Receptors, Opioid; D017450:Receptors, Opioid, mu; D004174:Diprenorphine; D009270:Naloxone; C017114:carfentanil; D005283:Fentanyl