3H-diprenorphine is selective for mu opiate receptors in vivo.
The displacement of 3H-diprenorphine from opiate receptors by mu-selective opiates was measured in the mouse striatum and thalamus in vivo. In addition, the regional distribution of opiate receptor binding using 3H-diprenorphine, 3H-naloxone and 3H-lofentanil was measured. The displacement of 3H-diprenorphine by naloxone and carfentanil in vivo showed no differences in the striatum and thalamus suggesting that 3H-diprenorphine binds only to one opiate receptor subtype in vivo. This finding is substantiated by the observation that the mu selective ligands 3H-naloxone and 3H-lofentanil have the same in vivo distribution of receptor binding as 3H-diprenorphine. The implication of these findings for PET imaging of opiate receptor subtypes is discussed.
D000818:Animals; D001667:Binding, Competitive; D003342:Corpus Striatum / Q000378:metabolism*; D004174:Diprenorphine / Q000378:metabolism*; D005283:Fentanyl / Q000031:analogs & derivatives / Q000494:pharmacology; D007700:Kinetics; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D009019:Morphinans / Q000378:metabolism*; D009270:Naloxone / Q000494:pharmacology; D011957:Receptors, Opioid / Q000187:drug effects / Q000378:metabolism*; D017450:Receptors, Opioid, mu; D013788:Thalamus / Q000378:metabolism*; D014316:Tritium
D009019:Morphinans; D011957:Receptors, Opioid; D017450:Receptors, Opioid, mu; D014316:Tritium; D004174:Diprenorphine; D009270:Naloxone; C017114:carfentanil; D005283:Fentanyl